{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,20]],"date-time":"2026-08-20T10:16:03Z","timestamp":1787220963144,"version":"build-2736575974"},"reference-count":301,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2019,12,1]],"date-time":"2019-12-01T00:00:00Z","timestamp":1575158400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2019,12,1]],"date-time":"2019-12-01T00:00:00Z","timestamp":1575158400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2019,9,11]],"date-time":"2019-09-11T00:00:00Z","timestamp":1568160000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/100008992","name":"Yantai University","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100008992","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100013152","name":"Shanghai Institute of Materia Medica, Chinese Academy of Sciences","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100013152","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Pharmacology & Therapeutics"],"published-print":{"date-parts":[[2019,12]]},"DOI":"10.1016\/j.pharmthera.2019.107406","type":"journal-article","created":{"date-parts":[[2019,9,12]],"date-time":"2019-09-12T12:00:23Z","timestamp":1568289623000},"page":"107406","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":41,"special_numbering":"C","title":["Targeting epigenetic machinery: Emerging novel allosteric inhibitors"],"prefix":"10.1016","volume":"204","author":[{"given":"Fei","family":"Ye","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jing","family":"Huang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hongbo","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Cheng","family":"Luo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kehao","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.pharmthera.2019.107406_bib0005","doi-asserted-by":"crossref","first-page":"6015","DOI":"10.1021\/acs.jmedchem.9b00021","article-title":"Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction","volume":"62","author":"Aguilar","year":"2019","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0010","doi-asserted-by":"crossref","DOI":"10.1038\/ncomms10204","article-title":"Epigenetic switch drives the conversion of fibroblasts into proinvasive cancer-associated fibroblasts","volume":"6","author":"Albrengues","year":"2015","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0015","doi-asserted-by":"crossref","first-page":"1000","DOI":"10.1038\/leu.2012.356","article-title":"The role of HOX genes in normal hematopoiesis and acute leukemia","volume":"27","author":"Alharbi","year":"2013","journal-title":"Leukemia"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0020","doi-asserted-by":"crossref","first-page":"22357","DOI":"10.1074\/jbc.M116.752626","article-title":"Targeted Disruption of the Interaction between WD-40 Repeat Protein 5 (WDR5) and Mixed Lineage Leukemia (MLL)\/SET1 Family Proteins Specifically Inhibits MLL1 and SETd1A Methyltransferase Complexes","volume":"291","author":"Alicea-Velazquez","year":"2016","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0025","doi-asserted-by":"crossref","first-page":"2113","DOI":"10.4161\/cc.25163","article-title":"Three-dimensional culture sensitizes epithelial ovarian cancer cells to EZH2 methyltransferase inhibition","volume":"12","author":"Amatangelo","year":"2013","journal-title":"Cell Cycle"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0030","doi-asserted-by":"crossref","first-page":"32412","DOI":"10.1074\/jbc.M805918200","article-title":"A thermodynamic model for Nap1-histone interactions","volume":"283","author":"Andrews","year":"2008","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0035","doi-asserted-by":"crossref","first-page":"1790","DOI":"10.1111\/j.1742-4658.2010.07606.x","article-title":"Mixed lineage leukemia: roles in gene expression, hormone signaling and mRNA processing","volume":"277","author":"Ansari","year":"2010","journal-title":"The FEBS Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0040","doi-asserted-by":"crossref","first-page":"3506","DOI":"10.1093\/nar\/29.17.3506","article-title":"Enzymatic properties of de novo-type mouse DNA (cytosine-5) methyltransferases","volume":"29","author":"Aoki","year":"2001","journal-title":"Nucleic Acids Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0045","doi-asserted-by":"crossref","first-page":"37","DOI":"10.1038\/s41594-017-0003-7","article-title":"Cryo-EM structures of the human INO80 chromatin-remodeling complex","volume":"25","author":"Aramayo","year":"2018","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0050","doi-asserted-by":"crossref","first-page":"818","DOI":"10.1038\/nature07249","article-title":"Recognition of hemi-methylated DNA by the SRA protein UHRF1 by a base-flipping mechanism","volume":"455","author":"Arita","year":"2008","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0055","doi-asserted-by":"crossref","first-page":"704","DOI":"10.1016\/j.jtho.2016.12.011","article-title":"Small cell lung cancer exhibits frequent inactivating mutations in the histone methyltransferase KMT2D\/MLL2: CALGB 151111 (Alliance)","volume":"12","author":"Augert","year":"2017","journal-title":"Journal of Thoracic Oncology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0060","doi-asserted-by":"crossref","first-page":"822","DOI":"10.1038\/nature07273","article-title":"Structural basis for recognition of hemi-methylated DNA by the SRA domain of human UHRF1","volume":"455","author":"Avvakumov","year":"2008","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0065","doi-asserted-by":"crossref","first-page":"391","DOI":"10.1038\/s41586-018-0021-6","article-title":"Structure and regulation of the human INO80-nucleosome complex","volume":"556","author":"Ayala","year":"2018","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0070","doi-asserted-by":"crossref","first-page":"5695","DOI":"10.1038\/sj.onc.1204639","article-title":"Molecular mechanisms of leukemogenesis mediated by MLL fusion proteins","volume":"20","author":"Ayton","year":"2001","journal-title":"Oncogene"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0075","first-page":"E8051","article-title":"Elucidating the druggable interface of protein-protein interactions using fragment docking and coevolutionary analysis","volume":"113","author":"Bai","year":"2016","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0080","doi-asserted-by":"crossref","first-page":"48","DOI":"10.1016\/j.bbrc.2018.10.029","article-title":"MALT1 activation by TRAF6 needs neither BCL10 nor CARD11","volume":"506","author":"Bardet","year":"2018","journal-title":"Biochemical and Biophysical Research Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0085","doi-asserted-by":"crossref","first-page":"161","DOI":"10.1021\/acscombsci.6b00174","article-title":"Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2","volume":"19","author":"Barnash","year":"2017","journal-title":"ACS Combinatorial Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0090","doi-asserted-by":"crossref","first-page":"823","DOI":"10.1016\/j.cell.2007.05.009","article-title":"High-resolution profiling of histone methylations in the human genome","volume":"129","author":"Barski","year":"2007","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0095","doi-asserted-by":"crossref","first-page":"4106","DOI":"10.1074\/jbc.M113.528893","article-title":"The UHRF1 protein stimulates the activity and specificity of the maintenance DNA methyltransferase DNMT1 by an allosteric mechanism","volume":"289","author":"Bashtrykov","year":"2014","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0100","doi-asserted-by":"crossref","first-page":"7650","DOI":"10.1021\/jm3006788","article-title":"Discovery of the first thumb pocket 1 NS5B polymerase inhibitor (BILB 1941) with demonstrated antiviral activity in patients chronically infected with genotype 1 hepatitis C virus (HCV)","volume":"55","author":"Beaulieu","year":"2012","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0105","doi-asserted-by":"crossref","first-page":"677","DOI":"10.1016\/j.ccr.2013.04.011","article-title":"EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation","volume":"23","author":"Beguelin","year":"2013","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0110","doi-asserted-by":"crossref","first-page":"3285","DOI":"10.1038\/emboj.2011.243","article-title":"Recognition of UbcH5c and the nucleosome by the Bmi1\/Ring1b ubiquitin ligase complex","volume":"30","author":"Bentley","year":"2011","journal-title":"The EMBO Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0115","doi-asserted-by":"crossref","first-page":"781","DOI":"10.1101\/gad.1787609","article-title":"An operational definition of epigenetics","volume":"23","author":"Berger","year":"2009","journal-title":"Genes & Development"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0120","doi-asserted-by":"crossref","first-page":"5543","DOI":"10.1038\/sj.onc.1208735","article-title":"CBX7 controls the growth of normal and tumor-derived prostate cells by repressing the Ink4a\/Arf locus","volume":"24","author":"Bernard","year":"2005","journal-title":"Oncogene"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0125","doi-asserted-by":"crossref","first-page":"2560","DOI":"10.1128\/MCB.26.7.2560-2569.2006","article-title":"Mouse polycomb proteins bind differentially to methylated histone H3 and RNA and are enriched in facultative heterochromatin","volume":"26","author":"Bernstein","year":"2006","journal-title":"Molecular and Cellular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0130","first-page":"74","article-title":"Germ-line and acquired mutations of INI1 in atypical teratoid and rhabdoid tumors","volume":"59","author":"Biegel","year":"1999","journal-title":"Cancer Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0135","doi-asserted-by":"crossref","first-page":"5","DOI":"10.1016\/0092-8674(92)90526-I","article-title":"The essentials of DNA methylation","volume":"70","author":"Bird","year":"1992","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0140","doi-asserted-by":"crossref","first-page":"6","DOI":"10.1101\/gad.947102","article-title":"DNA methylation patterns and epigenetic memory","volume":"16","author":"Bird","year":"2002","journal-title":"Genes & Development"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0145","doi-asserted-by":"crossref","first-page":"1445","DOI":"10.1016\/j.cell.2014.05.004","article-title":"Variant PRC1 complex-dependent H2A ubiquitylation drives PRC2 recruitment and polycomb domain formation","volume":"157","author":"Blackledge","year":"2014","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0150","doi-asserted-by":"crossref","first-page":"353","DOI":"10.1021\/ml300467n","article-title":"Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction","volume":"4","author":"Bolshan","year":"2013","journal-title":"ACS Medicinal Chemistry Letters"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0155","doi-asserted-by":"crossref","first-page":"589","DOI":"10.1016\/j.ccell.2015.02.016","article-title":"Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo","volume":"27","author":"Borkin","year":"2015","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0160","doi-asserted-by":"crossref","first-page":"4832","DOI":"10.1021\/acs.jmedchem.8b00071","article-title":"Complexity of Blocking Bivalent Protein-Protein Interactions: Development of a Highly Potent Inhibitor of the Menin-Mixed-Lineage Leukemia Interaction","volume":"61","author":"Borkin","year":"2018","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0165","doi-asserted-by":"crossref","first-page":"892","DOI":"10.1021\/acs.jmedchem.5b01305","article-title":"Property focused structure-based optimization of small molecule inhibitors of the protein-protein interaction between menin and mixed lineage leukemia (MLL)","volume":"59","author":"Borkin","year":"2016","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0170","doi-asserted-by":"crossref","first-page":"1760","DOI":"10.1126\/science.1147939","article-title":"UHRF1 plays a role in maintaining DNA methylation in mammalian cells","volume":"317","author":"Bostick","year":"2007","journal-title":"Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0175","doi-asserted-by":"crossref","first-page":"5323","DOI":"10.1093\/emboj\/cdg542","article-title":"EZH2 is downstream of the pRB-E2F pathway, essential for proliferation and amplified in cancer","volume":"22","author":"Bracken","year":"2003","journal-title":"The EMBO Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0180","doi-asserted-by":"crossref","first-page":"1751","DOI":"10.1038\/sj.leu.2403910","article-title":"Histone deacetylases in acute myeloid leukaemia show a distinctive pattern of expression that changes selectively in response to deacetylase inhibitors","volume":"19","author":"Bradbury","year":"2005","journal-title":"Leukemia"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0185","doi-asserted-by":"crossref","first-page":"22","DOI":"10.1021\/cb500996u","article-title":"Small molecule inhibitors of bromodomain-acetyl-lysine interactions","volume":"10","author":"Brand","year":"2015","journal-title":"ACS Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0190","article-title":"Polycomb complexes in X chromosome inactivation","volume":"372","author":"Brockdorff","year":"2017","journal-title":"Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0195","doi-asserted-by":"crossref","first-page":"1720","DOI":"10.1182\/blood-2013-02-483495","article-title":"Essential role of BRG, the ATPase subunit of BAF chromatin remodeling complexes, in leukemia maintenance","volume":"123","author":"Buscarlet","year":"2014","journal-title":"Blood"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0200","doi-asserted-by":"crossref","first-page":"247","DOI":"10.1016\/j.molcel.2013.12.001","article-title":"Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia","volume":"53","author":"Cao","year":"2014","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0205","doi-asserted-by":"crossref","first-page":"57","DOI":"10.1016\/j.molcel.2004.06.020","article-title":"SUZ12 is required for both the histone methyltransferase activity and the silencing function of the EED-EZH2 complex","volume":"15","author":"Cao","year":"2004","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0210","doi-asserted-by":"crossref","first-page":"1471","DOI":"10.1242\/dev.053652","article-title":"Polycomblike 2 facilitates the recruitment of PRC2 Polycomb group complexes to the inactive X chromosome and to target loci in embryonic stem cells","volume":"138","author":"Casanova","year":"2011","journal-title":"Development"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0215","doi-asserted-by":"crossref","first-page":"620","DOI":"10.1038\/nature01042","article-title":"FGFR-related gene nou-darake restricts brain tissues to the head region of planarians","volume":"419","author":"Cebria","year":"2002","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0220","doi-asserted-by":"crossref","first-page":"622","DOI":"10.1016\/j.cmet.2017.01.009","article-title":"Converting Adult Pancreatic Islet alpha Cells into beta Cells by Targeting Both Dnmt1 and Arx","volume":"25","author":"Chakravarthy","year":"2017","journal-title":"Cell Metabolism"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0225","doi-asserted-by":"crossref","first-page":"86","DOI":"10.1016\/j.ccr.2010.10.035","article-title":"EZH2 promotes expansion of breast tumor initiating cells through activation of RAF1-beta-catenin signaling","volume":"19","author":"Chang","year":"2011","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0230","doi-asserted-by":"crossref","first-page":"673","DOI":"10.1016\/j.exphem.2015.05.012","article-title":"Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyond","volume":"43","author":"Chen","year":"2015","journal-title":"Experimental Hematology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0235","doi-asserted-by":"crossref","first-page":"840","DOI":"10.1016\/j.molcel.2018.01.039","article-title":"Unique Structural Platforms of Suz12 Dictate Distinct Classes of PRC2 for Chromatin Binding","volume":"69","author":"Chen","year":"2018","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0240","doi-asserted-by":"crossref","first-page":"391","DOI":"10.1038\/ng1982","article-title":"Complete inactivation of DNMT1 leads to mitotic catastrophe in human cancer cells","volume":"39","author":"Chen","year":"2007","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0245","doi-asserted-by":"crossref","first-page":"380","DOI":"10.1016\/j.bioorg.2017.11.018","article-title":"Design, synthesis, and initial evaluation of affinity-based small molecular probe for detection of WDR5","volume":"76","author":"Chen","year":"2018","journal-title":"Bioorganic Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0250","doi-asserted-by":"crossref","first-page":"755","DOI":"10.1016\/j.ccell.2017.05.002","article-title":"MLL2, Not MLL1, Plays a Major Role in Sustaining MLL-Rearranged Acute Myeloid Leukemia","volume":"31","author":"Chen","year":"2017","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0255","doi-asserted-by":"crossref","first-page":"148","DOI":"10.1038\/nature18621","article-title":"Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases","volume":"535","author":"Chen","year":"2016","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0260","doi-asserted-by":"crossref","first-page":"7023","DOI":"10.1038\/ncomms8023","article-title":"Molecular mechanism for USP7-mediated DNMT1 stabilization by acetylation","volume":"6","author":"Cheng","year":"2015","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0265","doi-asserted-by":"crossref","first-page":"341","DOI":"10.1016\/j.str.2008.01.004","article-title":"Mammalian DNA methyltransferases: a structural perspective","volume":"16","author":"Cheng","year":"2008","journal-title":"Structure"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0270","doi-asserted-by":"crossref","first-page":"198","DOI":"10.1038\/nrd746","article-title":"Allosteric binding sites on cell-surface receptors: novel targets for drug discovery","volume":"1","author":"Christopoulos","year":"2002","journal-title":"Nature Reviews. Drug Discovery"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0275","doi-asserted-by":"crossref","DOI":"10.7554\/eLife.00005","article-title":"Molecular architecture of human polycomb repressive complex 2","volume":"1","author":"Ciferri","year":"2012","journal-title":"Elife"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0280","doi-asserted-by":"crossref","first-page":"810","DOI":"10.1158\/0008-5472.CAN-11-1052","article-title":"SMYD3 promotes cancer invasion by epigenetic upregulation of the metalloproteinase MMP-9","volume":"72","author":"Cock-Rada","year":"2012","journal-title":"Cancer Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0285","doi-asserted-by":"crossref","first-page":"354","DOI":"10.1097\/MOH.0000000000000245","article-title":"Deregulation of the HOXA9\/MEIS1 axis in acute leukemia","volume":"23","author":"Collins","year":"2016","journal-title":"Current Opinion in Hematology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0290","doi-asserted-by":"crossref","first-page":"803","DOI":"10.1038\/nrc.2016.83","article-title":"Maintaining cell identity: PRC2-mediated regulation of transcription and cancer","volume":"16","author":"Comet","year":"2016","journal-title":"Nature Reviews. Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0295","doi-asserted-by":"crossref","DOI":"10.1038\/ncomms13661","article-title":"Jarid2 binds mono-ubiquitylated H2A lysine 119 to mediate crosstalk between Polycomb complexes PRC1 and PRC2","volume":"7","author":"Cooper","year":"2016","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0300","doi-asserted-by":"crossref","first-page":"698","DOI":"10.1038\/nsmb1116","article-title":"Molecular recognition of histone H3 by the WD40 protein WDR5","volume":"13","author":"Couture","year":"2006","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0305","doi-asserted-by":"crossref","first-page":"27275","DOI":"10.1074\/jbc.M112.364125","article-title":"Structural basis for WDR5 interaction (Win) motif recognition in human SET1 family histone methyltransferases","volume":"287","author":"Dharmarajan","year":"2012","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0310","doi-asserted-by":"crossref","first-page":"713","DOI":"10.1038\/nsmb1128","article-title":"Regulation of MLL1 H3K4 methyltransferase activity by its core components","volume":"13","author":"Dou","year":"2006","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0315","doi-asserted-by":"crossref","first-page":"ra80","DOI":"10.1126\/scisignal.2001462","article-title":"DNMT1 stability is regulated by proteins coordinating deubiquitination and acetylation-driven ubiquitination","volume":"3","author":"Du","year":"2010","journal-title":"Science Signaling"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0320","doi-asserted-by":"crossref","first-page":"716","DOI":"10.1016\/j.molcel.2014.05.015","article-title":"Cancer epigenetics: tumor heterogeneity, plasticity of stem-like states, and drug resistance","volume":"54","author":"Easwaran","year":"2014","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0325","doi-asserted-by":"crossref","first-page":"1181","DOI":"10.1038\/sj.embor.7400295","article-title":"Replication-independent chromatin loading of Dnmt1 during G2 and M phases","volume":"5","author":"Easwaran","year":"2004","journal-title":"EMBO Reports"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0330","doi-asserted-by":"crossref","first-page":"577","DOI":"10.1038\/nrd4336","article-title":"The discovery of first-in-class drugs: origins and evolution","volume":"13","author":"Eder","year":"2014","journal-title":"Nature Reviews. Drug Discovery"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0335","article-title":"PCGF6-PRC1 suppresses premature differentiation of mouse embryonic stem cells by regulating germ cell-related genes","volume":"6","author":"Endoh","year":"2017","journal-title":"Elife"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0340","doi-asserted-by":"crossref","first-page":"722","DOI":"10.1038\/ng.621","article-title":"Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders","volume":"42","author":"Ernst","year":"2010","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0345","doi-asserted-by":"crossref","first-page":"649","DOI":"10.1080\/17425255.2018.1483336","article-title":"Pharmacokinetic and pharmacodynamic evaluation of daclatasvir, asunaprevir plus beclabuvir as a fixed-dose co-formulation for the treatment of hepatitis C","volume":"14","author":"Esposito","year":"2018","journal-title":"Expert Opinion on Drug Metabolism & Toxicology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0350","doi-asserted-by":"crossref","first-page":"564","DOI":"10.1093\/jnci\/92.7.564","article-title":"Promoter hypermethylation and BRCA1 inactivation in sporadic breast and ovarian tumors","volume":"92","author":"Esteller","year":"2000","journal-title":"Journal of the National Cancer Institute"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0355","doi-asserted-by":"crossref","first-page":"689","DOI":"10.1016\/S0002-9440(10)63156-2","article-title":"Increased DNA methyltransferase 1 (DNMT1) protein expression correlates significantly with poorer tumor differentiation and frequent DNA hypermethylation of multiple CpG islands in gastric cancers","volume":"164","author":"Etoh","year":"2004","journal-title":"The American Journal of Pathology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0360","doi-asserted-by":"crossref","first-page":"87","DOI":"10.1016\/j.stem.2007.04.001","article-title":"shRNA knockdown of Bmi-1 reveals a critical role for p21-Rb pathway in NSC self-renewal during development","volume":"1","author":"Fasano","year":"2007","journal-title":"Cell Stem Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0365","doi-asserted-by":"crossref","first-page":"8355","DOI":"10.1093\/nar\/gkr528","article-title":"The USP7\/Dnmt1 complex stimulates the DNA methylation activity of Dnmt1 and regulates the stability of UHRF1","volume":"39","author":"Felle","year":"2011","journal-title":"Nucleic Acids Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0370","doi-asserted-by":"crossref","first-page":"337","DOI":"10.1038\/nrd4286","article-title":"Targeting bromodomains: epigenetic readers of lysine acetylation","volume":"13","author":"Filippakopoulos","year":"2014","journal-title":"Nature Reviews. Drug Discovery"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0375","doi-asserted-by":"crossref","first-page":"24250","DOI":"10.1074\/jbc.274.34.24250","article-title":"Down-regulation of human DNA-(cytosine-5) methyltransferase induces cell cycle regulators p16(ink4A) and p21(WAF\/Cip1) by distinct mechanisms","volume":"274","author":"Fournel","year":"1999","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0380","article-title":"Abstract LB-A27: A novel small molecule menin-MLL inhibitor for potential treatment of MLL-rearranged leukemias and NPM1\/DNMT3A-mutant AML","volume":"17","author":"Francis Burrows","year":"2018","journal-title":"Molecular Cancer Therapeutics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0385","doi-asserted-by":"crossref","first-page":"1399","DOI":"10.1136\/gut.2009.180711","article-title":"HDAC2 mediates therapeutic resistance of pancreatic cancer cells via the BH3-only protein NOXA","volume":"58","author":"Fritsche","year":"2009","journal-title":"Gut"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0390","doi-asserted-by":"crossref","first-page":"3514","DOI":"10.1038\/s41598-019-40314-1","article-title":"DESTINI: A deep-learning approach to contact-driven protein structure prediction","volume":"9","author":"Gao","year":"2019","journal-title":"Scientific Reports"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0395","doi-asserted-by":"crossref","first-page":"344","DOI":"10.1016\/j.molcel.2012.01.002","article-title":"PCGF homologs, CBX proteins, and RYBP define functionally distinct PRC1 family complexes","volume":"45","author":"Gao","year":"2012","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0400","doi-asserted-by":"crossref","first-page":"118","DOI":"10.1038\/nchembio.2528","article-title":"Discovery and characterization of highly potent and selective allosteric USP7 inhibitors","volume":"14","author":"Gavory","year":"2018","journal-title":"Nature Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0405","doi-asserted-by":"crossref","first-page":"4800","DOI":"10.1021\/acs.jmedchem.6b00012","article-title":"Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit","volume":"59","author":"Gerstenberger","year":"2016","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0410","doi-asserted-by":"crossref","first-page":"2478","DOI":"10.1021\/acs.jmedchem.5b01630","article-title":"Structure-based optimization of a small molecule antagonist of the interaction between WD repeat-containing protein 5 (WDR5) and mixed-lineage leukemia 1 (MLL1)","volume":"59","author":"Getlik","year":"2016","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0415","doi-asserted-by":"crossref","first-page":"632","DOI":"10.1016\/j.tcb.2014.06.005","article-title":"PRC1 complex diversity: where is it taking us?","volume":"24","author":"Gil","year":"2014","journal-title":"Trends in Cell Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0420","doi-asserted-by":"crossref","first-page":"4057","DOI":"10.1128\/MCB.00400-09","article-title":"SWI\/SNF and Asf1p cooperate to displace histones during induction of the saccharomyces cerevisiae HO promoter","volume":"29","author":"Gkikopoulos","year":"2009","journal-title":"Molecular and Cellular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0425","doi-asserted-by":"crossref","first-page":"1087","DOI":"10.1038\/sj.bjc.6603024","article-title":"Epigenetics as a mechanism driving polygenic clinical drug resistance","volume":"94","author":"Glasspool","year":"2006","journal-title":"British Journal of Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0430","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0167379","article-title":"Identification of a Novel Inhibitory Allosteric Site in p38alpha","volume":"11","author":"Gomez-Gutierrez","year":"2016","journal-title":"PLoS One"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0435","doi-asserted-by":"crossref","first-page":"131","DOI":"10.1038\/nrd.2016.213","article-title":"DNA-encoded chemistry: enabling the deeper sampling of chemical space","volume":"16","author":"Goodnow","year":"2017","journal-title":"Nature Reviews. Drug Discovery"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0440","doi-asserted-by":"crossref","first-page":"571","DOI":"10.1038\/nchembio.1859","article-title":"Pharmacological targeting of the Wdr5-MLL interaction in C\/EBPalpha N-terminal leukemia","volume":"11","author":"Grebien","year":"2015","journal-title":"Nature Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0445","doi-asserted-by":"crossref","first-page":"40690","DOI":"10.1074\/jbc.M110.172783","article-title":"Molecular basis of the mixed lineage leukemia-menin interaction: implications for targeting mixed lineage leukemias","volume":"285","author":"Grembecka","year":"2010","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0450","doi-asserted-by":"crossref","first-page":"277","DOI":"10.1038\/nchembio.773","article-title":"Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia","volume":"8","author":"Grembecka","year":"2012","journal-title":"Nature Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0455","doi-asserted-by":"crossref","first-page":"869","DOI":"10.1038\/nature02935","article-title":"Morning and evening peaks of activity rely on different clock neurons of the Drosophila brain","volume":"431","author":"Grima","year":"2004","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0460","doi-asserted-by":"crossref","first-page":"20477","DOI":"10.1074\/jbc.M114.551119","article-title":"Allosteric inhibition of human immunodeficiency virus integrase: late block during viral replication and abnormal multimerization involving specific protein domains","volume":"289","author":"Gupta","year":"2014","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0465","doi-asserted-by":"crossref","first-page":"247","DOI":"10.2217\/epi.14.80","article-title":"Genetic alterations of DNA methylation machinery in human diseases","volume":"7","author":"Hamidi","year":"2015","journal-title":"Epigenomics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0470","doi-asserted-by":"crossref","first-page":"137","DOI":"10.1016\/j.molcel.2006.03.018","article-title":"Structural basis for the specific recognition of methylated histone H3 lysine 4 by the WD-40 protein WDR5","volume":"22","author":"Han","year":"2006","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0475","doi-asserted-by":"crossref","first-page":"1306","DOI":"10.1016\/j.str.2007.08.007","article-title":"Structural basis of EZH2 recognition by EED","volume":"15","author":"Han","year":"2007","journal-title":"Structure"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0480","doi-asserted-by":"crossref","DOI":"10.7554\/eLife.17101","article-title":"Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1","volume":"5","author":"Harrison","year":"2016","journal-title":"Elife"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0485","doi-asserted-by":"crossref","first-page":"826","DOI":"10.1038\/nature07280","article-title":"The SRA domain of UHRF1 flips 5-methylcytosine out of the DNA helix","volume":"455","author":"Hashimoto","year":"2008","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0490","doi-asserted-by":"crossref","first-page":"1332","DOI":"10.1002\/ijc.25151","article-title":"Type-specific roles of histone deacetylase (HDAC) overexpression in ovarian carcinoma: HDAC1 enhances cell proliferation and HDAC3 stimulates cell migration with downregulation of E-cadherin","volume":"127","author":"Hayashi","year":"2010","journal-title":"International Journal of Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0495","doi-asserted-by":"crossref","first-page":"1543","DOI":"10.1021\/jm401868d","article-title":"High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction","volume":"57","author":"He","year":"2014","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0500","doi-asserted-by":"crossref","first-page":"389","DOI":"10.1038\/nchembio.2306","article-title":"The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex","volume":"13","author":"He","year":"2017","journal-title":"Nature Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0505","first-page":"722","article-title":"Hypermethylation-associated inactivation indicates a tumor suppressor role for p15INK4B","volume":"56","author":"Herman","year":"1996","journal-title":"Cancer Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0510","doi-asserted-by":"crossref","first-page":"9700","DOI":"10.1073\/pnas.91.21.9700","article-title":"Silencing of the VHL tumor-suppressor gene by DNA methylation in renal carcinoma","volume":"91","author":"Herman","year":"1994","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0515","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0011333","article-title":"Disruption of Dnmt1\/PCNA\/UHRF1 interactions promotes tumorigenesis from human and mice glial cells","volume":"5","author":"Hervouet","year":"2010","journal-title":"PLoS One"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0520","doi-asserted-by":"crossref","DOI":"10.3390\/molecules23102520","article-title":"Artificial intelligence in drug design","volume":"23","author":"Hessler","year":"2018","journal-title":"Molecules"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0525","doi-asserted-by":"crossref","first-page":"2496","DOI":"10.1038\/s41467-018-04950-x","article-title":"KMT2D\/MLL2 inactivation is associated with recurrence in adult-type granulosa cell tumors of the ovary","volume":"9","author":"Hillman","year":"2018","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0530","doi-asserted-by":"crossref","first-page":"1139","DOI":"10.1128\/MCB.06441-11","article-title":"RYBP represses endogenous retroviruses and preimplantation- and germ line-specific genes in mouse embryonic stem cells","volume":"32","author":"Hisada","year":"2012","journal-title":"Molecular and Cellular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0535","doi-asserted-by":"crossref","first-page":"791","DOI":"10.1038\/ng.2643","article-title":"The mutational landscape of adenoid cystic carcinoma","volume":"45","author":"Ho","year":"2013","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0540","doi-asserted-by":"crossref","first-page":"531","DOI":"10.1016\/j.tibs.2017.04.003","article-title":"Mechanisms Regulating PRC2 Recruitment and Enzymatic Activity","volume":"42","author":"Holoch","year":"2017","journal-title":"Trends in Biochemical Sciences"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0545","doi-asserted-by":"crossref","first-page":"542","DOI":"10.1038\/nature10806","article-title":"The same pocket in menin binds both MLL and JUND but has opposite effects on transcription","volume":"482","author":"Huang","year":"2012","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0550","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pgen.1002576","article-title":"Polycomb-like 3 promotes polycomb repressive complex 2 binding to CpG islands and embryonic stem cell self-renewal","volume":"8","author":"Hunkapiller","year":"2012","journal-title":"PLoS Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0555","doi-asserted-by":"crossref","first-page":"761","DOI":"10.1016\/j.molcel.2010.08.013","article-title":"Loss of miR-200 inhibition of Suz12 leads to polycomb-mediated repression required for the formation and maintenance of cancer stem cells","volume":"39","author":"Iliopoulos","year":"2010","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0560","doi-asserted-by":"crossref","first-page":"350","DOI":"10.1016\/j.molcel.2017.09.037","article-title":"Structure of the Dnmt1 reader module Complexed with a unique two-mono-ubiquitin mark on histone H3 reveals the basis for DNA methylation maintenance","volume":"68","author":"Ishiyama","year":"2017","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0565","doi-asserted-by":"crossref","first-page":"164","DOI":"10.1038\/16476","article-title":"The oncogene and Polycomb-group gene bmi-1 regulates cell proliferation and senescence through the ink4a locus","volume":"397","author":"Jacobs","year":"1999","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0570","doi-asserted-by":"crossref","first-page":"aac4383","DOI":"10.1126\/science.aac4383","article-title":"Structural basis of histone H3K27 trimethylation by an active polycomb repressive complex 2","volume":"350","author":"Jiao","year":"2015","journal-title":"Science (New York, N.Y.)"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0575","doi-asserted-by":"crossref","DOI":"10.1126\/sciadv.1500447","article-title":"Mammalian SWI\/SNF chromatin remodeling complexes and cancer: Mechanistic insights gained from human genomics","volume":"1","author":"Kadoch","year":"2015","journal-title":"Science Advances"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0580","first-page":"10132","article-title":"Interdependence of PRC1 and PRC2 for recruitment to polycomb response elements","volume":"44","author":"Kahn","year":"2016","journal-title":"Nucleic Acids Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0585","doi-asserted-by":"crossref","first-page":"624","DOI":"10.1124\/jpet.112.200915","article-title":"ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization","volume":"344","author":"Kalinichev","year":"2013","journal-title":"The Journal of Pharmacology and Experimental Therapeutics"},{"issue":"4","key":"10.1016\/j.pharmthera.2019.107406_bib0590","first-page":"271","article-title":"Conserved threonine 1505 in the catalytic domain stabilizes mouse DNA methyltransferase 1","volume":"162","author":"Kanada","year":"2017","journal-title":"Journal of Biochemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0595","doi-asserted-by":"crossref","first-page":"705","DOI":"10.1128\/MCB.01598-07","article-title":"ICBP90, a novel methyl K9 H3 binding protein linking protein ubiquitination with heterochromatin formation","volume":"28","author":"Karagianni","year":"2008","journal-title":"Molecular and Cellular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0600","doi-asserted-by":"crossref","first-page":"4818","DOI":"10.1021\/acs.jmedchem.6b01796","article-title":"Discovery of a highly potent, cell-permeable macrocyclic peptidomimetic (MM-589) targeting the WD repeat domain 5 protein (WDR5)-mixed lineage leukemia (MLL) protein-protein interaction","volume":"60","author":"Karatas","year":"2017","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0605","doi-asserted-by":"crossref","first-page":"5179","DOI":"10.1021\/jm100139b","article-title":"Analysis of the binding of mixed lineage leukemia 1 (MLL1) and histone 3 peptides to WD repeat domain 5 (WDR5) for the design of inhibitors of the MLL1-WDR5 interaction","volume":"53","author":"Karatas","year":"2010","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0610","doi-asserted-by":"crossref","first-page":"669","DOI":"10.1021\/ja306028q","article-title":"High-affinity, small-molecule peptidomimetic inhibitors of MLL1\/WDR5 protein-protein interaction","volume":"135","author":"Karatas","year":"2013","journal-title":"Journal of the American Chemical Society"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0615","doi-asserted-by":"crossref","first-page":"940","DOI":"10.1126\/science.aar5700","article-title":"Structures of human PRC2 with its cofactors AEBP2 and JARID2","volume":"359","author":"Kasinath","year":"2018","journal-title":"Science (New York, N.Y.)"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0620","doi-asserted-by":"crossref","first-page":"521","DOI":"10.1074\/jbc.M110.191411","article-title":"Recognition and specificity determinants of the human cbx chromodomains","volume":"286","author":"Kaustov","year":"2011","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0625","doi-asserted-by":"crossref","first-page":"537","DOI":"10.1111\/j.1365-2141.2010.08127.x","article-title":"Blockade of the MEK\/ERK signalling cascade by AS703026, a novel selective MEK1\/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo","volume":"149","author":"Kim","year":"2010","journal-title":"British Journal of Haematology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0630","doi-asserted-by":"crossref","first-page":"353","DOI":"10.1038\/ncb2701","article-title":"Polycomb Cbx family members mediate the balance between haematopoietic stem cell self-renewal and differentiation","volume":"15","author":"Klauke","year":"2013","journal-title":"Nature Cell Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0635","doi-asserted-by":"crossref","first-page":"595","DOI":"10.1038\/ng.830","article-title":"Mutations in DNMT1 cause hereditary sensory neuropathy with dementia and hearing loss","volume":"43","author":"Klein","year":"2011","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0640","doi-asserted-by":"crossref","first-page":"682","DOI":"10.1038\/nsmb.3248","article-title":"The dynamic interactome and genomic targets of Polycomb complexes during stem-cell differentiation","volume":"23","author":"Kloet","year":"2016","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0645","doi-asserted-by":"crossref","first-page":"1574","DOI":"10.1016\/j.bmcl.2005.12.051","article-title":"1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors","volume":"16","author":"Klopfenstein","year":"2006","journal-title":"Bioorganic & Medicinal Chemistry Letters"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0650","doi-asserted-by":"crossref","first-page":"459","DOI":"10.1038\/s41571-018-0004-4","article-title":"Analysis of DNA methylation in cancer: location revisited","volume":"15","author":"Koch","year":"2018","journal-title":"Nature Reviews. Clinical Oncology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0655","doi-asserted-by":"crossref","first-page":"9512","DOI":"10.1021\/jm501230c","article-title":"Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2","volume":"57","author":"Kong","year":"2014","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0660","doi-asserted-by":"crossref","first-page":"693","DOI":"10.1016\/j.cell.2007.02.005","article-title":"Chromatin modifications and their function","volume":"128","author":"Kouzarides","year":"2007","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0665","doi-asserted-by":"crossref","first-page":"29","DOI":"10.1038\/nm.3418","article-title":"Self-renewal as a therapeutic target in human colorectal cancer","volume":"20","author":"Kreso","year":"2014","journal-title":"Nature Medicine"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0670","doi-asserted-by":"crossref","first-page":"823","DOI":"10.1038\/nrc2253","article-title":"MLL translocations, histone modifications and leukaemia stem-cell development","volume":"7","author":"Krivtsov","year":"2007","journal-title":"Nature Reviews Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0675","doi-asserted-by":"crossref","first-page":"650","DOI":"10.1021\/acs.jmedchem.7b01375","volume":"61","author":"Kung","year":"2018","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0680","doi-asserted-by":"crossref","first-page":"204","DOI":"10.1038\/nrg2719","article-title":"Establishing, maintaining and modifying DNA methylation patterns in plants and animals","volume":"11","author":"Law","year":"2010","journal-title":"Nature Reviews. Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0685","doi-asserted-by":"crossref","first-page":"422","DOI":"10.1016\/j.molcel.2018.03.020","article-title":"Allosteric activation dictates PRC2 activity independent of its recruitment to chromatin","volume":"70","author":"Lee","year":"2018","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0690","doi-asserted-by":"crossref","first-page":"447","DOI":"10.1126\/science.1149042","article-title":"Demethylation of H3K27 regulates polycomb recruitment and H2A ubiquitination","volume":"318","author":"Lee","year":"2007","journal-title":"Science (New York, N.Y.)"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0695","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1080\/10409238.2017.1380596","article-title":"Finding the needle in the haystack: towards solving the protein-folding problem computationally","volume":"53","author":"Li","year":"2018","journal-title":"Critical Reviews in Biochemistry and Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0700","doi-asserted-by":"crossref","first-page":"480","DOI":"10.1016\/j.ejmech.2016.08.036","article-title":"High-affinity small molecular blockers of mixed lineage leukemia 1 (MLL1)-WDR5 interaction inhibit MLL1 complex H3K4 methyltransferase activity","volume":"124","author":"Li","year":"2016","journal-title":"European Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0705","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/j.ejmech.2016.04.032","article-title":"Structure-based design and synthesis of small molecular inhibitors disturbing the interaction of MLL1-WDR5","volume":"118","author":"Li","year":"2016","journal-title":"European Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0710","doi-asserted-by":"crossref","first-page":"6109","DOI":"10.1016\/j.bmc.2016.09.073","article-title":"Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction","volume":"24","author":"Li","year":"2016","journal-title":"Bioorganic & Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0715","doi-asserted-by":"crossref","first-page":"662","DOI":"10.1038\/nrg887","article-title":"Chromatin modification and epigenetic reprogramming in mammalian development","volume":"3","author":"Li","year":"2002","journal-title":"Nature Reviews. Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0720","doi-asserted-by":"crossref","first-page":"915","DOI":"10.1016\/0092-8674(92)90611-F","article-title":"Targeted mutation of the DNA methyltransferase gene results in embryonic lethality","volume":"69","author":"Li","year":"1992","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0725","doi-asserted-by":"crossref","first-page":"287","DOI":"10.1038\/nature23881","article-title":"Polycomb-like proteins link the PRC2 complex to CpG islands","volume":"549","author":"Li","year":"2017","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0730","doi-asserted-by":"crossref","first-page":"2090","DOI":"10.1016\/j.bmcl.2014.03.055","article-title":"Discovery of two aminoglycoside antibiotics as inhibitors targeting the menin-mixed lineage leukaemia interface","volume":"24","author":"Li","year":"2014","journal-title":"Bioorganic & Medicinal Chemistry Letters"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0735","doi-asserted-by":"crossref","first-page":"409","DOI":"10.1038\/s41586-019-1029-2","article-title":"Mechanism of DNA translocation underlying chromatin remodelling by Snf2","volume":"567","author":"Li","year":"2019","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0740","doi-asserted-by":"crossref","first-page":"3218","DOI":"10.1093\/nar\/gky104","article-title":"Structural and mechanistic insights into UHRF1-mediated DNMT1 activation in the maintenance DNA methylation","volume":"46","author":"Li","year":"2018","journal-title":"Nucleic Acids Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0745","doi-asserted-by":"crossref","first-page":"642","DOI":"10.1158\/1535-7163.MCT-14-0650","article-title":"Validation of the Hsp70-Bag3 protein-protein interaction as a potential therapeutic target in cancer","volume":"14","author":"Li","year":"2015","journal-title":"Molecular Cancer Therapeutics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0750","doi-asserted-by":"crossref","first-page":"447","DOI":"10.1038\/nature16952","article-title":"Structural basis for activity regulation of MLL family methyltransferases","volume":"530","author":"Li","year":"2016","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0755","doi-asserted-by":"crossref","first-page":"136","DOI":"10.1038\/s41586-018-0751-5","article-title":"Stella safeguards the oocyte methylome by preventing de novo methylation mediated by DNMT1","volume":"564","author":"Li","year":"2018","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0760","doi-asserted-by":"crossref","first-page":"529","DOI":"10.1038\/nature07726","article-title":"Chromatin remodelling factor Mll1 is essential for neurogenesis from postnatal neural stem cells","volume":"458","author":"Lim","year":"2009","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0765","doi-asserted-by":"crossref","first-page":"440","DOI":"10.1038\/nature22036","article-title":"Mechanism of chromatin remodelling revealed by the Snf2-nucleosome structure","volume":"544","author":"Liu","year":"2017","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0770","doi-asserted-by":"crossref","first-page":"2251","DOI":"10.1016\/j.ejca.2014.05.017","article-title":"BRG1 promotes chemoresistance of pancreatic cancer cells through crosstalking with Akt signalling","volume":"50","author":"Liu","year":"2014","journal-title":"European Journal of Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0775","doi-asserted-by":"crossref","first-page":"431","DOI":"10.1007\/978-3-319-43624-1_16","article-title":"DNA Methyltransferase Inhibitors: Development and Applications","volume":"945","author":"Lopez","year":"2016","journal-title":"Advances in Experimental Medicine and Biology"},{"issue":"9","key":"10.1016\/j.pharmthera.2019.107406_bib0780","doi-asserted-by":"crossref","first-page":"1544","DOI":"10.1038\/aps.2017.188","article-title":"Identification of small molecule inhibitors targeting the SMARCA2 bromodomain from a high-throughput screening assay","volume":"39","author":"Lu","year":"2018","journal-title":"Acta Pharmacologica Sinica"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0785","doi-asserted-by":"crossref","first-page":"251","DOI":"10.1038\/38444","article-title":"Crystal structure of the nucleosome core particle at 2.8 A resolution","volume":"389","author":"Luger","year":"1997","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0790","doi-asserted-by":"crossref","first-page":"682","DOI":"10.1016\/j.stem.2010.11.013","article-title":"Bmi-1 is a crucial regulator of prostate stem cell self-renewal and malignant transformation","volume":"7","author":"Lukacs","year":"2010","journal-title":"Cell Stem Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0795","doi-asserted-by":"crossref","first-page":"344","DOI":"10.1038\/nm.3830","article-title":"Targeting the MLL complex in castration-resistant prostate cancer","volume":"21","author":"Malik","year":"2015","journal-title":"Nature Medicine"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0800","doi-asserted-by":"crossref","first-page":"90","DOI":"10.3389\/fgene.2015.00090","article-title":"DNA methyltransferase 1 mutations and mitochondrial pathology: is mtDNA methylated?","volume":"6","author":"Maresca","year":"2015","journal-title":"Frontiers in Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0805","doi-asserted-by":"crossref","first-page":"762","DOI":"10.1038\/nature08398","article-title":"Role of the polycomb protein EED in the propagation of repressive histone marks","volume":"461","author":"Margueron","year":"2009","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0810","doi-asserted-by":"crossref","first-page":"503","DOI":"10.1016\/j.molcel.2008.11.004","article-title":"Ezh1 and Ezh2 maintain repressive chromatin through different mechanisms","volume":"32","author":"Margueron","year":"2008","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0815","doi-asserted-by":"crossref","first-page":"267","DOI":"10.1111\/j.1365-2559.2008.03109.x","article-title":"Prognostic significance of the therapeutic targets histone deacetylase 1, 2, 6 and acetylated histone H4 in cutaneous T-cell lymphoma","volume":"53","author":"Marquard","year":"2008","journal-title":"Histopathology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0820","doi-asserted-by":"crossref","first-page":"688","DOI":"10.1111\/j.1365-2559.2009.03290.x","article-title":"Histone deacetylase 1, 2, 6 and acetylated histone H4 in B- and T-cell lymphomas","volume":"54","author":"Marquard","year":"2009","journal-title":"Histopathology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0825","doi-asserted-by":"crossref","first-page":"2989","DOI":"10.1073\/pnas.1116418109","article-title":"Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)","volume":"109","author":"McCabe","year":"2012","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0830","doi-asserted-by":"crossref","first-page":"108","DOI":"10.1038\/nature11606","article-title":"EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations","volume":"492","author":"McCabe","year":"2012","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0835","doi-asserted-by":"crossref","first-page":"591","DOI":"10.1038\/nature13890","article-title":"Crystal structure of the PRC1 ubiquitylation module bound to the nucleosome","volume":"514","author":"McGinty","year":"2014","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0840","doi-asserted-by":"crossref","first-page":"868","DOI":"10.1016\/j.jaci.2015.07.048","article-title":"Risk of anaphylaxis after vaccination in children and adults","volume":"137","author":"McNeil","year":"2016","journal-title":"The Journal of Allergy and Clinical Immunology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0845","doi-asserted-by":"crossref","first-page":"1490","DOI":"10.1038\/leu.2009.33","article-title":"New insights to the MLL recombinome of acute leukemias","volume":"23","author":"Meyer","year":"2009","journal-title":"Leukemia"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0850","doi-asserted-by":"crossref","first-page":"11367","DOI":"10.1158\/0008-5472.CAN-05-1041","article-title":"Leukemogenic MLL fusion proteins bind across a broad region of the Hox a9 locus, promoting transcription and multiple histone modifications","volume":"65","author":"Milne","year":"2005","journal-title":"Cancer Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0855","doi-asserted-by":"crossref","first-page":"286","DOI":"10.1038\/nm.2100","article-title":"An oncogene-tumor suppressor cascade drives metastatic prostate cancer by coordinately activating Ras and nuclear factor-kappaB","volume":"16","author":"Min","year":"2010","journal-title":"Nature Medicine"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0860","doi-asserted-by":"crossref","first-page":"300","DOI":"10.1016\/j.lungcan.2011.02.019","article-title":"Expression of histone deacetylase 1 correlates with a poor prognosis in patients with adenocarcinoma of the lung","volume":"74","author":"Minamiya","year":"2011","journal-title":"Lung Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0865","doi-asserted-by":"crossref","first-page":"665","DOI":"10.1111\/j.1365-2141.2010.08301.x","article-title":"Differential expression of HDAC3, HDAC7 and HDAC9 is associated with prognosis and survival in childhood acute lymphoblastic leukaemia","volume":"150","author":"Moreno","year":"2010","journal-title":"British Journal of Haematology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0870","doi-asserted-by":"crossref","first-page":"16937","DOI":"10.1073\/pnas.1417365111","article-title":"Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief","volume":"111","author":"Moriconi","year":"2014","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0875","doi-asserted-by":"crossref","first-page":"66","DOI":"10.1186\/s13041-015-0158-2","article-title":"Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage","volume":"8","author":"Motolese","year":"2015","journal-title":"Molecular Brain"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0880","doi-asserted-by":"crossref","first-page":"847","DOI":"10.1038\/nrd.2018.201","article-title":"Phosphatases start shedding their stigma of undruggability","volume":"17","author":"Mullard","year":"2018","journal-title":"Nature Reviews. Drug Discovery"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0885","doi-asserted-by":"crossref","first-page":"5028","DOI":"10.1073\/pnas.1202258109","article-title":"Polycomb repressive complex 2 is required for MLL-AF9 leukemia","volume":"109","author":"Neff","year":"2012","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0890","doi-asserted-by":"crossref","first-page":"17","DOI":"10.1186\/s13045-018-0562-z","article-title":"CBX7 regulates stem cell-like properties of gastric cancer cells via p16 and AKT-NF-kappaB-miR-21 pathways","volume":"11","author":"Ni","year":"2018","journal-title":"Journal of Hematology & Oncology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0895","doi-asserted-by":"crossref","first-page":"1064","DOI":"10.1038\/s41556-018-0169-1","article-title":"RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers","volume":"20","author":"Nichols","year":"2018","journal-title":"Nature Cell Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0900","doi-asserted-by":"crossref","first-page":"61","DOI":"10.1007\/s12013-011-9185-5","article-title":"The multifaceted roles of USP7: new therapeutic opportunities","volume":"60","author":"Nicholson","year":"2011","journal-title":"Cell Biochemistry and Biophysics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0905","doi-asserted-by":"crossref","first-page":"665","DOI":"10.1038\/ng.620","article-title":"Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes","volume":"42","author":"Nikoloski","year":"2010","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0910","doi-asserted-by":"crossref","first-page":"249","DOI":"10.1038\/nature12488","article-title":"Uhrf1-dependent H3K23 ubiquitylation couples maintenance DNA methylation and replication","volume":"502","author":"Nishiyama","year":"2013","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0915","doi-asserted-by":"crossref","first-page":"298","DOI":"10.1038\/nm.2651","article-title":"Genetic inactivation of the polycomb repressive complex 2 in T cell acute lymphoblastic leukemia","volume":"18","author":"Ntziachristos","year":"2012","journal-title":"Nature Medicine"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0920","doi-asserted-by":"crossref","first-page":"219","DOI":"10.1038\/890","article-title":"Cloning and characterization of a family of novel mammalian DNA (cytosine-5) methyltransferases","volume":"19","author":"Okano","year":"1998","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0925","doi-asserted-by":"crossref","first-page":"900","DOI":"10.1111\/bcp.13870","article-title":"Effects of the nitric oxide synthase inhibitor ronopterin (VAS203) on renal function in healthy volunteers","volume":"85","author":"Ott","year":"2019","journal-title":"British Journal of Clinical Pharmacology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0930","doi-asserted-by":"crossref","first-page":"10155","DOI":"10.1021\/acs.jmedchem.8b01318","article-title":"Discovery of orally active inhibitors of Brahma homolog (BRM)\/SMARCA2 ATPase activity for the treatment of brahma related gene 1 (BRG1)\/SMARCA4-mutant cancers","volume":"61","author":"Papillon","year":"2018","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0935","doi-asserted-by":"crossref","first-page":"306","DOI":"10.1038\/nature08788","article-title":"JARID2 regulates binding of the Polycomb repressive complex 2 to target genes in ES cells","volume":"464","author":"Pasini","year":"2010","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0940","doi-asserted-by":"crossref","first-page":"32158","DOI":"10.1074\/jbc.C800164200","article-title":"Structure of WDR5 bound to mixed lineage leukemia protein-1 peptide","volume":"283","author":"Patel","year":"2008","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0945","doi-asserted-by":"crossref","first-page":"24242","DOI":"10.1074\/jbc.M109.014498","article-title":"On the mechanism of multiple lysine methylation by the human mixed lineage leukemia protein-1 (MLL1) core complex","volume":"284","author":"Patel","year":"2009","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0950","doi-asserted-by":"crossref","first-page":"32162","DOI":"10.1074\/jbc.M806317200","article-title":"A conserved arginine-containing motif crucial for the assembly and enzymatic activity of the mixed lineage leukemia protein-1 core complex","volume":"283","author":"Patel","year":"2008","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0955","doi-asserted-by":"crossref","first-page":"6910","DOI":"10.1038\/ncomms7910","article-title":"DNMT1 is essential for mammary and cancer stem cell maintenance and tumorigenesis","volume":"6","author":"Pathania","year":"2015","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0960","doi-asserted-by":"crossref","first-page":"350","DOI":"10.1016\/j.ygeno.2008.12.004","article-title":"Phylogenetic analysis of the eukaryotic RNA (cytosine-5)-methyltransferases","volume":"93","author":"Pavlopoulou","year":"2009","journal-title":"Genomics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0965","doi-asserted-by":"crossref","first-page":"1160","DOI":"10.1093\/carcin\/bgi361","article-title":"DNA methylation of multiple tumor-related genes in association with overexpression of DNA methyltransferase 1 (DNMT1) during multistage carcinogenesis of the pancreas","volume":"27","author":"Peng","year":"2006","journal-title":"Carcinogenesis"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0970","doi-asserted-by":"crossref","first-page":"403","DOI":"10.1111\/j.1349-7006.2005.00071.x","article-title":"Increased DNA methyltransferase 1 (DNMT1) protein expression in precancerous conditions and ductal carcinomas of the pancreas","volume":"96","author":"Peng","year":"2005","journal-title":"Cancer Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0975","doi-asserted-by":"crossref","first-page":"1002","DOI":"10.1038\/s41588-018-0134-8","article-title":"MTF2 recruits Polycomb Repressive Complex 2 by helical-shape-selective DNA binding","volume":"50","author":"Perino","year":"2018","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0980","doi-asserted-by":"crossref","first-page":"1808","DOI":"10.1002\/tcr.201800074","article-title":"Bromodomain drug discovery - the past, the present, and the future","volume":"18","author":"Pervaiz","year":"2018","journal-title":"Chemical Record"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0985","doi-asserted-by":"crossref","first-page":"247","DOI":"10.1016\/S1097-2765(00)80315-9","article-title":"Reconstitution of a core chromatin remodeling complex from SWI\/SNF subunits","volume":"3","author":"Phelan","year":"1999","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0990","doi-asserted-by":"crossref","first-page":"154","DOI":"10.1038\/s41594-018-0023-y","article-title":"Cryo-EM structures of PRC2 simultaneously engaged with two functionally distinct nucleosomes","volume":"25","author":"Poepsel","year":"2018","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib0995","article-title":"MYC-driven epigenetic reprogramming favors the onset of tumorigenesis by inducing a stem cell-like state","volume":"9","author":"Poli","year":"2018","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1000","doi-asserted-by":"crossref","first-page":"7465","DOI":"10.1021\/acs.jmedchem.5b00975","article-title":"Rational design of orthogonal multipolar interactions with fluorine in protein-ligand complexes","volume":"58","author":"Pollock","year":"2015","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1005","doi-asserted-by":"crossref","first-page":"245","DOI":"10.1002\/ajh.22257","article-title":"Frequent deletions of JARID2 in leukemic transformation of chronic myeloid malignancies","volume":"87","author":"Puda","year":"2012","journal-title":"American Journal of Hematology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1010","doi-asserted-by":"crossref","first-page":"381","DOI":"10.1038\/nchembio.2304","article-title":"An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED","volume":"13","author":"Qi","year":"2017","journal-title":"Nature Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1015","doi-asserted-by":"crossref","first-page":"34490","DOI":"10.1074\/jbc.C800169200","article-title":"Structure and hemimethylated CpG binding of the SRA domain from human UHRF1","volume":"283","author":"Qian","year":"2008","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1020","doi-asserted-by":"crossref","first-page":"319","DOI":"10.1016\/j.stem.2012.06.002","article-title":"The polycomb group protein L3mbtl2 assembles an atypical PRC1-family complex that is essential in pluripotent stem cells and early development","volume":"11","author":"Qin","year":"2012","journal-title":"Cell Stem Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1025","doi-asserted-by":"crossref","first-page":"439","DOI":"10.1002\/jcb.22998","article-title":"Usp7 and Uhrf1 control ubiquitination and stability of the maintenance DNA methyltransferase Dnmt1","volume":"112","author":"Qin","year":"2011","journal-title":"Journal of Cellular Biochemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1030","doi-asserted-by":"crossref","first-page":"911","DOI":"10.1038\/cr.2015.72","article-title":"DNA methylation requires a DNMT1 ubiquitin interacting motif (UIM) and histone ubiquitination","volume":"25","author":"Qin","year":"2015","journal-title":"Cell Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1035","doi-asserted-by":"crossref","first-page":"26","DOI":"10.1186\/s12935-018-0523-1","article-title":"MLL2\/KMT2D and MLL3\/KMT2C expression correlates with disease progression and response to imatinib mesylate in chronic myeloid leukemia","volume":"18","author":"Rabello","year":"2018","journal-title":"Cancer Cell International"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1040","doi-asserted-by":"crossref","first-page":"604","DOI":"10.1126\/science.6254144","article-title":"DNA methylation and gene function","volume":"210","author":"Razin","year":"1980","journal-title":"Science (New York, N.Y.)"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1045","doi-asserted-by":"crossref","first-page":"403","DOI":"10.1038\/nrg1602","article-title":"Co-evolution of X-chromosome inactivation and imprinting in mammals","volume":"6","author":"Reik","year":"2005","journal-title":"Nature Reviews. Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1050","doi-asserted-by":"crossref","first-page":"161","DOI":"10.1016\/j.chembiol.2014.11.021","article-title":"Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain","volume":"22","author":"Ren","year":"2015","journal-title":"Chemistry & Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1055","doi-asserted-by":"crossref","DOI":"10.1038\/ncomms11938","article-title":"Chromatin accessibility maps of chronic lymphocytic leukaemia identify subtype-specific epigenome signatures and transcription regulatory networks","volume":"7","author":"Rendeiro","year":"2016","journal-title":"Nature Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1060","doi-asserted-by":"crossref","first-page":"61","DOI":"10.1038\/ng1068","article-title":"DNMT1 is required to maintain CpG methylation and aberrant gene silencing in human cancer cells","volume":"33","author":"Robert","year":"2003","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1065","doi-asserted-by":"crossref","first-page":"461","DOI":"10.1093\/carcin\/21.3.461","article-title":"DNA methylation: past, present and future directions","volume":"21","author":"Robertson","year":"2000","journal-title":"Carcinogenesis"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1070","doi-asserted-by":"crossref","first-page":"658","DOI":"10.1101\/gad.256628.114","article-title":"Brg1 promotes both tumor-suppressive and oncogenic activities at distinct stages of pancreatic cancer formation","volume":"29","author":"Roy","year":"2015","journal-title":"Genes & Development"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1075","doi-asserted-by":"crossref","first-page":"15","DOI":"10.1016\/j.molcel.2006.12.014","article-title":"Methylation of lysine 4 on histone H3: intricacy of writing and reading a single epigenetic mark","volume":"25","author":"Ruthenburg","year":"2007","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1080","doi-asserted-by":"crossref","first-page":"704","DOI":"10.1038\/nsmb1119","article-title":"Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex","volume":"13","author":"Ruthenburg","year":"2006","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1085","doi-asserted-by":"crossref","first-page":"769","DOI":"10.1016\/j.molcel.2014.12.020","article-title":"Jarid2 methylation via the PRC2 complex regulates H3K27me3 deposition during cell differentiation","volume":"57","author":"Sanulli","year":"2015","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1090","doi-asserted-by":"crossref","first-page":"20883","DOI":"10.1073\/pnas.1214735109","article-title":"Interactions between the nucleosome histone core and Arp8 in the INO80 chromatin remodeling complex","volume":"109","author":"Saravanan","year":"2012","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1095","doi-asserted-by":"crossref","first-page":"2718","DOI":"10.1128\/MCB.02017-07","article-title":"Ezh2 requires PHF1 to efficiently catalyze H3 lysine 27 trimethylation in vivo","volume":"28","author":"Sarma","year":"2008","journal-title":"Molecular and Cellular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1100","doi-asserted-by":"crossref","first-page":"57","DOI":"10.1016\/B978-0-12-380866-0.60003-4","article-title":"Histone modifications and cancer","volume":"70","author":"Sawan","year":"2010","journal-title":"Advances in Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1105","doi-asserted-by":"crossref","first-page":"330","DOI":"10.1016\/j.molcel.2011.03.025","article-title":"Histone methylation by PRC2 is inhibited by active chromatin marks","volume":"42","author":"Schmitges","year":"2011","journal-title":"Molecular Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1110","doi-asserted-by":"crossref","first-page":"3110","DOI":"10.1038\/sj.emboj.7601187","article-title":"Recruitment of PRC1 function at the initiation of X inactivation independent of PRC2 and silencing","volume":"25","author":"Schoeftner","year":"2006","journal-title":"The EMBO Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1115","doi-asserted-by":"crossref","first-page":"8120","DOI":"10.1021\/acs.jmedchem.8b01040","article-title":"Discovery of asciminib (ABL001), an allosteric inhibitor of the tyrosine kinase activity of BCR-ABL1","volume":"61","author":"Schoepfer","year":"2018","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1120","doi-asserted-by":"crossref","first-page":"3345","DOI":"10.1073\/pnas.1215379110","article-title":"Structure of an actin-related subcomplex of the SWI\/SNF chromatin remodeler","volume":"110","author":"Schubert","year":"2013","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1125","doi-asserted-by":"crossref","first-page":"4245","DOI":"10.1038\/sj.emboj.7601316","article-title":"Structural basis for molecular recognition and presentation of histone H3 by WDR5","volume":"25","author":"Schuetz","year":"2006","journal-title":"The EMBO Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1130","doi-asserted-by":"crossref","first-page":"2135","DOI":"10.1016\/j.celrep.2017.02.017","article-title":"Loss of Snf5 induces formation of an aberrant SWI\/SNF complex","volume":"18","author":"Sen","year":"2017","journal-title":"Cell Reports"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1135","doi-asserted-by":"crossref","first-page":"151","DOI":"10.1042\/BJ20121280","article-title":"Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5","volume":"449","author":"Senisterra","year":"2013","journal-title":"The Biochemical Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1140","doi-asserted-by":"crossref","first-page":"2720","DOI":"10.1016\/j.bmcl.2015.04.026","article-title":"Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility","volume":"25","author":"Senter","year":"2015","journal-title":"Bioorganic & Medicinal Chemistry Letters"},{"issue":"8","key":"10.1016\/j.pharmthera.2019.107406_bib1145","doi-asserted-by":"crossref","first-page":"494","DOI":"10.1038\/s41571-019-0190-8","article-title":"Emerging epigenetic-modulating therapies in lymphoma","volume":"16","author":"Sermer","year":"2019","journal-title":"Nature Reviews. Clinical Oncology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1150","doi-asserted-by":"crossref","first-page":"908","DOI":"10.1038\/nature06397","article-title":"The SRA protein Np95 mediates epigenetic inheritance by recruiting Dnmt1 to methylated DNA","volume":"450","author":"Sharif","year":"2007","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1155","doi-asserted-by":"crossref","first-page":"1804","DOI":"10.2174\/1568026619666181120150938","article-title":"Intelligently applying artificial intelligence in chemoinformatics","volume":"18","author":"Sharma","year":"2018","journal-title":"Current Topics in Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1160","doi-asserted-by":"crossref","first-page":"705","DOI":"10.1126\/science.aau3775","article-title":"De novo design of self-assembling helical protein filaments","volume":"362","author":"Shen","year":"2018","journal-title":"Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1165","doi-asserted-by":"crossref","first-page":"4461","DOI":"10.1182\/blood-2012-05-429274","article-title":"Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia","volume":"120","author":"Shi","year":"2012","journal-title":"Blood"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1170","doi-asserted-by":"crossref","first-page":"2648","DOI":"10.1101\/gad.232710.113","article-title":"Role of SWI\/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation","volume":"27","author":"Shi","year":"2013","journal-title":"Genes & Development"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1175","doi-asserted-by":"crossref","first-page":"341","DOI":"10.1016\/j.ceb.2008.03.019","article-title":"Molecular implementation and physiological roles for histone H3 lysine 4 (H3K4) methylation","volume":"20","author":"Shilatifard","year":"2008","journal-title":"Current Opinion in Cell Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1180","doi-asserted-by":"crossref","first-page":"1201","DOI":"10.1038\/cr.2010.128","article-title":"BRCA1 affects global DNA methylation through regulation of DNMT1","volume":"20","author":"Shukla","year":"2010","journal-title":"Cell Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1185","doi-asserted-by":"crossref","first-page":"1087","DOI":"10.1002\/jcb.20005","article-title":"ATP-dependent nucleosome remodeling complexes: enzymes tailored to deal with chromatin","volume":"91","author":"Sif","year":"2004","journal-title":"Journal of Cellular Biochemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1190","doi-asserted-by":"crossref","first-page":"186","DOI":"10.1038\/s41586-018-0830-7","article-title":"De novo design of potent and selective mimics of IL-2 and IL-15","volume":"565","author":"Silva","year":"2019","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1195","doi-asserted-by":"crossref","first-page":"2874","DOI":"10.1021\/jm401487x","article-title":"Chromodomain antagonists that target the polycomb-group methyllysine reader protein chromobox homolog 7 (CBX7)","volume":"57","author":"Simhadri","year":"2014","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1200","doi-asserted-by":"crossref","first-page":"697","DOI":"10.1038\/nrm2763","article-title":"Mechanisms of polycomb gene silencing: knowns and unknowns","volume":"10","author":"Simon","year":"2009","journal-title":"Nature Reviews. Molecular Cell Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1205","doi-asserted-by":"crossref","first-page":"1308","DOI":"10.1002\/cbic.200600562","article-title":"Structural ramification for acetyl-lysine recognition by the bromodomain of human BRG1 protein, a central ATPase of the SWI\/SNF remodeling complex","volume":"8","author":"Singh","year":"2007","journal-title":"Chembiochem"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1210","doi-asserted-by":"crossref","first-page":"20980","DOI":"10.1073\/pnas.1012525107","article-title":"Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas","volume":"107","author":"Sneeringer","year":"2010","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1215","doi-asserted-by":"crossref","first-page":"1036","DOI":"10.1126\/science.1195380","article-title":"Structure of DNMT1-DNA complex reveals a role for autoinhibition in maintenance DNA methylation","volume":"331","author":"Song","year":"2011","journal-title":"Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1220","doi-asserted-by":"crossref","first-page":"709","DOI":"10.1126\/science.1214453","article-title":"Structure-based mechanistic insights into DNMT1-mediated maintenance DNA methylation","volume":"335","author":"Song","year":"2012","journal-title":"Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1225","doi-asserted-by":"crossref","first-page":"35258","DOI":"10.1074\/jbc.M806900200","article-title":"WDR5 interacts with mixed lineage leukemia (MLL) protein via the histone H3-binding pocket","volume":"283","author":"Song","year":"2008","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1230","doi-asserted-by":"crossref","first-page":"565","DOI":"10.1083\/jcb.200610062","article-title":"DNMT1 but not its interaction with the replication machinery is required for maintenance of DNA methylation in human cells","volume":"176","author":"Spada","year":"2007","journal-title":"The Journal of Cell Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1235","first-page":"2229","article-title":"Extensive DNA methylation spanning the Rb promoter in retinoblastoma tumors","volume":"57","author":"Stirzaker","year":"1997","journal-title":"Cancer Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1240","doi-asserted-by":"crossref","first-page":"837","DOI":"10.1016\/j.ccell.2015.05.006","article-title":"Kinase and BET inhibitors together clamp inhibition of PI3K signaling and overcome resistance to therapy","volume":"27","author":"Stratikopoulos","year":"2015","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1245","doi-asserted-by":"crossref","first-page":"8","DOI":"10.1002\/ijc.23607","article-title":"Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine","volume":"123","author":"Stresemann","year":"2008","journal-title":"International Journal of Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1250","doi-asserted-by":"crossref","first-page":"180","DOI":"10.1038\/nchembio.2007","article-title":"A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1","volume":"12","author":"Stuckey","year":"2016","journal-title":"Nature Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1255","doi-asserted-by":"crossref","first-page":"5143","DOI":"10.1158\/0008-5472.CAN-15-0423","article-title":"WDR5 supports an N-Myc transcriptional complex that drives a protumorigenic gene expression signature in neuroblastoma","volume":"75","author":"Sun","year":"2015","journal-title":"Cancer Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1260","doi-asserted-by":"crossref","first-page":"469","DOI":"10.1038\/nsmb.1403","article-title":"The HSA domain binds nuclear actin-related proteins to regulate chromatin-remodeling ATPases","volume":"15","author":"Szerlong","year":"2008","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1265","doi-asserted-by":"crossref","first-page":"301","DOI":"10.1080\/13543784.2018.1442436","article-title":"Cenicriviroc for the treatment of non-alcoholic steatohepatitis and liver fibrosis","volume":"27","author":"Tacke","year":"2018","journal-title":"Expert Opinion on Investigational Drugs"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1270","doi-asserted-by":"crossref","first-page":"9055","DOI":"10.1073\/pnas.1019629108","article-title":"Structural insight into maintenance methylation by mouse DNA methyltransferase 1 (Dnmt1)","volume":"108","author":"Takeshita","year":"2011","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1275","doi-asserted-by":"crossref","first-page":"148","DOI":"10.1016\/j.ccr.2009.12.034","article-title":"MLL-AF9-induced leukemogenesis requires coexpression of the wild-type Mll allele","volume":"17","author":"Thiel","year":"2010","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1280","doi-asserted-by":"crossref","first-page":"1159","DOI":"10.1007\/s00262-006-0164-4","article-title":"Epigenetic regulation of immune escape genes in cancer","volume":"55","author":"Tomasi","year":"2006","journal-title":"Cancer Immunology, Immunotherapy"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1285","doi-asserted-by":"crossref","first-page":"1284","DOI":"10.1016\/j.cell.2017.10.022","article-title":"Epigenetic therapy ties MYC depletion to reversing immune evasion and treating lung cancer","volume":"171","author":"Topper","year":"2017","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1290","doi-asserted-by":"crossref","first-page":"835","DOI":"10.1038\/nrd.2016.185","article-title":"Epigenetic drug discovery: breaking through the immune barrier","volume":"15","author":"Tough","year":"2016","journal-title":"Nature Reviews. Drug Discovery"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1295","doi-asserted-by":"crossref","first-page":"24","DOI":"10.1111\/dom.12752","article-title":"Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus","volume":"19","author":"Vajda","year":"2017","journal-title":"Diabetes, Obesity & Metabolism"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1300","doi-asserted-by":"crossref","first-page":"662","DOI":"10.1002\/pro.3129","article-title":"Targeting human SET1\/MLL family of proteins","volume":"26","author":"Vedadi","year":"2017","journal-title":"Protein Science"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1305","doi-asserted-by":"crossref","first-page":"203","DOI":"10.1038\/28212","article-title":"Truncating mutations of hSNF5\/INI1 in aggressive paediatric cancer","volume":"394","author":"Versteege","year":"1998","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1310","doi-asserted-by":"crossref","first-page":"16572","DOI":"10.1073\/pnas.0805317105","article-title":"Different polycomb group CBX family proteins associate with distinct regions of chromatin using nonhomologous protein sequences","volume":"105","author":"Vincenz","year":"2008","journal-title":"Proceedings of the National Academy of Sciences of the United States of America"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1315","doi-asserted-by":"crossref","first-page":"2781","DOI":"10.1172\/JCI45349","article-title":"Constitutive IKK2 activation in intestinal epithelial cells induces intestinal tumors in mice","volume":"121","author":"Vlantis","year":"2011","journal-title":"The Journal of Clinical Investigation"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1320","doi-asserted-by":"crossref","first-page":"43","DOI":"10.5966\/sctm.2012-0036","article-title":"EZH2 is required for breast and pancreatic cancer stem cell maintenance and can be used as a functional cancer stem cell reporter","volume":"2","author":"van Vlerken","year":"2013","journal-title":"Stem Cells Translational Medicine"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1325","doi-asserted-by":"crossref","first-page":"153","DOI":"10.1016\/j.stem.2009.12.014","article-title":"Polycomb-like 2 associates with PRC2 and regulates transcriptional networks during mouse embryonic stem cell self-renewal and differentiation","volume":"6","author":"Walker","year":"2010","journal-title":"Cell Stem Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1330","doi-asserted-by":"crossref","first-page":"125","DOI":"10.1038\/ng.268","article-title":"The lysine demethylase LSD1 (KDM1) is required for maintenance of global DNA methylation","volume":"41","author":"Wang","year":"2009","journal-title":"Nature Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1335","doi-asserted-by":"crossref","first-page":"1012","DOI":"10.1093\/carcin\/bgt008","article-title":"Association of two BRM promoter polymorphisms with head and neck squamous cell carcinoma risk","volume":"34","author":"Wang","year":"2013","journal-title":"Carcinogenesis"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1340","doi-asserted-by":"crossref","first-page":"2153","DOI":"10.1038\/ajg.2009.300","article-title":"DNA promoter hypermethylation of p16 and APC predicts neoplastic progression in Barrett's esophagus","volume":"104","author":"Wang","year":"2009","journal-title":"The American Journal of Gastroenterology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1345","doi-asserted-by":"crossref","first-page":"5370","DOI":"10.1002\/j.1460-2075.1996.tb00921.x","article-title":"Purification and biochemical heterogeneity of the mammalian SWI-SNF complex","volume":"15","author":"Wang","year":"1996","journal-title":"The EMBO Journal"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1350","doi-asserted-by":"crossref","first-page":"1794","DOI":"10.1038\/sj.leu.2403917","article-title":"Direct evidence for cooperating genetic events in the leukemic transformation of normal human hematopoietic cells","volume":"19","author":"Warner","year":"2005","journal-title":"Leukemia"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1355","doi-asserted-by":"crossref","first-page":"1021","DOI":"10.1593\/neo.08474","article-title":"Expression of class I histone deacetylases indicates poor prognosis in endometrioid subtypes of ovarian and endometrial carcinomas","volume":"10","author":"Weichert","year":"2008","journal-title":"Neoplasia"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1360","doi-asserted-by":"crossref","first-page":"139","DOI":"10.1016\/S1470-2045(08)70004-4","article-title":"Association of patterns of class I histone deacetylase expression with patient prognosis in gastric cancer: a retrospective analysis","volume":"9","author":"Weichert","year":"2008","journal-title":"The Lancet Oncology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1365","doi-asserted-by":"crossref","first-page":"604","DOI":"10.1038\/sj.bjc.6604199","article-title":"Histone deacetylases 1, 2 and 3 are highly expressed in prostate cancer and HDAC2 expression is associated with shorter PSA relapse time after radical prostatectomy","volume":"98","author":"Weichert","year":"2008","journal-title":"British Journal of Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1370","doi-asserted-by":"crossref","first-page":"481","DOI":"10.1038\/nrc3068","article-title":"SWI\/SNF nucleosome remodellers and cancer","volume":"11","author":"Wilson","year":"2011","journal-title":"Nature Reviews. Cancer"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1375","doi-asserted-by":"crossref","first-page":"316","DOI":"10.1016\/j.ccr.2010.09.006","article-title":"Epigenetic antagonism between polycomb and SWI\/SNF complexes during oncogenic transformation","volume":"18","author":"Wilson","year":"2010","journal-title":"Cancer Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1380","doi-asserted-by":"crossref","first-page":"2205","DOI":"10.1093\/hmg\/dds035","article-title":"Mutations in DNMT1 cause autosomal dominant cerebellar ataxia, deafness and narcolepsy","volume":"21","author":"Winkelmann","year":"2012","journal-title":"Human Molecular Genetics"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1385","doi-asserted-by":"crossref","first-page":"733","DOI":"10.1038\/nature21702","article-title":"The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1","volume":"543","author":"Wylie","year":"2017","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1390","doi-asserted-by":"crossref","first-page":"859","DOI":"10.1016\/j.cell.2005.03.036","article-title":"WDR5 associates with histone H3 methylated at K4 and is essential for H3 K4 methylation and vertebrate development","volume":"121","author":"Wysocka","year":"2005","journal-title":"Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1395","doi-asserted-by":"crossref","first-page":"86","DOI":"10.1038\/nature04815","article-title":"A PHD finger of NURF couples histone H3 lysine 4 trimethylation with chromatin remodelling","volume":"442","author":"Wysocka","year":"2006","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1400","doi-asserted-by":"crossref","first-page":"847","DOI":"10.1111\/his.12334","article-title":"Loss of BRM expression is a frequently observed event in poorly differentiated clear cell renal cell carcinoma","volume":"64","author":"Xia","year":"2014","journal-title":"Histopathology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1405","doi-asserted-by":"crossref","first-page":"722","DOI":"10.1038\/nsmb.3259","article-title":"Structure of chromatin remodeler Swi2\/Snf2 in the resting state","volume":"23","author":"Xia","year":"2016","journal-title":"Nature Structural & Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1410","doi-asserted-by":"crossref","first-page":"1601","DOI":"10.1002\/anie.201711828","article-title":"Design of the first-in-class, highly potent irreversible inhibitor targeting the Menin-MLL protein-protein interaction","volume":"57","author":"Xu","year":"2018","journal-title":"Angewandte Chemie"},{"issue":"6","key":"10.1016\/j.pharmthera.2019.107406_bib1415","doi-asserted-by":"crossref","first-page":"567","DOI":"10.4155\/fmc-2018-0358","article-title":"Deep learning for molecular generation","volume":"11","author":"Xu","year":"2019","journal-title":"Future Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1420","doi-asserted-by":"crossref","first-page":"W374","DOI":"10.1093\/nar\/gky380","article-title":"CavityPlus: a web server for protein cavity detection with pharmacophore modelling, allosteric site identification and covalent ligand binding ability prediction","volume":"46","author":"Xu","year":"2018","journal-title":"Nucleic Acids Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1425","doi-asserted-by":"crossref","first-page":"1847","DOI":"10.1021\/acs.jcim.6b00185","article-title":"Discovery of novel inhibitors targeting the Menin-Mixed lineage leukemia interface using pharmacophore- and docking-based virtual screening","volume":"56","author":"Xu","year":"2016","journal-title":"Journal of Chemical Information and Modeling"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1430","doi-asserted-by":"crossref","first-page":"7","DOI":"10.1007\/s12185-016-2118-8","article-title":"SET\/MLL family proteins in hematopoiesis and leukemia","volume":"105","author":"Yang","year":"2017","journal-title":"International Journal of Hematology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1435","doi-asserted-by":"crossref","first-page":"2451","DOI":"10.1182\/blood-2010-11-321208","article-title":"Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation","volume":"117","author":"Yap","year":"2011","journal-title":"Blood"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1440","doi-asserted-by":"crossref","first-page":"772","DOI":"10.1021\/acschembio.7b00890","article-title":"Biochemical studies and molecular dynamic simulations reveal the molecular basis of conformational changes in DNA methyltransferase-1","volume":"13","author":"Ye","year":"2018","journal-title":"ACS Chemical Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1445","doi-asserted-by":"crossref","first-page":"903","DOI":"10.1101\/gad.325050.119","article-title":"PRC2 is high maintenance","volume":"33","author":"Yu","year":"2019","journal-title":"Genes & Development"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1450","doi-asserted-by":"crossref","first-page":"776","DOI":"10.2174\/1568026615666150302110135","article-title":"Small-molecule BET inhibitors in clinical and preclinical development and their therapeutic potential","volume":"15","author":"Yu","year":"2015","journal-title":"Current Topics in Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1455","doi-asserted-by":"crossref","first-page":"8503","DOI":"10.1039\/C6OB01248E","article-title":"Identification of novel small-molecule inhibitors targeting menin-MLL interaction, repurposing the antidiarrheal loperamide","volume":"14","author":"Yue","year":"2016","journal-title":"Organic & Biomolecular Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1460","doi-asserted-by":"crossref","first-page":"617","DOI":"10.1128\/MCB.24.2.617-628.2004","article-title":"Hoxa9 and Meis1 are key targets for MLL-ENL-mediated cellular immortalization","volume":"24","author":"Zeisig","year":"2004","journal-title":"Molecular and Cellular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1465","doi-asserted-by":"crossref","first-page":"2299","DOI":"10.1038\/s41386-018-0178-6","article-title":"Memory enhancing effects of BPN14770, an allosteric inhibitor of phosphodiesterase-4D, in wild-type and humanized mice","volume":"43","author":"Zhang","year":"2018","journal-title":"Neuropsychopharmacology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1470","doi-asserted-by":"crossref","first-page":"501","DOI":"10.1038\/nature08675","article-title":"Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors","volume":"463","author":"Zhang","year":"2010","journal-title":"Nature"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1475","doi-asserted-by":"crossref","first-page":"4237","DOI":"10.1093\/nar\/gkr1235","article-title":"The plasticity of WDR5 peptide-binding cleft enables the binding of the SET1 family of histone methyltransferases","volume":"40","author":"Zhang","year":"2012","journal-title":"Nucleic Acids Research"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1480","doi-asserted-by":"crossref","first-page":"1045","DOI":"10.1007\/s13238-018-0524-9","article-title":"Architecture of SWI\/SNF chromatin remodeling complex","volume":"9","author":"Zhang","year":"2018","journal-title":"Protein & Cell"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1485","doi-asserted-by":"crossref","first-page":"2520","DOI":"10.1016\/j.jmb.2015.06.001","article-title":"Crystal Structure of Human DNA Methyltransferase 1","volume":"427","author":"Zhang","year":"2015","journal-title":"Journal of Molecular Biology"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1490","doi-asserted-by":"crossref","first-page":"5788","DOI":"10.1039\/C6CC01079B","article-title":"Structure-based screening and optimization of cytisine derivatives as inhibitors of the menin-MLL interaction","volume":"52","author":"Zhong","year":"2016","journal-title":"Chemical Communications"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1495","doi-asserted-by":"crossref","first-page":"1113","DOI":"10.1021\/jm3015298","article-title":"Structure-based design of high-affinity macrocyclic peptidomimetics to block the menin-mixed lineage leukemia 1 (MLL1) protein\u2013protein interaction","volume":"56","author":"Zhou","year":"2013","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1500","doi-asserted-by":"crossref","first-page":"3","DOI":"10.2174\/1573406413666171020115539","article-title":"USP7: Target validation and drug discovery for cancer therapy","volume":"14","author":"Zhou","year":"2018","journal-title":"Medicinal Chemistry"},{"key":"10.1016\/j.pharmthera.2019.107406_bib1505","doi-asserted-by":"crossref","first-page":"206","DOI":"10.1038\/nature15251","article-title":"Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth","volume":"525","author":"Zhu","year":"2015","journal-title":"Nature"}],"container-title":["Pharmacology & Therapeutics"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0163725819301585?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0163725819301585?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,9,27]],"date-time":"2025-09-27T22:02:41Z","timestamp":1759010561000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0163725819301585"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2019,12]]},"references-count":301,"alternative-id":["S0163725819301585"],"URL":"https:\/\/doi.org\/10.1016\/j.pharmthera.2019.107406","relation":{},"ISSN":["0163-7258"],"issn-type":[{"value":"0163-7258","type":"print"}],"subject":[],"published":{"date-parts":[[2019,12]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Targeting epigenetic machinery: Emerging novel allosteric inhibitors","name":"articletitle","label":"Article Title"},{"value":"Pharmacology & Therapeutics","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.pharmthera.2019.107406","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2019 The Author(s). Published by Elsevier Inc.","name":"copyright","label":"Copyright"}],"article-number":"107406"}}