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Chem."},{"key":"10.1016\/j.bbcan.2026.189675_bb0520","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2026.118646","article-title":"Discovery of p300 histone acetyltransferase inhibitors bearing an imidazo[4,5-b]pyridine-2-one scaffold for the treatment of multiple myeloma","volume":"307","author":"Xiong","year":"2026","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bbcan.2026.189675_bb0525","doi-asserted-by":"crossref","first-page":"2242","DOI":"10.1038\/s41591-024-03060-0","article-title":"Inhibition of lysine acetyltransferase KAT6 in ER+HER2\u2212 metastatic breast cancer: a phase 1 trial","author":"Mukohara","year":"2024","journal-title":"Nat. Med."},{"key":"10.1016\/j.bbcan.2026.189675_bb0535","first-page":"1191","article-title":"Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A\/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer, cell","volume":"30","author":"Sharma","year":"2023","journal-title":"Chem. Biol."},{"key":"10.1016\/j.bbcan.2026.189675_bb1115","doi-asserted-by":"crossref","first-page":"2400","DOI":"10.1111\/cas.15785","article-title":"TIP60 is required for tumorigenesis in non-small cell lung cancer","volume":"114","author":"Shibahara","year":"2023","journal-title":"Cancer Sci."},{"key":"10.1016\/j.bbcan.2026.189675_bb1120","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0045539","article-title":"Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer","volume":"7","author":"Coffey","year":"2012","journal-title":"PLoS ONE"},{"key":"10.1016\/j.bbcan.2026.189675_bb0265","doi-asserted-by":"crossref","DOI":"10.1101\/cshperspect.a026831","article-title":"HDACs and HDAC inhibitors in cancer development and therapy","volume":"6","author":"Li","year":"2016","journal-title":"Cold Spring Harb. Perspect. Med."},{"key":"10.1016\/j.bbcan.2026.189675_bb0270","doi-asserted-by":"crossref","DOI":"10.1101\/cshperspect.a019521","article-title":"Histone modifications and cancer","volume":"8","author":"Audia","year":"2016","journal-title":"Cold Spring Harb. Perspect. Biol."},{"key":"10.1016\/j.bbcan.2026.189675_bb0275","doi-asserted-by":"crossref","first-page":"849","DOI":"10.1007\/s40265-024-02052-1","article-title":"Givinostat: first approval","author":"Lamb","year":"2024","journal-title":"Drugs"},{"key":"10.1016\/j.bbcan.2026.189675_bb0280","doi-asserted-by":"crossref","first-page":"1","DOI":"10.2119\/2006-00005.Dinarello","article-title":"The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo","volume":"11","author":"Leoni","year":"2005","journal-title":"Mol. Med."},{"key":"10.1016\/j.bbcan.2026.189675_bb0285","doi-asserted-by":"crossref","DOI":"10.3389\/fphar.2022.932914","article-title":"Therapeutic potential of tucidinostat, a subtype-selective HDAC inhibitor, in cancer treatment","volume":"13","author":"Sun","year":"2022","journal-title":"Front. Pharmacol."},{"key":"10.1016\/j.bbcan.2026.189675_bb0380","doi-asserted-by":"crossref","first-page":"1067","DOI":"10.1038\/nature09504","article-title":"Selective inhibition of BET bromodomains","volume":"468","author":"Filippakopoulos","year":"2010","journal-title":"Nature"},{"key":"10.1016\/j.bbcan.2026.189675_bb0385","doi-asserted-by":"crossref","DOI":"10.1016\/j.pharmthera.2023.108354","article-title":"BET proteins: biological functions and therapeutic interventions","volume":"243","author":"Guo","year":"2023","journal-title":"Pharmacol. Ther."},{"key":"10.1016\/j.bbcan.2026.189675_bb0390","doi-asserted-by":"crossref","first-page":"166","DOI":"10.1186\/s13148-020-00943-0","article-title":"BET protein inhibitor apabetalone (RVX-208) suppresses spro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes","volume":"12","author":"Wasiak","year":"2020","journal-title":"Clin. Epigenetics"},{"key":"10.1016\/j.bbcan.2026.189675_bb0395","doi-asserted-by":"crossref","first-page":"5585","DOI":"10.1021\/acs.jmedchem.0c00628","article-title":"Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H-pyrrolo[2,3- c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain inhibitor with selectivity for the second Bromodomain","volume":"63","author":"Sheppard","year":"2020","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bbcan.2026.189675_bb0400","doi-asserted-by":"crossref","first-page":"306","DOI":"10.1038\/s41586-020-1930-8","article-title":"Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer","volume":"578","author":"Faivre","year":"2020","journal-title":"Nature"},{"key":"10.1016\/j.bbcan.2026.189675_bb0405","doi-asserted-by":"crossref","unstructured":"O. Gilan, I. Rioja, K. Knezevic, M.J. Bell, M.M. Yeung, N.R. Harker, E.Y.N. Lam, C.-w. Chung, P. Bamborough, M. Petretich, M. Urh, S.J. Atkinson, A.K. Bassil, E.J. Roberts, D. Vassiliadis, M.L. Burr, A.G.S. Preston, C. Wellaway, T. Werner, J.R. Gray, A.-M. Michon, T. Gobbetti, V. Kumar, P.E. Soden, A. Haynes, J. Vappiani, D.F. Tough, S. Taylor, S.-J. Dawson, M. Bantscheff, M. Lindon, G. Drewes, E.H. Demont, D.L. Daniels, P. Grandi, R.K. Prinjha, M.A. Dawson, Selective targeting of BD1 and BD2 of the BET proteins in cancer and Immunoinflammation, Science 368 (2020) 387\u2013394.","DOI":"10.1126\/science.aaz8455"},{"key":"10.1016\/j.bbcan.2026.189675_bb0410","doi-asserted-by":"crossref","first-page":"27","DOI":"10.1038\/s41389-021-00316-z","article-title":"Resistance to BET inhibitors in lung adenocarcinoma is mediated by casein kinase phosphorylation of BRD4","volume":"10","author":"Calder","year":"2021","journal-title":"Oncogenesis"},{"key":"10.1016\/j.bbcan.2026.189675_bb0415","doi-asserted-by":"crossref","first-page":"1154","DOI":"10.1158\/1535-7163.MCT-23-0065","article-title":"First-in-human study of AZD5153, A small-molecule inhibitor of bromodomain protein 4, in patients with relapsed\/refractory malignant solid tumors and lymphoma","volume":"22","author":"Hamilton","year":"2023","journal-title":"Mol. Cancer Ther."},{"key":"10.1016\/j.bbcan.2026.189675_bb0435","doi-asserted-by":"crossref","first-page":"755","DOI":"10.1016\/j.chembiol.2015.05.009","article-title":"Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4","volume":"22","author":"Lu","year":"2015","journal-title":"Chem. Biol."},{"key":"10.1016\/j.bbcan.2026.189675_bb0440","doi-asserted-by":"crossref","first-page":"1376","DOI":"10.1126\/science.aab1433","article-title":"Phthalimide conjugation as a strategy for in vivo target protein degradation","volume":"348","author":"Winter","year":"2015","journal-title":"Science"},{"key":"10.1016\/j.bbcan.2026.189675_bb0445","doi-asserted-by":"crossref","first-page":"514","DOI":"10.1038\/nchembio.2329","article-title":"Structural basis of PROTAC cooperative recognition for selective protein degradation","volume":"13","author":"Gadd","year":"2017","journal-title":"Nat. Chem. 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Commun."},{"key":"10.1016\/j.bbcan.2026.189675_bb0480","series-title":"Handbook of Cancer and Immunology","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1007\/978-3-032-00771-1_259","article-title":"Acylases","author":"Brown","year":"2025"},{"key":"10.1016\/j.bbcan.2026.189675_bb0485","doi-asserted-by":"crossref","first-page":"5310","DOI":"10.1038\/sj.onc.1210599","article-title":"HATs and HDACs: from structure, function and regulation to novel strategies for therapy and prevention","volume":"26","author":"Yang","year":"2007","journal-title":"Oncogene"},{"key":"10.1016\/j.bbcan.2026.189675_bb0490","doi-asserted-by":"crossref","DOI":"10.1097\/HS9.0000000000000610","article-title":"The novel Oral BET-CBP\/p300 dual inhibitor NEO2734 is highly effective in eradicating acute myeloid leukemia blasts and stem\/progenitor cells","volume":"5","author":"van Gils","year":"2021","journal-title":"HemaSphere"},{"key":"10.1016\/j.bbcan.2026.189675_bb0530","doi-asserted-by":"crossref","first-page":"253","DOI":"10.1038\/s41586-018-0387-5","article-title":"Inhibitors of histone acetyltransferases KAT6A\/B induce senescence and arrest tumour growth","volume":"560","author":"Baell","year":"2018","journal-title":"Nature"},{"key":"10.1016\/j.bbcan.2026.189675_bb0540","doi-asserted-by":"crossref","first-page":"3854","DOI":"10.1007\/s12035-015-9314-z","article-title":"Epigenetic regulation of cytosolic phospholipase A2 in SH-SY5Y human neuroblastoma cells","volume":"53","author":"Tan","year":"2016","journal-title":"Mol. 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Chem."},{"key":"10.1016\/j.bbcan.2026.189675_bb0555","doi-asserted-by":"crossref","first-page":"1527","DOI":"10.1038\/s41467-017-01657-3","article-title":"Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors","volume":"8","author":"Dahlin","year":"2017","journal-title":"Nat. Commun."},{"key":"10.1016\/j.bbcan.2026.189675_bb0560","doi-asserted-by":"crossref","DOI":"10.1038\/emm.2017.11","article-title":"Writing, erasing and reading histone lysine methylations","volume":"49","author":"Hyun","year":"2017","journal-title":"Exp. Mol. Med."},{"key":"10.1016\/j.bbcan.2026.189675_bb0565","doi-asserted-by":"crossref","first-page":"689","DOI":"10.1016\/j.molcel.2010.11.031","article-title":"The chromatin signaling pathway: diverse mechanisms of recruitment of histone-modifying enzymes and varied biological outcomes","volume":"40","author":"Smith","year":"2010","journal-title":"Mol. 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Res."},{"key":"10.1016\/j.bbcan.2026.189675_bb0785","doi-asserted-by":"crossref","first-page":"3561","DOI":"10.1158\/0008-5472.CAN-21-4045","article-title":"A novel selective inhibitor JBI-589 targets PAD4-mediated neutrophil migration to suppress tumor progression","volume":"82","author":"Deng","year":"2022","journal-title":"Cancer Res."},{"key":"10.1016\/j.bbcan.2026.189675_bb0790","doi-asserted-by":"crossref","first-page":"389","DOI":"10.1016\/j.celrep.2018.03.051","article-title":"JMJD1B demethylates H4R3me2s and H3K9me2 to facilitate gene expression for development of hematopoietic stem and progenitor cells","volume":"23","author":"Li","year":"2018","journal-title":"Cell Rep."},{"key":"10.1016\/j.bbcan.2026.189675_bb0795","doi-asserted-by":"crossref","first-page":"6","DOI":"10.1186\/s13072-020-00331-1","article-title":"JMJD1B, a novel player in histone H3 and H4 processing to ensure genome stability","volume":"13","author":"Saavedra","year":"2020","journal-title":"Epigenetics Chromatin"},{"key":"10.1016\/j.bbcan.2026.189675_bb0800","doi-asserted-by":"crossref","first-page":"186","DOI":"10.1016\/j.ccell.2018.04.011","article-title":"Biological role and therapeutic potential of IDH mutations in cancer","volume":"34","author":"Waitkus","year":"2018","journal-title":"Cancer Cell"},{"key":"10.1016\/j.bbcan.2026.189675_bb0805","doi-asserted-by":"crossref","DOI":"10.3390\/toxins12050320","article-title":"Extracting and analyzing pyrrolizidine alkaloids in medicinal plants: a review","volume":"12","author":"Kopp","year":"2020","journal-title":"Toxins (Basel)"},{"key":"10.1016\/j.bbcan.2026.189675_bb0810","doi-asserted-by":"crossref","DOI":"10.3389\/fphar.2022.982424","article-title":"Recent advances of IDH1 mutant inhibitor in cancer therapy","volume":"13","author":"Tian","year":"2022","journal-title":"Front. 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