{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,23]],"date-time":"2026-09-23T16:10:20Z","timestamp":1790179820667,"version":"4.1.0"},"reference-count":45,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2024,12,1]],"date-time":"2024-12-01T00:00:00Z","timestamp":1733011200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100010029","name":"Taishan Scholar Foundation of Shandong Province","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100010029","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100007129","name":"Natural Science Foundation of Shandong Province","doi-asserted-by":"publisher","award":["ZR2018ZC0233"],"award-info":[{"award-number":["ZR2018ZC0233"]}],"id":[{"id":"10.13039\/501100007129","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100007129","name":"Natural Science Foundation of Shandong Province","doi-asserted-by":"publisher","award":["ZR2022LSW013"],"award-info":[{"award-number":["ZR2022LSW013"]}],"id":[{"id":"10.13039\/501100007129","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["82273892"],"award-info":[{"award-number":["82273892"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81874308"],"award-info":[{"award-number":["81874308"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["82361138572"],"award-info":[{"award-number":["82361138572"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic Chemistry"],"published-print":{"date-parts":[[2024,12]]},"DOI":"10.1016\/j.bioorg.2024.107801","type":"journal-article","created":{"date-parts":[[2024,9,3]],"date-time":"2024-09-03T19:12:23Z","timestamp":1725390743000},"page":"107801","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":7,"special_numbering":"C","title":["Discovery of novel 20S proteasome subunit \u03b25 PROTAC degraders as potential therapeutics for pharyngeal carcinoma and Bortezomib-resistant multiple myeloma"],"prefix":"10.1016","volume":"153","author":[{"given":"Shumei","family":"Wang","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhenzhen","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Siyue","family":"Ma","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shuxin","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shuxian","family":"Guo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhao","family":"Ma","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lupei","family":"Du","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Minyong","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"issue":"6779","key":"10.1016\/j.bioorg.2024.107801_b0005","doi-asserted-by":"crossref","first-page":"770","DOI":"10.1038\/35008096","article-title":"Rapid degradation of a large fraction of newly synthesized proteins by proteasomes","volume":"404","author":"Schubert","year":"2000","journal-title":"Nature"},{"issue":"3","key":"10.1016\/j.bioorg.2024.107801_b0010","doi-asserted-by":"crossref","first-page":"249","DOI":"10.1111\/j.1756-185X.2012.01737.x","article-title":"The ubiquitin proteasome system and efficacy of proteasome inhibitors in diseases","volume":"15","author":"Chitra","year":"2012","journal-title":"Int. J. Rheum. Dis."},{"issue":"22","key":"10.1016\/j.bioorg.2024.107801_b0015","doi-asserted-by":"crossref","first-page":"3500","DOI":"10.1016\/j.jmb.2017.05.027","article-title":"Proteasome Structure and Assembly","volume":"429","author":"Budenholzer","year":"2017","journal-title":"J. Mol. Biol."},{"issue":"2","key":"10.1016\/j.bioorg.2024.107801_b0020","doi-asserted-by":"crossref","first-page":"170","DOI":"10.1124\/pr.117.015370","article-title":"A Practical Review of Proteasome Pharmacology","volume":"71","author":"Thibaudeau","year":"2019","journal-title":"Pharmacol. Rev."},{"key":"10.1016\/j.bioorg.2024.107801_b0025","doi-asserted-by":"crossref","first-page":"132","DOI":"10.1016\/j.abb.2015.12.012","article-title":"Mammalian proteasome subtypes: Their diversity in structure and function","volume":"591","author":"Dahlmann","year":"2016","journal-title":"Arch. Biochem. Biophys."},{"key":"10.1016\/j.bioorg.2024.107801_b0030","doi-asserted-by":"crossref","unstructured":"M. Unno, T. Mizushima, Y. Morimoto, Y. Tomisugi, K. Tanaka, N. Yasuoka, T. Tsukihara, The structure of the mammalian 20S proteasome at 2.75 angstrom resolution, Structure (London, England : 1993) 10(5) (2002) 609-618.","DOI":"10.1016\/S0969-2126(02)00748-7"},{"issue":"1","key":"10.1016\/j.bioorg.2024.107801_b0035","doi-asserted-by":"crossref","first-page":"79","DOI":"10.1038\/nrm1552","article-title":"Proteolysis: from the lysosome to ubiquitin and the proteasome","volume":"6","author":"Ciechanover","year":"2005","journal-title":"Nat. Rev. Mol. Cell Biol."},{"issue":"7","key":"10.1016\/j.bioorg.2024.107801_b0040","doi-asserted-by":"crossref","first-page":"307","DOI":"10.1016\/S1359-6446(03)02647-3","article-title":"Potential for proteasome inhibition in the treatment of cancer","volume":"8","author":"Adams","year":"2003","journal-title":"Drug Discov. Today"},{"issue":"4 Suppl 92","key":"10.1016\/j.bioorg.2024.107801_b0045","first-page":"S74","article-title":"The immunoproteasome: a novel drug target for autoimmune diseases","volume":"33","author":"Basler","year":"2015","journal-title":"Clin. Exp. Rheumatol."},{"key":"10.1016\/j.bioorg.2024.107801_b0050","doi-asserted-by":"crossref","first-page":"73","DOI":"10.3389\/fnmol.2014.00073","article-title":"The ubiquitin proteasome system in glia and its role in neurodegenerative diseases","volume":"7","author":"Jansen","year":"2014","journal-title":"Front. Mol. Neurosci."},{"issue":"5","key":"10.1016\/j.bioorg.2024.107801_b0055","doi-asserted-by":"crossref","DOI":"10.3390\/biom10050796","article-title":"Unstructured Biology of Proteins from Ubiquitin-Proteasome System: Roles in Cancer and Neurodegenerative Diseases","volume":"10","author":"Gadhave","year":"2020","journal-title":"Biomolecules"},{"issue":"2","key":"10.1016\/j.bioorg.2024.107801_b0060","doi-asserted-by":"crossref","first-page":"117","DOI":"10.1517\/13543784.15.2.117","article-title":"Targeting the proteasome as a therapeutic strategy against haematological malignancies","volume":"15","author":"Orlowski","year":"2006","journal-title":"Expert Opin Inv Drug"},{"issue":"4","key":"10.1016\/j.bioorg.2024.107801_b0065","doi-asserted-by":"crossref","first-page":"804","DOI":"10.1042\/BST20140126","article-title":"Overcoming bortezomib resistance in multiple myeloma","volume":"42","author":"Murray","year":"2014","journal-title":"Biochem Soc T"},{"issue":"9","key":"10.1016\/j.bioorg.2024.107801_b0070","doi-asserted-by":"crossref","first-page":"4701","DOI":"10.1021\/acs.jmedchem.9b02161","article-title":"Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma","volume":"63","author":"Zhou","year":"2020","journal-title":"J. Med. Chem."},{"issue":"46","key":"10.1016\/j.bioorg.2024.107801_b0075","doi-asserted-by":"crossref","first-page":"13162","DOI":"10.1073\/pnas.1608067113","article-title":"Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma","volume":"113","author":"Hideshima","year":"2016","journal-title":"PNAS"},{"issue":"1","key":"10.1016\/j.bioorg.2024.107801_b0080","doi-asserted-by":"crossref","first-page":"13","DOI":"10.1186\/2050-7771-1-13","article-title":"The resistance mechanisms of proteasome inhibitor bortezomib","volume":"1","author":"L\u00fc","year":"2013","journal-title":"Biomark Res"},{"issue":"10","key":"10.1016\/j.bioorg.2024.107801_b0085","doi-asserted-by":"crossref","first-page":"1278","DOI":"10.1016\/j.exphem.2008.04.013","article-title":"Overexpression of the PSMB5 gene contributes to bortezomib resistance in T-lymphoblastic lymphoma\/leukemia cells derived from Jurkat line","volume":"36","author":"L\u00fc","year":"2008","journal-title":"Exp. Hematol."},{"issue":"6","key":"10.1016\/j.bioorg.2024.107801_b0090","doi-asserted-by":"crossref","first-page":"2489","DOI":"10.1182\/blood-2007-08-104950","article-title":"Molecular basis of bortezomib resistance: proteasome subunit beta5 (PSMB5) gene mutation and overexpression of PSMB5 protein","volume":"112","author":"Oerlemans","year":"2008","journal-title":"Blood"},{"issue":"12","key":"10.1016\/j.bioorg.2024.107801_b0095","doi-asserted-by":"crossref","first-page":"11840","DOI":"10.1074\/jbc.M413007200","article-title":"Overexpression of proteasome \u03b2 subunit increases the amount of assembled proteasome and confers ameliorated response to oxidative stress and higher survival rates","volume":"280","author":"Chondrogianni","year":"2005","journal-title":"J. Biol. Chem."},{"issue":"1","key":"10.1016\/j.bioorg.2024.107801_b0100","doi-asserted-by":"crossref","first-page":"102","DOI":"10.5301\/ijbm.5000283","article-title":"PSMB5 is associated with proliferation and drug resistance in triple-negative breast cancer","volume":"33","author":"Wei","year":"2018","journal-title":"Int J Biol Marker"},{"issue":"2","key":"10.1016\/j.bioorg.2024.107801_b0105","doi-asserted-by":"crossref","first-page":"212","DOI":"10.1016\/j.leukres.2011.09.011","article-title":"Bortezomib resistance in a myeloma cell line is associated to PSM\u03b25 overexpression and polyploidy","volume":"36","author":"Balsas","year":"2012","journal-title":"Leukemia Res"},{"issue":"5","key":"10.1016\/j.bioorg.2024.107801_b0110","doi-asserted-by":"crossref","DOI":"10.3390\/cancers13050951","article-title":"The Prognostic Value of Whole-Blood PSMB5, CXCR4, POMP, and RPL5 mRNA Expression in Patients with Multiple Myeloma Treated with Bortezomib","volume":"13","author":"Robak","year":"2021","journal-title":"Cancers"},{"issue":"7","key":"10.1016\/j.bioorg.2024.107801_b0115","doi-asserted-by":"crossref","first-page":"1230","DOI":"10.1093\/carcin\/bgq097","article-title":"G\u03b1 inhibition enhances the anticancer effect of bortezomib through PSMB5 downregulation","volume":"31","author":"Yang","year":"2010","journal-title":"Carcinogenesis"},{"key":"10.1016\/j.bioorg.2024.107801_b0120","doi-asserted-by":"crossref","DOI":"10.1016\/j.phymed.2020.153312","article-title":"Curcumin inhibits proteasome activity in triple-negative breast cancer cells through regulating p300\/miR-142-3p\/PSMB5 axis","volume":"78","author":"Liu","year":"2020","journal-title":"Phytomedicine"},{"issue":"1","key":"10.1016\/j.bioorg.2024.107801_b0125","article-title":"MiR-383 sensitizes osteosarcoma cells to bortezomib treatment via down-regulating PSMB5","volume":"51","author":"Wang","year":"2024","journal-title":"Mol Bio Rep"},{"issue":"12","key":"10.1016\/j.bioorg.2024.107801_b0130","first-page":"1884","article-title":"Dihydrocelastrol induces antitumor activity and enhances the sensitivity of bortezomib in resistant multiple myeloma by inhibiting STAT3-dependent PSMB5 regulation","volume":"55","author":"Jin","year":"2023","journal-title":"Acta Bioch Bioph Sin"},{"key":"10.1016\/j.bioorg.2024.107801_b0135","doi-asserted-by":"crossref","DOI":"10.1182\/blood-2020-141461","article-title":"Nx-2127, a Degrader of BTK and IMiD Neosubstrates, for the Treatment of B-Cell Malignancies","volume":"136","author":"Robbins","year":"2020","journal-title":"Blood"},{"issue":"7","key":"10.1016\/j.bioorg.2024.107801_b0140","article-title":"ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer","volume":"37","author":"Neklesa","year":"2019","journal-title":"J. Clin. Oncol."},{"issue":"4","key":"10.1016\/j.bioorg.2024.107801_b0145","article-title":"Novel chimeric small molecule AC682 potently degrades estrogen receptor with oral anti-tumor efficacy superior to fulvestrant","volume":"81","author":"He","year":"2021","journal-title":"Cancer Res."},{"issue":"4","key":"10.1016\/j.bioorg.2024.107801_b0150","doi-asserted-by":"crossref","first-page":"265","DOI":"10.1038\/s41571-023-00736-3","article-title":"Protein degraders enter the clinic - a new approach to cancer therapy","volume":"20","author":"Chirnomas","year":"2023","journal-title":"Nat. Rev. Clin. Oncol."},{"issue":"15","key":"10.1016\/j.bioorg.2024.107801_b0155","doi-asserted-by":"crossref","first-page":"8554","DOI":"10.1073\/pnas.141230798","article-title":"Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation","volume":"98","author":"Sakamoto","year":"2001","journal-title":"P Natl Acad Sci USA"},{"key":"10.1016\/j.bioorg.2024.107801_b0160","doi-asserted-by":"crossref","unstructured":"G.E. Winter, D.L. Buckley, J. Paulk, J.M. Roberts, A. Souza, S. Dhe-Paganon, J.E. Bradner, DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation, Science (New York, N.Y.) 348(6241) (2015) 1376-1381.","DOI":"10.1126\/science.aab1433"},{"issue":"12","key":"10.1016\/j.bioorg.2024.107801_b0165","doi-asserted-by":"crossref","first-page":"5214","DOI":"10.1039\/D2CS00193D","article-title":"PROTACs: past, present and future","volume":"51","author":"Li","year":"2022","journal-title":"Chem. Soc. Rev."},{"issue":"8","key":"10.1016\/j.bioorg.2024.107801_b0170","doi-asserted-by":"crossref","first-page":"998","DOI":"10.1016\/j.chembiol.2020.07.020","article-title":"PROTACs: An Emerging Therapeutic Modality in Precision Medicine","volume":"27","author":"Nalawansha","year":"2020","journal-title":"Cell Chem. Biol."},{"issue":"3","key":"10.1016\/j.bioorg.2024.107801_b0175","doi-asserted-by":"crossref","first-page":"181","DOI":"10.1038\/s41573-021-00371-6","article-title":"PROTAC targeted protein degraders: the past is prologue","volume":"21","author":"B\u00e9k\u00e9s","year":"2022","journal-title":"Nat. Rev. Drug Discov."},{"issue":"9","key":"10.1016\/j.bioorg.2024.107801_b0180","doi-asserted-by":"crossref","first-page":"1669","DOI":"10.1016\/j.apsb.2020.01.014","article-title":"First small-molecule PROTACs for G protein-coupled receptors: inducing \u03b1 (1A)-adrenergic receptor degradation","volume":"10","author":"Li","year":"2020","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.bioorg.2024.107801_b0185","doi-asserted-by":"crossref","first-page":"15","DOI":"10.1016\/j.ddtec.2019.01.002","article-title":"PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future","volume":"31","author":"Pettersson","year":"2019","journal-title":"Drug Discov. Today Technol."},{"issue":"16","key":"10.1016\/j.bioorg.2024.107801_b0190","doi-asserted-by":"crossref","first-page":"7066","DOI":"10.1039\/D2CS00220E","article-title":"Chemistries of bifunctional PROTAC degraders","volume":"51","author":"Cao","year":"2022","journal-title":"Chem. Soc. Rev."},{"issue":"2","key":"10.1016\/j.bioorg.2024.107801_b0195","doi-asserted-by":"crossref","first-page":"337","DOI":"10.1002\/ddr.22026","article-title":"Progress of small molecules for targeted protein degradation: PROTACs and other technologies","volume":"84","author":"Zhao","year":"2023","journal-title":"Drug Develop Res"},{"issue":"6","key":"10.1016\/j.bioorg.2024.107801_b0200","doi-asserted-by":"crossref","first-page":"2726","DOI":"10.1021\/jm500045x","article-title":"Structurally Novel Highly Potent Proteasome Inhibitors Created by the Structure-Based Hybridization of Nonpeptidic Belactosin Derivatives and Peptide Boronates","volume":"57","author":"Kawamura","year":"2014","journal-title":"J. Med. Chem."},{"issue":"14","key":"10.1016\/j.bioorg.2024.107801_b0205","doi-asserted-by":"crossref","first-page":"4192","DOI":"10.1021\/jm9005093","article-title":"Design, Synthesis, Biological Evaluation, and Structure-Activity Relationship (SAR) Discussion of Dipeptidyl Boronate Proteasome Inhibitors Part I: Comprehensive Understanding of the SAR of \u03b1-Amino Acid Boronates","volume":"52","author":"Zhu","year":"2009","journal-title":"J. Med. Chem."},{"issue":"34","key":"10.1016\/j.bioorg.2024.107801_b0210","doi-asserted-by":"crossref","first-page":"7105","DOI":"10.1016\/j.tet.2009.06.042","article-title":"A convergent approach to synthesis of bortezomib: the use of TBTU suppresses racemization in the fragment condensation","volume":"65","author":"Ivanov","year":"2009","journal-title":"Tetrahedron"},{"key":"10.1016\/j.bioorg.2024.107801_b0215","doi-asserted-by":"crossref","unstructured":"A. Frostell L. Vinterback H. Sjobom Protein-Ligand Interactions Using SPR Systems, Methods Mol Biol 2013, 1008, (Clifton, N.J.) 139 165.","DOI":"10.1007\/978-1-62703-398-5_6"},{"issue":"21","key":"10.1016\/j.bioorg.2024.107801_b0220","doi-asserted-by":"crossref","first-page":"5226","DOI":"10.1182\/blood.V124.21.5226.5226","article-title":"The Establishment of Bortezomib Resistant Myeloma Cell Line KM3\/BTZ and Explore the Resistance Mechanism","volume":"124","author":"Wang","year":"2014","journal-title":"Blood"},{"key":"10.1016\/j.bioorg.2024.107801_b0225","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2021.113608","article-title":"Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC)","volume":"222","author":"Li","year":"2021","journal-title":"Eur. J. Med. Chem."}],"container-title":["Bioorganic Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0045206824007065?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0045206824007065?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T23:02:53Z","timestamp":1778713373000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0045206824007065"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,12]]},"references-count":45,"alternative-id":["S0045206824007065"],"URL":"https:\/\/doi.org\/10.1016\/j.bioorg.2024.107801","relation":{},"ISSN":["0045-2068"],"issn-type":[{"value":"0045-2068","type":"print"}],"subject":[],"published":{"date-parts":[[2024,12]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of novel 20S proteasome subunit \u03b25 PROTAC degraders as potential therapeutics for pharyngeal carcinoma and Bortezomib-resistant multiple myeloma","name":"articletitle","label":"Article Title"},{"value":"Bioorganic Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bioorg.2024.107801","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2024 Elsevier Inc. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"107801"}}