{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,21]],"date-time":"2026-07-21T01:03:08Z","timestamp":1784595788757,"version":"3.55.0"},"reference-count":26,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2026,1,1]],"date-time":"2026-01-01T00:00:00Z","timestamp":1767225600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81673354"],"award-info":[{"award-number":["81673354"]}],"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 &amp; Medicinal Chemistry"],"published-print":{"date-parts":[[2026,1]]},"DOI":"10.1016\/j.bmc.2025.118427","type":"journal-article","created":{"date-parts":[[2025,10,7]],"date-time":"2025-10-07T00:14:57Z","timestamp":1759796097000},"page":"118427","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":1,"special_numbering":"C","title":["Synthesis and degradation effect of PROTACs targeting EGFR triple mutants"],"prefix":"10.1016","volume":"132","author":[{"given":"Xiao-Xiao","family":"Xi","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hong-Yi","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Minhang","family":"Xin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shuai","family":"Mao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"San-Qi","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmc.2025.118427_bb0005","doi-asserted-by":"crossref","first-page":"4233s","DOI":"10.1158\/1078-0432.CCR-040005","article-title":"The role of gefitinib in lung cancer treatment","volume":"10","author":"Giaccone","year":"2004","journal-title":"Clin Cancer Res"},{"issue":"9","key":"10.1016\/j.bmc.2025.118427_bb0010","doi-asserted-by":"crossref","first-page":"2145","DOI":"10.1158\/2159-8290.CD-21-0226","article-title":"Targeting EGFR exon 20 insertions in non-small cell lung cancer: recent advances and clinical updates","volume":"11","author":"Meador","year":"2021","journal-title":"Cancer Discov"},{"issue":"5","key":"10.1016\/j.bmc.2025.118427_bb0015","doi-asserted-by":"crossref","first-page":"410","DOI":"10.1038\/s41573-023-00652-2","article-title":"Delivering on the promise of protein degraders","volume":"22","author":"O\u2019Brien Laramy","year":"2023","journal-title":"Nat Rev Drug Discov"},{"issue":"3","key":"10.1016\/j.bmc.2025.118427_bb0020","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":"3","key":"10.1016\/j.bmc.2025.118427_bb0025","doi-asserted-by":"crossref","first-page":"725","DOI":"10.1039\/D1CB00011J","article-title":"Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation","volume":"2","author":"Bond","year":"2021","journal-title":"RSC Chem Biol"},{"issue":"16","key":"10.1016\/j.bmc.2025.118427_bb0030","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":"4","key":"10.1016\/j.bmc.2025.118427_bb0035","doi-asserted-by":"crossref","first-page":"306","DOI":"10.2174\/1568009621666210203110857","article-title":"PROTACs: promising approaches for epigenetic strategies to overcome drug resistance","volume":"21","author":"Giardina","year":"2021","journal-title":"Curr Cancer Drug Tar"},{"key":"10.1016\/j.bmc.2025.118427_bb0040","doi-asserted-by":"crossref","first-page":"493","DOI":"10.1038\/s41568-025-00817-8","article-title":"Targeted protein degradation for cancer therapy","volume":"25","author":"Hinterndorfer","year":"2025","journal-title":"Nat Rev Cancer"},{"issue":"3","key":"10.1016\/j.bmc.2025.118427_bb0045","doi-asserted-by":"crossref","first-page":"422","DOI":"10.1002\/ddr.21765","article-title":"Proteolysis targeting chimera (PROTAC) for epidermal growth factor receptor enhances anti-tumor immunity in non-small cell lung cancer","volume":"82","author":"Wang","year":"2021","journal-title":"Drug Develop Res"},{"issue":"12","key":"10.1016\/j.bmc.2025.118427_bb0050","doi-asserted-by":"crossref","first-page":"8416","DOI":"10.1021\/acs.jmedchem.2c00345","article-title":"Exploring degradation of mutant and wild-type epidermal growth factor receptors induced by proteolysis-targeting chimeras","volume":"65","author":"Yu","year":"2022","journal-title":"J Med Chem"},{"issue":"95","key":"10.1016\/j.bmc.2025.118427_bb0055","doi-asserted-by":"crossref","first-page":"12852","DOI":"10.1039\/D1CC05715D","article-title":"Development of hypoxia-activated PROTAC exerting a more potent effect in tumor hypoxia than in normoxia","volume":"57","author":"Cheng","year":"2021","journal-title":"Chem Commun"},{"key":"10.1016\/j.bmc.2025.118427_bb0060","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.112781","article-title":"Discovery of potent small molecule PROTACs targeting mutant EGFR","volume":"208","author":"Zhao","year":"2020","journal-title":"Eur J Med Chem"},{"issue":"3","key":"10.1016\/j.bmc.2025.118427_bb0065","doi-asserted-by":"crossref","first-page":"1216","DOI":"10.1021\/acs.jmedchem.9b01566","article-title":"Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders","volume":"63","author":"Cheng","year":"2020","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2025.118427_bb0070","doi-asserted-by":"crossref","DOI":"10.1016\/j.bioorg.2022.105605","article-title":"Discovery of novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy","volume":"120","author":"Shi","year":"2022","journal-title":"Bioorg Chem"},{"issue":"12","key":"10.1016\/j.bmc.2025.118427_bb0075","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmcl.2020.127167","article-title":"Discovery and biological evaluation of proteolysis targeting chimeras (PROTACs) as an EGFR degraders based on osimertinib and lenalidomide","volume":"30","author":"He","year":"2020","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmc.2025.118427_bb0080","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.112199","article-title":"Design and synthesis of selective degraders of EGFRL858R\/T790M mutant","volume":"192","author":"Zhang","year":"2020","journal-title":"Eur J Med Chem"},{"key":"10.1016\/j.bmc.2025.118427_bb0085","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2022.114509","article-title":"Discovery of highly potent and selective CRBN-recruiting EGFRL858R\/T790M degraders in vivo","volume":"238","author":"Zhang","year":"2022","journal-title":"Eur J Med Chem"},{"issue":"6","key":"10.1016\/j.bmc.2025.118427_bb0090","doi-asserted-by":"crossref","first-page":"4709","DOI":"10.1021\/acs.jmedchem.1c01827","article-title":"Discovery of potent PROTACs targeting EGFR mutants through the optimization of covalent EGFR ligands","volume":"65","author":"Zhao","year":"2022","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2025.118427_bb0095","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.112061","article-title":"Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC)","volume":"189","author":"Zhang","year":"2020","journal-title":"Eur J Med Chem"},{"issue":"12","key":"10.1016\/j.bmc.2025.118427_bb0100","doi-asserted-by":"crossref","first-page":"1835","DOI":"10.1021\/acsmedchemlett.2c00459","article-title":"Potent PROTACs targeting EGFR mutants in drug discovery","volume":"13","author":"Kargbo","year":"2022","journal-title":"ACS Med Chem Lett"},{"issue":"7","key":"10.1016\/j.bmc.2025.118427_bb0105","doi-asserted-by":"crossref","first-page":"1060","DOI":"10.1158\/1535-7163.MCT-21-0835","article-title":"HJM-561, a potent, selective, and orally bioavailable EGFR PROTAC that overcomes osimertinib-resistant EGFR triple mutations","volume":"21","author":"Du","year":"2022","journal-title":"Mol Cancer Ther"},{"issue":"2","key":"10.1016\/j.bmc.2025.118427_bb0110","doi-asserted-by":"crossref","first-page":"278","DOI":"10.1021\/acsmedchemlett.1c00645","article-title":"Design, synthesis, and biological evaluation of novel EGFR PROTACs targeting Del19\/T790M\/C797S mutation","volume":"13","author":"Zhang","year":"2022","journal-title":"ACS Med Chem Lett"},{"key":"10.1016\/j.bmc.2025.118427_bb0115","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2023.115865","article-title":"Modification of osimertinib to discover new potent EGFRC797S-TK inhibitors","volume":"261","author":"Xi","year":"2023","journal-title":"Eur J Med Chem"},{"key":"10.1016\/j.bmc.2025.118427_bb0120","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2019.111888","article-title":"Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R\/T790M\/C797S mutant EGFR tyrosine kinase inhibitors","volume":"186","author":"Lei","year":"2020","journal-title":"Eur J Med Chem"},{"key":"10.1016\/j.bmc.2025.118427_bb0125","doi-asserted-by":"crossref","first-page":"10685","DOI":"10.1021\/jm301365e","article-title":"Structural optimization and structure activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations","volume":"55","author":"Yang","year":"2012","journal-title":"J Med Chem"},{"issue":"1","key":"10.1016\/j.bmc.2025.118427_bb0130","doi-asserted-by":"crossref","first-page":"78","DOI":"10.1016\/j.chembiol.2017.09.010","article-title":"Lessons in PROTAC design from selective degradation with a promiscuous warhead","volume":"25","author":"Bondeson","year":"2018","journal-title":"Cell Chem Biol"}],"container-title":["Bioorganic &amp; Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0968089625003682?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0968089625003682?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,6,5]],"date-time":"2026-06-05T05:04:30Z","timestamp":1780635870000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0968089625003682"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,1]]},"references-count":26,"alternative-id":["S0968089625003682"],"URL":"https:\/\/doi.org\/10.1016\/j.bmc.2025.118427","relation":{},"ISSN":["0968-0896"],"issn-type":[{"value":"0968-0896","type":"print"}],"subject":[],"published":{"date-parts":[[2026,1]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Synthesis and degradation effect of PROTACs targeting EGFR triple mutants","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmc.2025.118427","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Published by Elsevier Ltd.","name":"copyright","label":"Copyright"}],"article-number":"118427"}}