{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,3]],"date-time":"2026-07-03T16:21:22Z","timestamp":1783095682846,"version":"3.54.6"},"reference-count":30,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2027,5,22]],"date-time":"2027-05-22T00:00:00Z","timestamp":1810944000000},"content-version":"am","delay-in-days":233,"URL":"http:\/\/www.elsevier.com\/open-access\/userlicense\/1.0\/"},{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T00:00:00Z","timestamp":1790812800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100006545","name":"National Institute on Minority Health and Health Disparities","doi-asserted-by":"publisher","award":["U54MD007595"],"award-info":[{"award-number":["U54MD007595"]}],"id":[{"id":"10.13039\/100006545","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2026,10]]},"DOI":"10.1016\/j.ejmech.2026.118956","type":"journal-article","created":{"date-parts":[[2026,5,14]],"date-time":"2026-05-14T05:10:15Z","timestamp":1778735415000},"page":"118956","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":0,"special_numbering":"C","title":["Developing orally active estrogen receptor degraders by conjugation of boronic tamoxifen and cereblon ligands"],"prefix":"10.1016","volume":"315","author":[{"given":"Xianyou","family":"Peng","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ahamed","family":"Hossain","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Peng","family":"Ma","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shanchun","family":"Guo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Madhusoodanan","family":"Mottamal","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Changde","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shilong","family":"Zheng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Borui","family":"Kang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3999-8213","authenticated-orcid":false,"given":"Guangdi","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"issue":"32","key":"10.1016\/j.ejmech.2026.118956_bib1","doi-asserted-by":"crossref","first-page":"2447","DOI":"10.1080\/14796694.2024.2377530","article-title":"VERITAC-2: a phase III study of vepdegestrant, a PROTAC ER degrader, versus fulvestrant in ER+\/HER2- advanced breast cancer","volume":"20","author":"Hamilton","year":"2024","journal-title":"Future Oncol."},{"issue":"3","key":"10.1016\/j.ejmech.2026.118956_bib2","doi-asserted-by":"crossref","first-page":"431","DOI":"10.1007\/s11523-025-01137-5","article-title":"PROteolysis TArgeting chimera (PROTAC) estrogen receptor degraders for treatment of estrogen receptor-positive advanced breast cancer","volume":"20","author":"Hamilton","year":"2025","journal-title":"Targeted Oncol."},{"issue":"1","key":"10.1016\/j.ejmech.2026.118956_bib3","doi-asserted-by":"crossref","first-page":"33","DOI":"10.3390\/molecules31010033","article-title":"An update on clinically advanced PROTAC degraders and their synthesis","volume":"31","author":"Acharyya","year":"2025","journal-title":"Molecules"},{"issue":"8","key":"10.1016\/j.ejmech.2026.118956_bib4","doi-asserted-by":"crossref","first-page":"1089","DOI":"10.1021\/acs.bioconjchem.4c00253","article-title":"Targeted protein degradation (TPD) for immunotherapy: understanding proteolysis targeting chimera\u2010driven ubiquitin\u2010proteasome interactions","volume":"35","author":"Kamaraj","year":"2024","journal-title":"Bioconjug. Chem."},{"key":"10.1016\/j.ejmech.2026.118956_bib5","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2023.115127","article-title":"Developments of PROTACs technology in immune-related diseases","volume":"249","author":"Wang","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2026.118956_bib6","first-page":"6739","article-title":"Comparison of the short-term biological effects of 7alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17beta-diol (Faslodex) versus tamoxifen in postmenopausal women with primary breast cancer","volume":"61","author":"Robertson","year":"2001","journal-title":"Cancer Res."},{"issue":"24","key":"10.1016\/j.ejmech.2026.118956_bib7","doi-asserted-by":"crossref","first-page":"15094","DOI":"10.1021\/acs.jmedchem.0c00913","article-title":"Selective estrogen receptor degraders (SERDs): a promising strategy for estrogen receptor positive endocrine-resistant breast cancer","volume":"63","author":"Lu","year":"2020","journal-title":"J. Med. Chem."},{"issue":"30","key":"10.1016\/j.ejmech.2026.118956_bib8","doi-asserted-by":"crossref","first-page":"4594","DOI":"10.1200\/JCO.2010.28.8415","article-title":"Results of the CONFIRM phase III trial comparing fulvestrant 250 mg with fulvestrant 500 mg in postmenopausal women with estrogen receptor-positive advanced breast cancer","volume":"28","author":"Di Leo","year":"2010","journal-title":"J. Clin. Oncol."},{"issue":"6","key":"10.1016\/j.ejmech.2026.118956_bib9","doi-asserted-by":"crossref","first-page":"477","DOI":"10.1634\/theoncologist.7-6-477","article-title":"FDA drug approval summaries: fulvestrant","volume":"7","author":"Bross","year":"2002","journal-title":"Oncologist"},{"issue":"18","key":"10.1016\/j.ejmech.2026.118956_bib10","first-page":"6739","article-title":"Comparison of the short-term biological effects of 7alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17beta-diol (Faslodex) versus tamoxifen in postmenopausal women with primary breast cancer","volume":"61","author":"Robertson","year":"2001","journal-title":"Cancer Res."},{"issue":"1","key":"10.1016\/j.ejmech.2026.118956_bib11","doi-asserted-by":"crossref","first-page":"237","DOI":"10.1007\/s10549-011-1947-7","article-title":"Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: results from NEWEST, a randomized phase II study","volume":"133","author":"Kuter","year":"2012","journal-title":"Breast Cancer Res. Treat."},{"key":"10.1016\/j.ejmech.2026.118956_bib12","doi-asserted-by":"crossref","first-page":"138","DOI":"10.1016\/j.pharmthera.2017.02.027","article-title":"Targeted protein degradation by PROTACs","volume":"174","author":"Neklesa","year":"2017","journal-title":"Pharmacol. Ther."},{"issue":"3","key":"10.1016\/j.ejmech.2026.118956_bib13","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":"21","key":"10.1016\/j.ejmech.2026.118956_bib14","doi-asserted-by":"crossref","first-page":"19010","DOI":"10.1021\/acs.jmedchem.4c01521","article-title":"Discovery of ERD-1233 as a potent and orally efficacious estrogen receptor PROTAC degrader for the treatment of ER+ human breast cancer","volume":"67","author":"Acharyya","year":"2024","journal-title":"J. Med. Chem."},{"issue":"16","key":"10.1016\/j.ejmech.2026.118956_bib15","doi-asserted-by":"crossref","first-page":"3549","DOI":"10.1158\/1078-0432.CCR-23-3465","article-title":"Oral estrogen receptor PROTAC vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4\/6 or PI3K\/mTOR pathway inhibitors in preclinical ER+ breast cancer models","volume":"30","author":"Gough","year":"2024","journal-title":"Clin. Cancer Res."},{"key":"10.1016\/j.ejmech.2026.118956_bib16","doi-asserted-by":"crossref","first-page":"625","DOI":"10.1186\/s12885-015-1621-2","article-title":"Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status","volume":"15","author":"Zhong","year":"2015","journal-title":"BMC Cancer"},{"issue":"2","key":"10.1016\/j.ejmech.2026.118956_bib17","doi-asserted-by":"crossref","first-page":"283","DOI":"10.1007\/s10549-015-3461-9","article-title":"Boronic prodrug of endoxifen as an effective hormone therapy for breast cancer","volume":"152","author":"Zhang","year":"2015","journal-title":"Breast Cancer Res. Treat."},{"issue":"1","key":"10.1016\/j.ejmech.2026.118956_bib18","doi-asserted-by":"crossref","first-page":"102","DOI":"10.1021\/acsmedchemlett.6b00410","article-title":"Rational design of a boron-modified triphenylethylene (GLL398) as an oral selective estrogen receptor downregulator","volume":"8","author":"Liu","year":"2016","journal-title":"ACS Med. Chem. Lett."},{"issue":"2","key":"10.1016\/j.ejmech.2026.118956_bib19","doi-asserted-by":"crossref","first-page":"305","DOI":"10.1677\/joe.0.0750305","article-title":"A monohydroxylated metabolite of tamoxifen with potent antiestrogenic activity","volume":"75","author":"Jordan","year":"1977","journal-title":"J. Endocrinol."},{"issue":"22","key":"10.1016\/j.ejmech.2026.118956_bib20","doi-asserted-by":"crossref","first-page":"1609","DOI":"10.1056\/NEJM199811263392207","article-title":"Tamoxifen in the treatment of breast cancer","volume":"339","author":"Osborne","year":"1998","journal-title":"N. Engl. J. Med."},{"issue":"7","key":"10.1016\/j.ejmech.2026.118956_bib21","doi-asserted-by":"crossref","first-page":"927","DOI":"10.1016\/S0092-8674(00)81717-1","article-title":"The structural basis of estrogen receptor\/coactivator recognition and the antagonism of this interaction by tamoxifen","volume":"95","author":"Shiau","year":"1998","journal-title":"Cell"},{"issue":"8","key":"10.1016\/j.ejmech.2026.118956_bib22","doi-asserted-by":"crossref","first-page":"3522","DOI":"10.1021\/acs.jmedchem.5b00066","article-title":"Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic acids as oral selective estrogen receptor down-regulators","volume":"58","author":"Degorce","year":"2015","journal-title":"J. Med. Chem."},{"issue":"20","key":"10.1016\/j.ejmech.2026.118956_bib23","doi-asserted-by":"crossref","first-page":"7171","DOI":"10.1073\/pnas.0710802105","article-title":"Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method","volume":"105","author":"Dai","year":"2008","journal-title":"Proc. Natl. Acad. Sci. U. S. A"},{"issue":"22","key":"10.1016\/j.ejmech.2026.118956_bib24","doi-asserted-by":"crossref","first-page":"6772","DOI":"10.1021\/jm050723z","article-title":"A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats","volume":"48","author":"Hummel","year":"2005","journal-title":"J. Med. Chem."},{"issue":"16","key":"10.1016\/j.ejmech.2026.118956_bib25","doi-asserted-by":"crossref","first-page":"2251","DOI":"10.1002\/cbic.201000532","article-title":"Synthesis and crystal structure of a phosphorylated estrogen receptor ligand binding domain","volume":"11","author":"Mocklinghoff","year":"2010","journal-title":"Chembiochem"},{"issue":"6","key":"10.1016\/j.ejmech.2026.118956_bib26","doi-asserted-by":"crossref","first-page":"6924","DOI":"10.18632\/oncotarget.24023","article-title":"ZB716, a steroidal selective estrogen receptor degrader (SERD), is orally efficacious in blocking tumor growth in mouse xenograft models","volume":"9","author":"Guo","year":"2018","journal-title":"Oncotarget"},{"issue":"2","key":"10.1016\/j.ejmech.2026.118956_bib27","doi-asserted-by":"crossref","first-page":"359","DOI":"10.1007\/s10549-020-05558-w","article-title":"GLL398, an oral selective estrogen receptor degrader (SERD), blocks tumor growth in xenograft breast cancer models","volume":"180","author":"Guo","year":"2020","journal-title":"Breast Cancer Res. Treat."},{"key":"10.1016\/j.ejmech.2026.118956_bib28","unstructured":"Schr\u04e7dinger Release 2022-3: Glide, Schr\u04e7dinger, LLC, New York, NY, USA."},{"issue":"4","key":"10.1016\/j.ejmech.2026.118956_bib29","doi-asserted-by":"crossref","first-page":"1634","DOI":"10.1021\/acs.jcim.8b00872","article-title":"In silico modeling of PROTAC-mediated ternary complexes: validation and application","volume":"59","author":"Drummond","year":"2019","journal-title":"J. Chem. Inf. Model."},{"issue":"10","key":"10.1016\/j.ejmech.2026.118956_bib30","doi-asserted-by":"crossref","first-page":"5234","DOI":"10.1021\/acs.jcim.0c00897","article-title":"Improved accuracy for modeling PROTAC-mediated ternary complex formation and targeted protein degradation via new in silico methodologies","volume":"60","author":"Drummond","year":"2020","journal-title":"J. Chem. Inf. Model."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523426004010?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523426004010?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,7,3]],"date-time":"2026-07-03T15:41:30Z","timestamp":1783093290000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523426004010"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,10]]},"references-count":30,"alternative-id":["S0223523426004010"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2026.118956","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2026,10]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Developing orally active estrogen receptor degraders by conjugation of boronic tamoxifen and cereblon ligands","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2026.118956","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2026 Elsevier Masson SAS. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"118956"}}