{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Lee TK"],"funding":["National Cancer Institute","NCI NIH HHS","Welch Foundation"],"pagination":["2023-2043"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11249634"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["7(7)"],"pubmed_abstract":["Estrogen receptor coregulator binding modulators (ERXs) are a novel class of molecules targeting the interaction between estrogen receptor α (ERα) and its coregulator proteins, which has proven to be an attractive strategy for overcoming endocrine resistance in breast cancer. We previously reported ERX-11, an orally bioavailable tris-benzamide, that demonstrated promising antitumor activity against ERα-positive breast cancer cells. To comprehend the significance of the substituents in ERX-11, we carried out structure-activity relationship studies. In addition, we introduced additional alkyl substituents at either the N- or C-terminus to improve binding affinity and biological activity. Further optimization guided by conformational restriction led to the identification of a <i>trans</i>-4-p"],"journal":["ACS pharmacology & translational science"],"pubmed_title":["Structure-Activity Relationship Study of Tris-Benzamides as Estrogen Receptor Coregulator Binding Modulators."],"pmcid":["PMC11249634"],"funding_grant_id":["1R01CA223828","R01 CA223828","AT-1595","R01 CA262757","1R01CA262757"],"pubmed_authors":["Chen CY","Lee TK","Vadlamudi RK","Ahn JM","Kassees K","Viswanadhapalli S","Parra K"],"additional_accession":[]},"is_claimable":false,"name":"Structure-Activity Relationship Study of Tris-Benzamides as Estrogen Receptor Coregulator Binding Modulators.","description":"Estrogen receptor coregulator binding modulators (ERXs) are a novel class of molecules targeting the interaction between estrogen receptor α (ERα) and its coregulator proteins, which has proven to be an attractive strategy for overcoming endocrine resistance in breast cancer. We previously reported ERX-11, an orally bioavailable tris-benzamide, that demonstrated promising antitumor activity against ERα-positive breast cancer cells. To comprehend the significance of the substituents in ERX-11, we carried out structure-activity relationship studies. In addition, we introduced additional alkyl substituents at either the N- or C-terminus to improve binding affinity and biological activity. Further optimization guided by conformational restriction led to the identification of a <i>trans</i>-4-p","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Jul","modification":"2026-06-01T13:55:07.513Z","creation":"2026-04-08T13:04:44.01Z"},"accession":"S-EPMC11249634","cross_references":{"pubmed":["39022350"],"doi":["10.1021/acsptsci.4c00125"]}}