Estrogen receptor α (ERα) is a crucial target for ERα positive breast cancer treatment. Previous drug discovery efforts were focused on developing inhibitors that targeted the canonical ligand binding pockets of the ligand binding domain (LBD) of ERα. However, significant percentage of patients developed cancer relapse with drug-resistance. ERα peptidomimetic modulators have been considered as promising treatments for drug resistant breast cancers as they are targeting ERα-coactivator interacting interface instead of the ligand binding pocket of ERα. Herein, we reviewed the recent development of ERα peptidomimetics antagonists.

中文翻译：

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靶向雌激素受体α-共激活因子相互作用的拟肽拮抗剂在癌症治疗中的最新进展

雌激素受体α（ERα）是ERα阳性乳腺癌治疗的关键靶标。先前的药物发现工作集中在开发针对ERα配体结合域（LBD）的规范配体结合口袋的抑制剂。然而，相当大比例的患者因耐药而复发。ERα拟肽调节剂被认为是抗药性乳腺癌的有前途的治疗方法，因为它们靶向ERα-共活化剂相互作用的界面而不是ERα的配体结合口袋。在这里，我们审查了ERα拟肽拮抗剂的最新发展。