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Review Article

靶向雌激素受体的PROTACs综述：生物学和药物研究成果

卷 29, 期 22, 2022

发表于: 13 January, 2022

页: [3922 - 3944] 页: 23

弟呕挨: 10.2174/0929867328666211110101018

价格: $65

Open Access Journals Promotions 2
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摘要

雌激素受体（ER）是类固醇激素受体，它属于一个大型核受体家族。内分泌疾病与雌激素受体信号失调密切相关。传统疗法继续依赖小分子抑制剂，包括芳香化酶抑制剂（AIs）和选择性雌激素受体调节剂（SERM），所有这些都会对内分泌治疗产生获得性抵抗。蛋白水解靶向嵌合体（PROTACs）具有前所未有的解决获得性内分泌抵抗的潜力。ARV-471是Arvinas开发的一种靶向ER的PROTAC，在2019年时被美国FDA认定为一种研究新药，并启动了一项针对局部晚期或转移性ER阳性/HER2阴性乳腺癌患者的I期试验。在这篇综述中，我们将重点介绍从内分泌疾病治疗的出版物和专利中开发ER靶向PROTAC的进展。

关键词: 蛋白质水解靶向嵌合体，雌激素受体（ERs），核受体，DNA结合功能域，α雌激素受体多肽，β雌激素受体多肽

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