Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer,Journal of Medicinal Chemistry

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Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-11-02 , DOI: 10.1021/acs.jmedchem.0c00913
Yunlong Lu _{1,

2} , Wukun Liu _{1,

3,

4}

Affiliation

Estrogen receptor (ER) plays important roles in gene transcription and the proliferation of ER positive breast cancers. Selective modulation of ER has been a therapeutic target for this specific type of breast cancer for more than 30 years. Selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs) have been demonstrated to be effective therapeutic approaches for ER positive breast cancers. Unfortunately, 30–50% of ER positive tumors become resistant to SERM/AI treatment after 3–5 years. Fulvestrant, the only approved selective estrogen receptor degrader (SERD), is currently an important therapeutic approach for the treatment of endocrine-resistant breast cancers. The poor pharmacokinetic properties of fulvestrant have inspired the development of a new generation of oral SERDs to overcome drug resistance. In this review, we describe recent advances in ERα structure, functions, and mechanisms of endocrine resistance and summarize the development of oral SERDs in both academic and industrial areas.

中文翻译：

选择性雌激素受体降解剂（SERDs）：雌激素受体阳性内分泌抗性乳腺癌的有前途的策略

雌激素受体（ER）在ER阳性乳腺癌的基因转录和增殖中起重要作用。ER的选择性调节已超过30年来一直是这种特定类型乳腺癌的治疗目标。选择性雌激素受体调节剂（SERMs）和芳香化酶抑制剂（AIs）已被证明是ER阳性乳腺癌的有效治疗方法。不幸的是，3–5年后，有30–50％的ER阳性肿瘤对SERM / AI治疗产生抗药性。Fulvestrant是唯一获得批准的选择性雌激素受体降解剂（SERD），目前是治疗内分泌耐药性乳腺癌的重要治疗方法。氟维司群的不良药代动力学特性激发了新一代口服SERD克服耐药性的发展。在这篇评论中

更新日期：2020-12-24

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