首页|选择性雌激素受体降解剂研究进展

选择性雌激素受体降解剂研究进展

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1雌激素受体阳性乳腺癌是乳腺癌最常见的亚型,内分泌治疗是其主要的治疗手段.为克服内分泌治疗中药物不耐受和耐药等问题,开发选择性雌激素受体降解剂(SERD)成为研究热点.为改善SERD的药动学特性,多个口服SERD的临床研究取得了阳性结果.同时,为提高雌激素受体的降解效率,还利用蛋白水解靶向嵌合体、分子胶降解等靶蛋白降解技术开发新型SERD药物.综述内分泌治疗的现状、口服SERD的开发和临床研究及新型雌激素受体降解技术药物的研发进展,以期为改善乳腺癌患者的预后提供参考.
Advances in Selective Estrogen Receptor Degraders
Estrogen receptor-positive breast cancer is the most common subtype,which is most commonly treated with endocrine therapy.In order to address the issues of drug resistance and intolerance in endocrine therapy,selective estrogen receptor degrader(SERD)has become a hotspot in the research.Several oral SERDs have been developed to improve the pharmacokinetic properties with positive results in several clinical studies.Besides,novel target protein degradation technologies have been adopted to improve the degradation efficiency of estrogen receptor,with new SERDs being developed through protein hydrolysis targeting chimera and molecular gel technologies.This article reviews the status of endocrine therapy and the progress in the development and clinical research of oral SERD and novel protein degradation drugs,in the hope of providing some reference for the improvement of the prognosis of breast cancer patients.

selective estrogen receptor degraderprotein hydrolysis targeting chimeramolecular glue degrader

房文通、郭明鑫、曹孟妲、殷咏梅

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南京医科大学第一附属医院/江苏省人民医院药学部,江苏南京 210029

宜兴市人民医院药学部,江苏无锡 214200

东南大学附属中大医院药学部,江苏南京 210009

南京医科大学第一附属医院/江苏省人民医院肿瘤科,江苏南京 210029

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雌激素受体降解剂 蛋白水解靶向嵌合体 分子胶降解

国家自然科学基金江苏省人民医院优秀中青年人才支持计划

82204454YNRCQN0306

2024

药学进展
中国药科大学

药学进展

影响因子:0.624
ISSN:1001-5094
年,卷(期):2024.48(2)
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