靶向雌激素受体的PROTACs的开发：一种对抗内分泌抵抗的新兴技术。
Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance.
作者信息
Peng Rouming, Liu Xin, Chen Chun-Chi, Guo Rey-Ting, Min Jian
机构信息
State Key Laboratory of Biocatalysis and Enzyme Engineering, National & Local Joint Engineering Research Center of High-throughput Drug Screening Technology, School of Life Sciences, Hubei University Wuhan 430062 China
Department of Immunology and Pathogen Biology, School of Basic Medical Sciences, Hangzhou Normal University Hangzhou 311121 China.
出版信息
RSC Med Chem. 2024 Dec 30. doi: 10.1039/d4md00961d.
Despite the success of endocrine therapies in treating ER-positive breast cancer, the development of resistance remains a significant challenge. Estrogen receptor targeting proteolysis-targeting chimeras (ER PROTACs) offer a unique approach by harnessing the ubiquitin-proteasome system to degrade ER, potentially bypassing resistance mechanisms. In this review, we present the drug design, efficacy and early clinical trials of these ER PROTACs. This review underscores the academic and industrial opportunities presented by this emerging technology, as well as the challenges that must be addressed to translate these findings into effective clinical therapies.
尽管内分泌疗法在治疗雌激素受体（ER）阳性乳腺癌方面取得了成功，但耐药性的产生仍然是一个重大挑战。靶向雌激素受体的蛋白酶靶向嵌合体（ER PROTACs）通过利用泛素-蛋白酶体系统降解ER，提供了一种独特的方法，有可能绕过耐药机制。在这篇综述中，我们介绍了这些ER PROTACs的药物设计、疗效和早期临床试验。这篇综述强调了这项新兴技术带来的学术和产业机遇，以及将这些研究结果转化为有效的临床疗法必须解决的挑战。
Zotero 插件