当前位置: X-MOL 学术Chem. Soc. Rev. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
SERDs: a case study in targeted protein degradation
Chemical Society Reviews ( IF 46.2 ) Pub Date : 2022-09-08 , DOI: 10.1039/d2cs00117a
Lucia Wang 1 , Abhishek Sharma 1
Affiliation  

Endocrine therapies for breast cancer target ERα which is found in more than 70% of breast cancers. Unfortunately, endocrine resistance typically occurs, in which case Selective Estrogen Receptor Degraders (SERDs) represent the last line of treatment for metastatic breast cancer patients. Fulvestrant, the only currently approved SERD and one of the first targeted protein degradation therapies, presents poor drug-like properties which has led to the development of a new generation of oral SERDs. This review summarizes recent progress in the evolution of SERDs, focusing on clinical candidates and their degradation motifs within the broader context of targeted protein degradation therapies.

中文翻译:

SERD:靶向蛋白质降解的案例研究

乳腺癌的内分泌治疗靶向 ERα,ERα 存在于 70% 以上的乳腺癌中。不幸的是,通常会发生内分泌抗性,在这种情况下,选择性雌激素受体降解剂 (SERD) 代表了转移性乳腺癌患者的最后一线治疗。Fulvestrant 是目前唯一获批的 SERD,也是最早的靶向蛋白质降解疗法之一,其药物样特性较差,这导致了新一代口服 SERD 的开发。本综述总结了 SERD 进化的最新进展,重点关注临床候选物及其在靶向蛋白质降解疗法的更广泛背景下的降解基序。
更新日期:2022-09-08
down
wechat
bug