ARV-471在雌激素受体阳性乳腺癌治疗中的研究进展  

Research progresses of ARV-471 in therapy of estrogen receptor-positive breast cancer

作　　者：吴舒怡 张陶晶 姚萱捷 郝杰 Wu Shuyi;Zhang Taojing;Yao Xuanjie;Hao jie(College of Life Sciences Zhejiang Chinese Medicine University,Hangzhou 310053,China;the Fourth Clinical Medical College,Zhejiang Chinese Medicine University,Hangzhou 310053,China)

机构地区：[1]浙江中医药大学生命科学学院,杭州310053 [2]浙江中医药大学第四临床医学院,杭州310053

出　　处：《中华转移性肿瘤杂志》2024年第2期174-178,共5页Chinese Journal of Metastatic Cancer

基　　金：浙江中医药大学生命科学学院基本科研能力孵化项目(2022FH002)。

摘　　要：蛋白水解靶向嵌合体(PROTAC)技术是一种新型的靶向蛋白质降解技术,已经广泛应用于疾病相关蛋白的降解,在一定程度上解决了某些调控肿瘤的关键靶点的“不可成药”性和因靶点突变或表达水平增加导致的耐药性。利用这项技术研发出了一种靶向雌激素受体(ER)的口服新药——ARV-471,为ER阳性乳腺癌的治疗提供了新动力。为了促进乳腺癌治疗的进一步发展,本综述就PROTAC应用于转移性ER阳性乳腺癌治疗的可行性和必要性进行分析,为其治疗提供理论基础。Proteolysis-targeting chimera(PROTAC)technology is a novel targeted protein degradation technology,which has been widely used in the degradation of disease-related proteins.PROTAC has solved the"undrugability"of some key targets regulating tumors and drug resistance caused by mutations or increased expression levels of the targets to a certain extent.ARV-471,an oral new drug targeting estrogen receptor,was developed by using this technology,which provides a new impetus for therapy of estrogen receptor-positive breast cancer.In order to promote the further development of therapy for breast cancer,this review highligts the feasibility and necessity of PROTAC application for the therapy of metastatic estrogen receptor-positive breast cancer,and provides a theoretical basis for treatment of estrogen receptor-positive breast cancer.

关 键 词：蛋白水解靶向嵌合体 ARV-471 乳腺癌 

分 类 号：R737.9[医药卫生—肿瘤]