蛋白水解靶向嵌合体在白血病靶向治疗中的研究进展  

The Recent Findings of PROTAC in Targeted Therapies for Leukemia

作　　者：辛本凯 郭磊 肖业臣[1,2] 张纪周 Xin Benkai;Guo Lei;Xiao Yechen;Zhang Jizhou(Department of Biochemistry,College of Basic Medical Sciences,Jilin University,Changchun 130021;Department of Biotechnology,College of Basic Medical Sciences,Guangdong Medical University,Dongguan 523000)

机构地区：[1]吉林大学基础医学院生物化学教研室,长春130021 [2]广东医科大学基础医学院生物技术系,东莞523000

出　　处：《国际老年医学杂志》2021年第6期376-380,共5页International Journal of Geriatrics

基　　金：国家自然科学基金青年基金项目(82000390);中国博士后科学基金第68批面上资助项目(2020M681048);广东医科大学学科建设项目(81570149);。

摘　　要：蛋白水解靶向嵌合体(PROTAC)是一种双功能分子,通过使靶蛋白(POI)泛素化,继而使其在蛋白酶体中降解,这种蛋白降解机制已广泛用于与疾病相关的蛋白质降解中。利用PROTAC的靶向蛋白质降解可能会成为白血病靶向治疗中药物研发的新方向。本文将介绍PROTAC的研究进展及其在白血病靶向治疗中的应用。Proteolysis targeting chimeras(PROTACs)are heterobifunctional molecules that mediate the degradation of protein of interest(POI)by ubiquitination and subsequent degradation in the proteasome.This protein degradation mechanism has been used to degrade various types of disease-related proteins.Therefore,targeted protein degradation using PROTAC may be a new direction of targeted therapies for leukemia.This review focuses on recent findings of PROTAC application in targeted therapies for leukemia.

关 键 词：蛋白降解 白血病 靶向治疗 PROTAC 

分 类 号：R733.7[医药卫生—肿瘤]