蛋白降解靶向嵌合体药物的研究进展  

Research Progress of Proteolysis Targeting Chimera Drugs

作　　者：钱浩 周伟澄[1] 蔡正艳[1] QIAN Hao;ZHOU Weicheng;CAI Zhengyan(National Key Lab.of Lead Druggability Research,Shanghai Institute of Pharmaceutical Industry,State Institute of Pharmaceutical Industry,Shanghai 201203)

机构地区：[1]中国医药工业研究总院上海医药工业研究院,先导物成药性研究全国重点实验室,上海201203

出　　处：《中国医药工业杂志》2024年第6期750-760,共11页Chinese Journal of Pharmaceuticals

摘　　要：蛋白降解靶向嵌合体(PROTACs)是当前抗肿瘤药物研究的热点之一,具有抗肿瘤作用高效且持久、选择性好、毒性低的特点。文章总结了靶向雌激素受体、雄激素受体、BCR-ABL、组蛋白去乙酰化酶4以及甲基转移酶样3等PROTACs新药的研究进展。Proteolysis targeting chimeras(PROTACs)are currently one of the hot spots in antineoplastic agent research.They have efficient and durable anti-tumor effects,good selectivity,and low possible toxicity.This review summarizes the research progress of new PROTAC drugs targeting estrogen receptors,androgen receptors,BCR-ABL,histone deacetylase 4,methyltransferase-like 3.

关 键 词：蛋白降解靶向嵌合体 抗肿瘤活性 新药发现 临床研究 ARV-471 ARV-110 ARV-766 研究进展 

分 类 号：R979.1[医药卫生—药品] R914.2[医药卫生—药学]