靶向半胱天冬蛋白酶-3前体的抗肿瘤药物研究进展  

Advance of Anti-tumor Drugs Targeting Procaspase-3

作　　者：易勤 朱刚直[1] YI Qin;ZHU Gangzhi(The Affiliated Haikou Hospital of Xiangya School of Medicine,Central South University,Haikou,Hainan,570311,China)

机构地区：[1]中南大学湘雅医学院附属海口医院,海南海口570311

出　　处：《肿瘤药学》2018年第3期318-323,共6页Anti-Tumor Pharmacy

摘　　要：半胱天冬蛋白酶-3前体(Procaspase-3)是细胞凋亡级联反应的关键执行者,在多种肿瘤细胞中过表达。首次发现的小分子化合物半天冬蛋白酶-3活化物1(PAC-1)是基于Procaspase-3激活而导致肿瘤细胞凋亡的。本文以PAC-1及其衍生物S-PAC-1、SM-1、WF-210和WF-208为代表,就其构效关系、作用机制、抗肿瘤活性以及药代动力学的研究成果作一综述,为新的Procaspase-3靶向药物的设计和研发提供参考依据。Caspase-3 is a critical executor in apoptosis cascade and is over-expressed in many tumor cells.Procaspase-activating compound 1(PAC-1),the first discovered small molecule compound,could induce the apoptosis of tumor cells on the base of the activation of Procaspase-3.In this paper,PAC-1 and its derivatives like S-PAC-1,SM-1,WF-210 and WF-208,are representative,and their structure-activity relationship,mechanism,anti-tumor activity and pharmacokinetics research results are reviewed.It provides references for the design and research of new Procaspase-3 targeting drugs.

关 键 词：Procasepase-3 抗肿瘤药物 PAC-1 细胞凋亡 衍生物 

分 类 号：R96[医药卫生—药理学]