Mcl-1小分子抑制剂研究进展  

Research progress of small-molecule Mcl-1 inhibitors

作　　者：吴贯召 何雄 董雪洋 于日磊[1] 江涛[1] WU Guan-zhao;HE Xiong;DONG Xue-yang;YU Ri-lei;JIANG Tao(Key Laboratory of Marine Drugs,Ministry of Education of China,School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China)

机构地区：[1]中国海洋大学海洋药物教育部重点实验室医药学院,山东青岛266003

出　　处：《中国海洋药物》2018年第4期80-86,共7页Chinese Journal of Marine Drugs

基　　金：国家自然科学基金--山东省联合基金项目(U1706213;U1406403);山东省泰山学者专项资助

摘　　要：Mcl-1(myeloid cell leukemia-1)蛋白是Bcl-2(B-cell lymphoma-2)蛋白家族中重要的抗凋亡蛋白成员之一,在多种肿瘤细胞中过表达。Mcl-1蛋白的过表达不仅与肿瘤的发生发展密切相关,还会导致肿瘤细胞对化疗药物产生耐药性,因此以Mcl-1为靶点的小分子抑制剂是未来抗肿瘤药物研发的重点之一。本文对2012-2017年间发表的Mcl-1小分子抑制剂进行了综述,主要介绍小分子抑制剂的化学结构和生物活性,旨在为Mcl-1小分子抑制剂的深入研究以及更多海洋来源的新型Mcl-1小分子抑制剂的开发提供参考。Myeloid cell leukemia-1（Mcl-1）protein is one of the key anti-apoptotic protein members of the B-cell lymphoma-2 protein family.Overexpression of Mcl-1 is not only closely related to the tumor survival,but also leads to the resistance to chemotherapeutic drug.Therefore,developing small-molecule inhibitors targeting Mcl-1 is promising for cancer therapy.This review summarized the Mcl-1 small-molecule inhibitors published from 2012 to 2017,including their chemical structures and biological activities,and thus attracted the interest of chemists and biologists.

关 键 词：BCL-2 MCL-1 凋亡 小分子抑制剂 

分 类 号：R914[医药卫生—药物化学]