以分子开关Ras蛋白为靶点的抗肿瘤药物研究进展  

Advances in Ras-targeted Anticancer Drugs

作　　者：庄健[1] 张奕华[1] 赖宜生[1] 

机构地区：[1]中国药科大学新药研究中心,天然药物活性组分与药效国家重点实验室,江苏省代谢性疾病药物重点实验室,江苏南京210009

出　　处：《药学进展》2016年第10期745-755,共11页Progress in Pharmaceutical Sciences

摘　　要：Ras原癌基因编码的蛋白是细胞信号转导中不可或缺的分子开关,在细胞增殖、分化、凋亡等生理过程中起着重要的作用。Ras基因的功能获得性突变是肿瘤发生和发展的重要驱动因素,因此多年来人们一直致力于靶向Ras蛋白的抗肿瘤药物研究。简介Ras的结构与功能及其与肿瘤的相关性,着重综述近年来靶向Ras的小分子抑制剂的研究进展。Ras is the first discovered proto-oncogene,and its encoded protein is an indispensable switch molecule playing critical roles in cell proliferation,differentiation and apoptosis.Moreover,the gain-of-function mutation of Ras is one of the most common oncogenic drivers.Great efforts have been in the study of Ras-targeted anticancer drugs for years.In this paper,the structure and function of Ras as well as its implication in tumorigenesis were introduced.Especially,the recent advances in small molecule Ras inhibitors were also reviewed.

关 键 词：分子开关 突变 RAS抑制剂 抗肿瘤药物 

分 类 号：R979.1[医药卫生—药品]