摘要
RAS原癌基因是人类重要的肿瘤相关基因,RAS基因突变可导致肿瘤的发生与发展。RAL是RAS-RalGEFs-RAL信号通路中的关键分子,在维护正常细胞的基本功能中起着重要的作用。然而RAL功能的异常与肿瘤的发生发展密切相关,因此靶向RAL的药物研发逐渐受到关注。本文主要简介RAL蛋白的结构、信号调控和生理功能,并且综述RAL与肿瘤相关性及其靶向药物研发的进展与未来趋势。
Ras proto oncogene is an important gene related to tumor in human, whose mutation drives the occurrence and development of 30% human tumors.RAL is a key molecule in RAS-RalGEFs-RAL signaling pathway, which plays an important role in maintaining the basic function of normal cells.However, the abnormal function of RAL is closely related to the tumorigenesis and development of tumor cells, so the research and development of drug targeting RAL is gradually concerned.In this review, we mainly introduce the protein structure, signal regulation and physiological function of RAL,the relationship between RAL and tumor, as well as the progress and future trend of RAL-targeted drugs.
作者
徐乔亮
张雅亮
闫超
赖宜生
XU Qiao-liang;ZHANG Ya-liang;YAN Chao;LAI Yi-sheng(Center of Drug Discovery,State Key Laboratory of National Medicines,Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases,China Pharmaceutical University,Nanjing 210009,China;State Key Laboratory of Pharmaceutical Biotechnology,School of Life Sciences,Nanjing University,Nanjing 210093,China)
出处
《中国药物化学杂志》
CAS
CSCD
2022年第2期152-160,共9页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(21977117、21877060)。
关键词
RAL
小G蛋白
变构抑制剂
钉合肽
膜定位抑制剂
RAL
small G protein
allosteric inhibitor
stapled peptide
membrane localization inhibitor
