靶向特定氨基酸的活性探针研究进展  

Research progress of active probes targeting specific aminoacids

作　　者：李惠兰[1] 杨尊华[2] 应宇琦 房元英[1] LI Hui-lan;YANG Zun-hua;YING Yu-qi;FANG Yuan-ying(National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation,Jiangxi University of Chinese Medicine,Nanchang 330004,China;College of Pharmacy,Jiangxi University of Chinese Medicine,Nanchang 330004,China)

机构地区：[1]江西中医药大学中药固体制剂制造技术国家工程研究中心,江西南昌330004 [2]江西中医药大学药学院,江西南昌330004

出　　处：《药学学报》2023年第6期1557-1565,共9页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(82160663);江西省教育厅科技项目(GJJ201211);江西省自然科学基金资助项目(20212BAB206015,20212BAB206016);江西中医药大学校级科技创新团队发展计划项目(CXTD22001)。

摘　　要：基于活性的蛋白质(蛋白质组)分析(ABPP)因为能够直接分析生命系统中酶活性,这个化学技术成为了这一广泛领域的关键组成部分。随着对亲电弹头和亲核氨基酸研究的不断深入,靶向氨基酸的活性探针在各种生物系统中的应用促进了各种疾病背景下新靶点的识别和抑制剂的发现。本文旨在总结和归纳靶向特定氨基酸的活性探针的设计和应用的最新进展,以期为进一步开发靶向特定氨基酸的共价抑制剂药物提供支持。Activity-based protein(proteomic)profiling(ABPP)has emerged as a key component of the broad field of chemical techniques capable of directly analyzing enzyme activity in living systems.With the deepening of research on electrophilic warheads and nucleophilic amino acids,and the continuous proposal and improvement of effective development strategies,the application of amino acid-targeting active probes in various biological systems has facilitated the identification,development of new targets in various disease contexts and discovery of inhibitors.The purpose of this review is to summarize the latest progress in the design and application of active probes targeting specific amino acids,in order to provide support for the further development of amino acid-targeted covalent inhibitordrugs.

关 键 词：氨基酸 靶向 活性探针 活性蛋白质分析 

分 类 号：R914[医药卫生—药物化学]