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基于蛋白结构的靶向氨酰-tRNA合成酶的药物研究进展

Research progress in drugs targeting aminoacyl-tRNA synthetase based on protein structure
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摘要 在全球抗菌药物严重滥用的情况下,发展具有全新靶标的抗菌药物是一种重要的解决方案,目前,已有大量靶向氨酰-tRNA合成酶(aaRS)的药物被发现和改造。本文对aaRS的蛋白结构和作用机制进行了详细的介绍,并根据其蛋白结构特点总结了包括aaRS合成位点和催化位点的抗菌药物,并对这些药物的发现、改造和活性研究进行简要介绍,为进一步开发出以该靶点为作用目标的抗菌药物提供参考。 With antimicrobial abuse worldwide,the development of antimicrobial drugs with new targets is an important solution.Many drugs targeting aminoacyl-tRNA synthetase (aaRS) have been discovered and modified.This article introduces in detail the protein structure and action mechanism of aaRS,and summarizes the antibacterial drugs (including the synthesis site and catalytic site of aaRS) according to their protein structure characteristics.The discovery,modification and activity was briefly introduced to further develop antibacterial drugs targeting this target.
作者 罗菁汉 胡燕君 李政 苏睿 吴成军 孙铁民 LUO Jing-han;HU Yan-jun;LI Zheng;SU Rui;WU Cheng-jun;SUN Tie-min(Shenyang Pharmaceutical University Innovation Laboratory of Drug Research and Design,Ministry of Education,Shenyang 110016)
出处 《中南药学》 CAS 2020年第8期1283-1289,共7页 Central South Pharmacy
基金 国家自然科学基金青年项目(No.81903474)。
关键词 抗菌药物 氨酰-TRNA合成酶 氨酰-tRNA合成酶抑制剂 antibacterial aminoacyl-tRNA synthetase aminoacyl-tRNA synthetase inhibitor
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