Advances of bacterial transferase Mra Y and its inhibitors  

细菌转位酶MraY及其抑制剂的研究进展（英文）

作　　者：金媛媛[1] 刘娟娟[1,2] 冯晓洲[1] 李亚东[1,2] 汪康游 孙婉[1] 田喜凤[2] 杨兆勇[1] 

机构地区：[1]中国医学科学院北京协和医学院,医药生物技术研究所,卫生部抗生素生物工程重点实验室,北京100050 [2]河北联合大学,河北唐山063000

出　　处：《Journal of Chinese Pharmaceutical Sciences》2015年第3期137-147,共11页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.81273414 and Grant No.81321004);NSFC-NIH International Cooperation and Exchange Programs(Grant No.81261120417,2012-2013)

摘　　要：The phospho-mur NAc-pentapeptide translocase（Mra Y, translocase I） is a good target for the development of new antibiotics as it is ubiquitous and essential for bacterial growth. Furthermore, several inhibitors targeting towards this enzyme have been discovered. Recently, the crystal structure of Mra Y has been presented by Chung et al. Combination of the crystal structure and structure-activity relationship studies on these inhibitors could lead to the identification of active pharmacophores, and insight into their mechanisms of action. In this review, we described the structure and inhibitors of Mra Y. In addition, we also discussed the structure-activity relationship of these inhibitors and prospects of Mra Y as an antibacterial target.磷酸-N-乙酰胞壁酸酯-胸腺喷丁转位酶(Mra Y,转位酶I)是细菌中普遍存在且对细菌生长有重要作用的一种酶,是发展新的抗菌药物的重要靶点。此外,几类此酶的抑制剂已经被发现。近来,Mra Y的晶体结构也被Chung等阐明。结合晶体结构及其抑制剂的构效关系研究将有助于活性药效团的确定和对作用机制的深入了解。本文概述了Mra Y的整体结构及其抑制剂,并对这些抑制剂的构效关系和Mra Y作为抗菌药物靶点的前景进行了讨论。

关 键 词：PEPTIDOGLYCAN Mra Y Antibiotic Structure-activity relationships 

分 类 号：R96[医药卫生—药理学]