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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。
Phospho-N-acetylmuramicacid-thymidine translocase (Mra Y, translocase I) is an ubiquitous enzyme in bacteria that plays an important role in bacterial growth and is important for the development of new antimicrobials Targets. In addition, several classes of inhibitors of this enzyme have been discovered. Recently, the crystal structure of Mra Y has also been elucidated by Chung et al. The study of the structure-activity relationship of the crystal structure and its inhibitor will be helpful for the determination of the active pharmacophore and its deep understanding of the mechanism of action. This article summarizes the overall structure of Mra Y and its inhibitors, and discusses the structure-activity relationship of these inhibitors and the prospect of Mra Y as an antimicrobial target.