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 targ...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.展开更多
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)
文摘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.