MCR-1: a promising target for structure-based design of inhibitors to tackle polymyxin resistance,Drug Discovery Today

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MCR-1: a promising target for structure-based design of inhibitors to tackle polymyxin resistance
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-07-20 , DOI: 10.1016/j.drudis.2018.07.004
Soo Jung Son , Renjie Huang , Christopher J. Squire , Ivanhoe K.H. Leung

The spread of a novel mobile colistin resistance gene (mcr1) has jeopardised the use of polymyxins, last-resort antibiotics that are used increasingly to treat infections caused by multidrug-resistant (MDR) Gram-negative pathogens. In early 2017, the WHO reported the global spread of mcr1 within a few years after its initial discovery in China. The protein encoded by mcr1 is a putative 60-kDa phosphoethanolamine (pEtN) transferase, MCR-1, and has been studied extensively since its discovery. Herein, we present a comprehensive review of MCR-1 covering its structure, function, and mechanism, to call for the rational drug design of molecular inhibitors of MCR-1 to use in colistin-based combination therapies.

更新日期：2018-07-20

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