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

Soo Jung Son1, Renjie Huang1, Christopher J Squire2

  • 1School of Chemical Sciences, The University of Auckland, Victoria Street West, Private Bag 92019, Auckland 1142, New Zealand.

Drug Discovery Today
|July 24, 2018
PubMed

Insights

The mobile colistin resistance gene (mcr1) threatens last-resort polymyxin antibiotics. This review details the MCR-1 enzyme

Area of Science:

  • Microbiology
  • Molecular Biology
  • Drug Resistance

Background:

  • The emergence of the mobile colistin resistance gene (mcr1) poses a significant threat to public health.
  • Colistin, a last-resort antibiotic, is crucial for treating multidrug-resistant (MDR) Gram-negative infections.
  • The global spread of mcr1, reported by WHO in 2017, necessitates a deeper understanding of its mechanisms.

Purpose of the Study:

  • To provide a comprehensive review of the MCR-1 enzyme.
  • To elucidate the structure, function, and mechanism of MCR-1.
  • To advocate for the rational drug design of MCR-1 inhibitors for combination therapies.

Main Methods:

  • Literature review of MCR-1 research.
  • Analysis of MCR-1 structure and function.
  • Exploration of MCR-1 inhibition strategies.

Main Results:

  • The mcr1 gene encodes a 60-kDa phosphoethanolamine (pEtN) transferase, MCR-1.
  • MCR-1 confers resistance to colistin by modifying the lipid A component of lipopolysaccharides.
  • Extensive research has been conducted on MCR-1 since its discovery.

Conclusions:

  • MCR-1 is a critical determinant of colistin resistance.
  • Understanding MCR-1's mechanism is key to developing effective countermeasures.
  • Targeting MCR-1 in drug design offers a promising strategy for combating MDR Gram-negative infections.

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