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Review
. 2020 Aug 15:200:112390.
doi: 10.1016/j.ejmech.2020.112390. Epub 2020 May 4.

MmpL3 inhibitors as antituberculosis drugs

Affiliations
Review

MmpL3 inhibitors as antituberculosis drugs

Min Shao et al. Eur J Med Chem. .

Abstract

The mycobacterial membrane protein Large 3 (MmpL3) is an inner membrane protein that transports trehalose-monomycolates, precursors for trehalose-dimycolates and mycolic acids that make up essential components of the mycobacterial outer membrane. Inhibition of MmpL3 weakens the mycobacterial cell wall and ultimately results in cell death in both in vitro and in vivo infection models. This highlights the therapeutic potential of MmpL3 as a drug target. High-throughput whole-cell screening along with whole genome sequencing of resistant mutants has identified numerous classes of compounds that can be classified as MmpL3 inhibitors. In this review, we provide insights into the current development of various MmpL3 inhibitors and discuss the potential challenges in this area.

Keywords: Antituberculosis drug; Drug design; MmpL3 inhibitor; SAR.

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Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing interests or personal relationships that could have appeared to influence the work reported in this paper.

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