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Issue 69, 2019

Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen

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Abstract

The L,D-transpeptidases (Ldts) are promising antibiotic targets for treating tuberculosis. We report screening of cysteine-reactive inhibitors against LdtMt2 from Mycobacterium tuberculosis. Structural studies on LdtMt2 with potent inhibitor ebselen reveal opening of the benzisoselenazolone ring by a nucleophilic cysteine, forming a complex involving extensive hydrophobic interactions with a substrate-binding loop.

Graphical abstract: Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen

Supplementary files

Article information


Submitted
30 May 2019
Accepted
25 Jun 2019
First published
05 Aug 2019

This article is Open Access

Chem. Commun., 2019,55, 10214-10217
Article type
Communication

Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen

M. de Munnik, C. T. Lohans, P. A. Lang, G. W. Langley, T. R. Malla, A. Tumber, C. J. Schofield and J. Brem, Chem. Commun., 2019, 55, 10214 DOI: 10.1039/C9CC04145A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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