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Issue 69, 2019
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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

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Publication details

The article was received on 30 May 2019, accepted on 25 Jun 2019 and first published on 05 Aug 2019


Article type: Communication
DOI: 10.1039/C9CC04145A
Chem. Commun., 2019,55, 10214-10217
  • Open access: Creative Commons BY license
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    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

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