High-throughput screen with the <scp>l,d</scp>-transpeptidase Ldt<sub>Mt2</sub> of <i>Mycobacterium tuberculosis</i> reveals novel classes of covalently reacting inhibitors-Reference-Cited by-同舟云学术

High-throughput screen with the l,d-transpeptidase Ldt_Mt2 of Mycobacterium tuberculosis reveals novel classes of covalently reacting inhibitors

Published:2023 Issue:26 Volume:14 Page:7262-7278
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

de Munnik Mariska¹^ORCID,Lang Pauline A.¹^ORCID,De Dios Anton Francisco²,Cacho Mónica²^ORCID,Bates Robert H.²^ORCID,Brem Jürgen¹^ORCID,Rodríguez Miquel Beatriz²^ORCID,Schofield Christopher J.¹^ORCID

Affiliation:

1. Chemistry Research Laboratory, Department of Chemistry, the Ineos Oxford Institute of Antimicrobial Research, University of Oxford, 12 Mansfield Road, Oxford, OX1 3TA, UK

2. Tres Cantos Medicines Development Campus, GlaxoSmithKline, Calle Severo Ochoa 2, Tres Cantos, Madrid, Spain

Abstract

10 000 electrophilic compounds were screened for inhibition of the essential l,d-transpeptidase (LdtMt2) of Mycobacterium tuberculosis. Potent covalently reacting inhibitors were identified and characterised by protein X-ray and MS studies.

Funder

Biotechnology and Biological Sciences Research Council

Medical Research Foundation

Wellcome Trust

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/SC/D2SC06858C

Reference59 articles.

1. Global tuberculosis report 2020 , Report Licence: CC BY-NC-SA 3.0 IGO, World Health Organization , Geneva , 2020