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Targeting the Mycobacterium tuberculosis transpeptidase Ldt Mt2 with cysteine-reactive inhibitors including ebselen

DOI: 10.1039/C9CC04145A DOI Help

Authors: Mariska De Munnik (University of Oxford) , Christopher T. Lohans (University of Oxford; Queen's University, Canada) , Pauline A. Lang (University of Oxford) , Gareth W. Langley (University of Oxford) , Tika R. Malla (University of Oxford) , Anthony Tumber (University of Oxford) , Christopher J. Schofield (University of Oxford) , Jurgen Brem (University of Oxford)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Chemical Communications , VOL 469

State: Published (Approved)
Published: August 2019
Diamond Proposal Number(s): 18069 , 19458

Open Access Open Access

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.

Subject Areas: Biology and Bio-materials


Instruments: I04-Macromolecular Crystallography

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