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

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.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/c9cc04145a

Authors


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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
Expand authors...
Publisher:
Royal Society of Chemistry Publisher's website
Journal:
Chemical Communications Journal website
Volume:
55
Issue:
69
Article number:
10214
Publication date:
2019-08-05
Acceptance date:
2019-06-25
DOI:
EISSN:
1364-548X
ISSN:
1359-7345
Source identifiers:
1028648
Pubs id:
pubs:1028648
UUID:
uuid:3e16fb22-e697-412c-b913-4757c08a9e43
Local pid:
pubs:1028648
Deposit date:
2019-07-08

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