Journal article
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
- Publisher:
- Royal Society of Chemistry
- Journal:
- Chemical Communications More from this journal
- Volume:
- 55
- Issue:
- 69
- Article number:
- 10214
- Publication date:
- 2019-08-05
- Acceptance date:
- 2019-06-25
- DOI:
- EISSN:
-
1364-548X
- ISSN:
-
1359-7345
- Pubs id:
-
pubs:1028648
- UUID:
-
uuid:3e16fb22-e697-412c-b913-4757c08a9e43
- Local pid:
-
pubs:1028648
- Source identifiers:
-
1028648
- Deposit date:
-
2019-07-08
- ARK identifier:
Terms of use
- Copyright holder:
- The Royal Society of Chemistry
- Copyright date:
- 2019
- Notes:
- © The Royal Society of Chemistry 2019. Open Access. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Supplementary materials are available online from the Royal Society of Chemistry at: http://doi.org/10.1039/C9CC04145A
- Licence:
- CC Attribution (CC BY)
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