Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen.
Chem Commun (Camb)
; 55(69): 10214-10217, 2019 Aug 22.
Article
in En
| MEDLINE
| ID: mdl-31380528
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Azoles
/
Peptidyl Transferases
/
Organoselenium Compounds
/
Enzyme Inhibitors
/
Mycobacterium tuberculosis
Limits:
Humans
Language:
En
Journal:
Chem Commun (Camb)
Journal subject:
QUIMICA
Year:
2019
Document type:
Article