Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen.
Chem Commun (Camb)
; 55(69): 10214-10217, 2019 Aug 22.
Article
em 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.
Texto completo:
1
Coleções:
01-internacional
Contexto em Saúde:
3_ND
Base de dados:
MEDLINE
Assunto principal:
Azóis
/
Peptidil Transferases
/
Compostos Organosselênicos
/
Inibidores Enzimáticos
/
Mycobacterium tuberculosis
Limite:
Humans
Idioma:
En
Revista:
Chem Commun (Camb)
Ano de publicação:
2019
Tipo de documento:
Article