Structural basis for producing selective MAP2K7 inhibitors.
Bioorg Med Chem Lett
; 30(22): 127546, 2020 11 15.
Article
en En
| MEDLINE
| ID: mdl-32931911
ABSTRACT
Mitogen-activated protein kinase kinase 7 (MAP2K7) in the c-Jun N-terminal kinase signal cascade is an attractive drug target for a variety of diseases. The selectivity of MAP2K7 inhibitors against off-target kinases is a major barrier in drug development. We report a crystal structure of MAP2K7 complexed with a potent covalent inhibitor bearing an acrylamide moiety as an electrophile, which discloses a structural basis for producing selective and potent MAP2K7 inhibitors.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Acrilamida
/
MAP Quinasa Quinasa 7
/
Inhibidores de Proteínas Quinasas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2020
Tipo del documento:
Article
País de afiliación:
Japón