A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1.
Acta Crystallogr F Struct Biol Commun
; 75(Pt 7): 515-519, 2019 Jul 01.
Article
en En
| MEDLINE
| ID: mdl-31282872
ABSTRACT
Protein kinase CK2a1 is a serine/threonine kinase that plays a crucial role in the growth, proliferation and survival of cells and is a well known target for tumour and glomerulonephritis therapies. Here, the crystal structure of the kinase domain of CK2a1 complexed with 5-iodotubercidin (5IOD), an ATP-mimetic inhibitor, was determined at 1.78â
Å resolution. The structure shows distinct structural features and, in combination with a comparison of the crystal structures of five off-target kinases complexed with 5IOD, provides valuable information for the development of highly selective inhibitors.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Proteínas Serina-Treonina Quinasas
/
Inhibidores de Proteínas Quinasas
Límite:
Humans
Idioma:
En
Revista:
Acta Crystallogr F Struct Biol Commun
Año:
2019
Tipo del documento:
Article
País de afiliación:
Japón