Structural and Mechanistic Basis of the Inhibitory Potency of Selected 2-Aminothiazole Compounds on Protein Kinase CK2.
J Med Chem
; 63(14): 7766-7772, 2020 07 23.
Article
em En
| MEDLINE
| ID: mdl-32589844
ABSTRACT
Selective inhibitors of protein kinase CK2 with significant cytotoxicity on tumor cells based on a 2-aminothiazole scaffold were described recently. Here, these studies are supplemented with representative CK2α/CK2α' complex structures. They reveal that the 2-aminothiazole-based inhibitors occupy the ATP cavity, whereas preliminary data had indicated an allosteric binding site. The crystal structure findings are corroborated by subsequent enzyme kinetic studies; their atomic-resolution quality provides the basis for future optimization of these promising CK2 inhibitors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Caseína Quinase II
/
Inibidores de Proteínas Quinases
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article