Small-molecule WNK inhibition regulates cardiovascular and renal function.
Nat Chem Biol
; 12(11): 896-898, 2016 Nov.
Article
em En
| MEDLINE
| ID: mdl-27595330
ABSTRACT
The With-No-Lysine (K) (WNK) kinases play a critical role in blood pressure regulation and body fluid and electrolyte homeostasis. Herein, we introduce the first orally bioavailable pan-WNK-kinase inhibitor, WNK463, that exploits unique structural features of the WNK kinases for both affinity and kinase selectivity. In rodent models of hypertension, WNK463 affects blood pressure and body fluid and electro-lyte homeostasis, consistent with WNK-kinase-associated physiology and pathophysiology.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Sistema Cardiovascular
/
Proteínas Serina-Treonina Quinases
/
Inibidores de Proteínas Quinases
/
Bibliotecas de Moléculas Pequenas
/
Imidazóis
/
Rim
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Nat Chem Biol
Assunto da revista:
BIOLOGIA
/
QUIMICA
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Estados Unidos