MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Bioorg Med Chem Lett
; 8(20): 2839-44, 1998 Oct 20.
Article
em En
| MEDLINE
| ID: mdl-9873633
ABSTRACT
In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with an IC50 of 0.07 microM for MEK 1 and 0.06 microM for MEK 2. U0126 can undergo isomerization and cyclization reactions to form a variety of products, both chemically and in vivo, all of which exhibit less affinity for MEK and lower inhibition of AP-1 activity than parent, U0126.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Butadienos
/
Proteínas Serina-Treonina Quinases
/
Inibidores Enzimáticos
/
Nitrilas
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
1998
Tipo de documento:
Article
País de afiliação:
Estados Unidos