On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.
J Med Chem
; 50(26): 6722-4, 2007 Dec 27.
Article
em En
| MEDLINE
| ID: mdl-18052088
ABSTRACT
The estrogen-related receptor alpha (ERRalpha) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRalpha have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRgamma. The results suggest that ERRalpha may be intractable as a direct target for pharmacologic activation.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores de Estrogênio
/
Hidrazonas
Limite:
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article