The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
Bioorg Med Chem Lett
; 20(2): 493-8, 2010 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-20005104
ABSTRACT
Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the potential function of FFA2 in various disease conditions.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Receptores de Superfície Celular
/
Receptores Acoplados a Proteínas G
/
Acetamidas
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article