Strategies for the identification of allosteric modulators of G-protein-coupled receptors.
Biochem Pharmacol
; 81(6): 691-702, 2011 Mar 15.
Article
en En
| MEDLINE
| ID: mdl-21184747
ABSTRACT
Once considered a pharmacological curiosity, allosteric modulation of seven transmembrane domain G-protein-coupled receptors (GPCRs) has emerged as a potentially powerful means to affect receptor function for therapeutic purposes. Allosteric modulators, which interact with binding sites topologically distinct from the orthosteric ligand binding sites, can potentially provide improved selectivity and safety, along with maintenance of spatial and temporal aspects of GPCR signaling. Accordingly, drug discovery efforts for GPCRs have increasingly focused on the identification of allosteric modulators. This review is devoted to an examination of the strategies, challenges, and opportunities for high-throughput screening for allosteric modulators of GPCRs, with particular focus on the identification of positive allosteric modulators.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores Acoplados a Proteínas G
/
Regulación Alostérica
/
Descubrimiento de Drogas
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Biochem Pharmacol
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos