Innovative functional cAMP assay for studying G protein-coupled receptors: application to the pharmacological characterization of GPR17.
Purinergic Signal
; 7(4): 463-8, 2011 Dec.
Article
en En
| MEDLINE
| ID: mdl-21773766
ABSTRACT
In this work, an innovative and non-radioactive functional cAMP assay was validated at the GPR17 receptor. This assay provides a simple and powerful new system to monitor G protein-coupled receptor activity through change in the intracellular cAMP concentration by using a mutant form of Photinus pyralis luciferase into which a cAMP-binding protein moiety has been inserted. Results, expressed as EC(50) or IC(50) values for agonists and antagonists, respectively, showed a strong correlation with those obtained with [(35)S]GTPγS binding assay, thus confirming the validity of this approach in the study of new ligands for GPR17. Moreover, this method allowed confirming that GPR17 is coupled with a G(αi).
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Idioma:
En
Revista:
Purinergic Signal
Año:
2011
Tipo del documento:
Article
País de afiliación:
Italia