Metabolic Actions of the Type 1 Cholecystokinin Receptor: Its Potential as a Therapeutic Target.
Trends Endocrinol Metab
; 27(9): 609-619, 2016 09.
Article
en En
| MEDLINE
| ID: mdl-27156041
Cholecystokinin (CCK) regulates appetite and reduces food intake by activating the type 1 CCK receptor (CCK1R). Attempts to develop CCK1R agonists for obesity have yielded active agents that have not reached clinical practice. Here we discuss why, along with new strategies to target CCK1R more effectively. We examine signaling events and the possibility of developing agents that exhibit ligand-directed bias, to dissociate satiety activity from undesirable side effects. Potential allosteric sites of modulation are also discussed, along with desired properties of a positive allosteric modulator (PAM) without intrinsic agonist action as another strategy to treat obesity. These new types of CCK1R-active drugs could be useful as standalone agents or as part of a rational drug combination for management of obesity.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores de Colecistoquinina
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Trends Endocrinol Metab
Asunto de la revista:
ENDOCRINOLOGIA
/
METABOLISMO
Año:
2016
Tipo del documento:
Article
Pais de publicación:
Estados Unidos