Subtleties in GPCR drug discovery: a medicinal chemistry perspective.
Drug Discov Today
; 17(19-20): 1133-8, 2012 Oct.
Article
en En
| MEDLINE
| ID: mdl-22732182
ABSTRACT
Therapeutic effects through G protein-coupled receptors (GPCRs) are promoted by a full agonist, partial agonist, neutral antagonist or inverse agonist. Dramatic change of function such as from a neutral antagonist to a full agonist with minimal variation of ligand structure is a phenomenon that medicinal chemists often encounter. This is also influenced by a change of assay format. The subtle nature of structure-function relationships is difficult to grasp unless carefully considered from both chemistry and assay perspectives. In this article we discuss the subtle aspects of GPCR drug discovery from the medicinal chemistry perspective.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores Acoplados a Proteínas G
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Drug Discov Today
Asunto de la revista:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Año:
2012
Tipo del documento:
Article
País de afiliación:
Japón