Cell-based assays in GPCR drug discovery.
Biotechnol J
; 3(4): 471-83, 2008 Apr.
Article
em En
| MEDLINE
| ID: mdl-18383022
ABSTRACT
G protein-coupled receptors (GPCRs) transmit extracellular signals into the intracellular space, and play key roles in the physiological regulation of virtually every cell and tissue. Characteristic for the GPCR superfamily of cell surface receptors are their seven transmembrane-spanning alpha-helices, an extracellular N terminus and intracellular C-terminal tail. Besides transmission of extracellular signals, their activity is modulated by cellular signals in an auto- or transregulatory fashion. The molecular complexity of GPCRs and their regulated signaling networks triggered the interest in academic research groups to explore them further, and their drugability and role in pathophysiology triggers pharmaceutical research towards small molecular weight ligands and therapeutic antibodies. About 30% of marketed drugs target GPCRs, which underlines the importance of this target class. This review describes current and emerging cellular assays for the ligand discovery of GPCRs.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Bioensaio
/
Preparações Farmacêuticas
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Desenho de Fármacos
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Transdução de Sinais
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Sistemas de Liberação de Medicamentos
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Receptores Acoplados a Proteínas G
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Biotechnol J
Assunto da revista:
BIOTECNOLOGIA
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Suíça