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Cell-based assays in GPCR drug discovery.

Siehler Wagner, Sandra (2008) Cell-based assays in GPCR drug discovery. Biotechnology Journal, 3 (4). pp. 471-483. ISSN 1860-7314


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.

Item Type: Article
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Additional Information: archiving not allowed on institutional repository
Keywords: Adenylyl cyclase; Extracellular signal-regulated kinase; G protein-coupled receptor; Phospholipase C; Rho
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Date Deposited: 14 Dec 2009 13:52
Last Modified: 31 Jan 2013 01:04


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