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Cell‐based assays in GPCR drug discovery
Author(s) -
Siehler Sandra
Publication year - 2008
Publication title -
biotechnology journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.144
H-Index - 84
eISSN - 1860-7314
pISSN - 1860-6768
DOI - 10.1002/biot.200800001
Subject(s) - g protein coupled receptor , drug discovery , extracellular , intracellular , biology , receptor , microbiology and biotechnology , computational biology , cell signaling , signal transduction , superfamily , transmembrane protein , small molecule , cell , biochemistry
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 α‐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.