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The superfamily of G-protein-coupled receptors (GPCRs) is the largest single class of receptors. In vertebrates, they are estimated to account for approximately 1% of the entire genome. Despite extremely diverse roles in the cell, all GPCRs share the structural hallmark of seven helical transmembrane domains. Most receptors are able to couple to and thus activate more than one G-protein subtype mediating the transduction of various signalling cascades.
GPCRs play key roles in a large number of physiological and pathophysiological conditions. Pathways involving GPCRs are the targets of hundreds of therapeutically useful drugs, including antihistamines, neuroleptics, antidepressants, and antihypertensives.
