G-protein-coupled receptors


G-protein-coupled receptors

G-protein-coupled receptors (GPCRs) are among the largest and most diverse family of proteins in the mammalian genome, which transduce signals as a response to a wide range of stimuli. GPCRs are major targets in drug discovery, as reflected by the fact that they encompass about 50% of current medicinal compounds. In humans, the completed human genome project has led to the identification of over 865 GPCR genes. The diversity of GPCRs is dictated not only by the variety of stimuli that they respond to, but also their participation in various signaling pathways. Their widespread expression, especially on the cell surface, that makes them accessible to antagonists, agonists, hormones and drugs, as well as tissue and cell type specificity, which provide selectivity for the receptors and ligands. Exploration of various drug targets has lead to the identification of multiple ways in which GPCRs contribute to a disease state. Classification of GPCR related diseases fall into categories of either rare.

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