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Structural diversity of G protein-coupled receptors and significance for drug discovery.

Lagerström MC, Schiöth HB

Department of Neuroscience, Functional Pharmacology, Uppsala University, BMC, BOX 593, 751 24, Uppsala, Sweden.

G protein-coupled receptors (GPCRs) are the largest family of membrane-bound receptors and also the targets of many drugs. Understanding of the functional significance of the wide structural diversity of GPCRs has been aided considerably in recent years by the sequencing of the human genome and by structural studies, and has important implications for the future therapeutic potential of targeting this receptor family. This article aims to provide a comprehensive overview of the five main human GPCR families--Rhodopsin, Secretin, Adhesion, Glutamate and Frizzled/Taste2--with a focus on gene repertoire, general ligand preference, common and unique structural features, and the potential for future drug discovery.

Published 2 April 2008 in Nat Rev Drug Discov, 7(4): 339-57.
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