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Adv Exp Med Biol. 2014;796:3-13. doi: 10.1007/978-94-007-7423-0_1.

The GPCR crystallography boom: providing an invaluable source of structural information and expanding the scope of homology modeling.

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Department of Chemistry and Center for Behavioral Neuroscience, American University, Washington, DC, 20016, USA,


G protein-coupled receptors (GPCRs) are integral membrane proteins of high pharmaceutical interest. Until relatively recently, their structures have been particularly elusive, and rhodopsin has been for many years the only member of the superfamily with experimentally elucidated structures. However, a number of recent technical and scientific advancements made the determination of GPCR structures more feasible, thus leading to the solution of the structures of several receptors. Besides providing direct structural information, these experimental GPCR structures also provide templates for the construction of GPCR models. In depth studies have been performed to probe the accuracy of these models, in particular with respect to the interactions with their ligands, and to assess their applicability the rational discovery of GPCR modulators. Given the current state of the art and the pace of the field, the future of GPCR structural studies is likely to be characterized by a landscape populated by an increasingly higher number of experimental and theoretical structures.

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