Structural insights into G-protein-coupled receptor activation |
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Authors: | Weis William I Kobilka Brian K |
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Institution: | Department of Molecular & Cellular Physiology, Stanford University School of Medicine, USA. bill.weis@stanford.edu |
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Abstract: | G-protein-coupled receptors (GPCRs) are the largest family of eukaryotic plasma membrane receptors, and are responsible for the majority of cellular responses to external signals. GPCRs share a common architecture comprising seven transmembrane (TM) helices. Binding of an activating ligand enables the receptor to catalyze the exchange of GTP for GDP in a heterotrimeric G protein. GPCRs are in a conformational equilibrium between inactive and activating states. Crystallographic and spectroscopic studies of the visual pigment rhodopsin and two beta-adrenergic receptors have defined some of the conformational changes associated with activation. |
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