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Cell. 2012 Sep 28;151(1):14-23. doi: 10.1016/j.cell.2012.09.003.

Restructuring G-protein- coupled receptor activation.

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Department of Biochemistry, Institute for Research in Immunology and Cancer, Université de Montréal, QC, Canada.


G-protein-coupled receptors serve as key signal transduction conduits, linking extracellular inputs with diverse cellular responses. These receptors eluded structural characterization for decades following their identification. A landmark structure of rhodopsin provided a basis for structure-function studies and homology modeling, but advances in receptor biology suffered from a lack of receptor-specific structural insights. The recent explosion in GPCR structures confirms some features predicted by rhodopsin-based models, and more importantly, it reveals unexpected ligand-binding modes and critical aspects of the receptor activation process. The new structures also promise to foster studies testing emerging models for GPCR function such as receptor dimerization and ligand-biased signaling.

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