The structure and function of G-protein-coupled receptors.
Rosenbaum, Daniel M. 1; Rasmussen, Soren G. F. 1; Kobilka, Brian K. 1
[Review]
Nature.
459(7245):356-363, May 21, 2009.
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: G-protein-coupled receptors (GPCRs) mediate most of our physiological responses to hormones, neurotransmitters and environmental stimulants, and so have great potential as therapeutic targets for a broad spectrum of diseases. They are also fascinating molecules from the perspective of membrane-protein structure and biology. Great progress has been made over the past three decades in understanding diverse GPCRs, from pharmacology to functional characterization in vivo. Recent high-resolution structural studies have provided insights into the molecular mechanisms of GPCR activation and constitutive activity.
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