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The structure and function of G-protein-coupled receptors.

Nature

Signal Transduction, Animals, Conserved Sequence, Cytoplasm, metabolism, Humans, Opsins, chemistry, Protein Conformation, Receptors, G-Protein-Coupled

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      Abstract

      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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      Journal
      19458711
      3967846
      10.1038/nature08144

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