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Efficacy at g-protein-coupled receptors [PDF]
Nature Reviews Drug Discovery, 2002 At present, the drug-discovery process centres on ligands that either block or produce physiological responses. However, there are therapeutic uses for ligands that do neither of these things, but which still affect receptors in other ways. This review discusses the intimate relationship between the affinity of a ligand for its receptor, and the ...
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G-protein coupled receptors in bone
Frontiers in Bioscience, 1998The skeleton is a dynamic structure that undergoes continuous remodeling, a prerequisite to meeting the constant loading demands placed upon it. This process is controlled by a multitude of systemic and local factors which interact with receptors presented on the surface of both osteoblasts and osteoclasts; the osteogenic and osteolytic cells of bone ...
W.B. Bowler +2 more
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Deorphanization of G-Protein-Coupled Receptors
2007G-protein-coupled receptors constitute one of the major families of drug targets. Orphan receptors, for which the ligands and function are still unknown, are an attractive set of future targets for presently unmet medical needs. Screening strategies have been developed over the years in order to identify the natural ligands of these receptors.
Parmentier, Marc, Detheux, Michel
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The family of G‐protein‐coupled receptors
The FASEB Journal, 1995The family of G-protein-coupled receptors can be defined by their similar structural and functional characteristics. Although their primary sequences are quite diverse, these proteins share several common structural features that reflect their common mechanism of action.
Michael R. Tota +3 more
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Activation of G Protein–Coupled Receptors
2007G protein-coupled receptors (GPCRs) mediate responses to hormones and neurotransmitters, as well as the senses of sight, smell, and taste. These remarkably versatile signaling molecules respond to structurally diverse ligands. Many GPCRs couple to multiple G protein subtypes, and several have been shown to activate G protein-independent signaling ...
Brian K. Kobilka, Xavier Deupi
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G protein—coupled receptor kinases
Cell, 1993G protein‐coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein‐coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
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Molecular signatures of G-protein-coupled receptors
Nature, 2013A. Venkatakrishnan +6 more
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Crystal Structure of Rhodopsin: A G‐Protein‐Coupled Receptor
ChemBioChem, 2002R. Stenkamp, D. Teller, K. Palczewski
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Mechanisms of signalling and biased agonism in G protein-coupled receptors
Nature reviews. Molecular cell biology, 2018D. Wootten +6 more
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