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G-Protein-Coupled Receptor Microarrays
ChemBioChem, 2002Membrane-bound proteins represent the single most important class of drug targets. Arraying these proteins is difficult because they typically need to be embedded in membranes to maintain their correctly folded conformations. We describe here the fabrication of microarrays consisting of G-protein-coupled receptors (GPCRs)--the single largest family of ...
Anthony G. Frutos +2 more
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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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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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Molecular signatures of G-protein-coupled receptors
Nature, 2013A. Venkatakrishnan +6 more
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2019
NOVEL LIGANDS: LIGAND SCREENING SYSTEMS AND ORPHAN RECEPTORS Measurement of Competitive and Allosteric Interactions in Radioligand Binding Studies-S. Lazareno and N.Birdsall Ligand Screening of G Protein-Coupled Receptors in Yeast-J. Hadcock and M. Pausch Ligand Screening Using Melanophore Cells: Frog Skin to Combinatorial Chemistry-J.
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NOVEL LIGANDS: LIGAND SCREENING SYSTEMS AND ORPHAN RECEPTORS Measurement of Competitive and Allosteric Interactions in Radioligand Binding Studies-S. Lazareno and N.Birdsall Ligand Screening of G Protein-Coupled Receptors in Yeast-J. Hadcock and M. Pausch Ligand Screening Using Melanophore Cells: Frog Skin to Combinatorial Chemistry-J.
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Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors
Nature, 1996H. Daub +3 more
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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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