Results 311 to 320 of about 793,543 (339)
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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 ...
Ye, Fang +2 more
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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, J A, Gallagher, G, Bilbe
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Fingerprinting G-protein-coupled receptors
"Protein Engineering, Design and Selection", 1994Recently we reported the design of a discriminating fingerprint for rhodopsin-like G-protein-coupled receptors (GPCRs). The fingerprint encodes the seven putative membrane-spanning motifs and was potently diagnostic of all GPCRs (52 in all) in version 8.1 of the OWL composite sequence database, readily distinguishing them from all other integral ...
T K, Attwood, J B, Findlay
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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 ...
Xavier, Deupi, Brian, Kobilka
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Efficacy at g-protein-coupled receptors
Nature Reviews Drug Discovery, 2002At 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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Downregulation of G protein-coupled receptors
Current Opinion in Neurobiology, 2000Major advances have been made in understanding mechanisms mediating downregulation of G protein-coupled receptors. Recent studies emphasize the role of multiple proteolytic mechanisms in downregulation. A specific mechanism of downregulation, mediated by endocytosis of receptors via clathrin-coated pits followed by sorting to lysosomes, has been ...
P, Tsao, M, von Zastrow
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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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Yeast Assays for G-Protein-Coupled Receptors
Receptors and Channels, 2002The functional coupling of heterologous G protein-coupled receptors (GPCRs) to the pheromone-response pathway of the budding yeast Saccharomyces cerevisiae is well established as an experimental system for ligand identification and for characterizing receptor pharmacology and signal transduction mechanisms.
S J, Dowell, A J, Brown
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Oligomerisation of G-protein-coupled receptors
Journal of Cell Science, 2001ABSTRACT A range of approaches have recently provided evidence that G-protein-coupled receptors can exist as oligomeric complexes. Both homo-oligomers, comprising multiple copies of the same gene product, and hetero-oligomers containing more than one receptor have been detected.
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G‐Protein–Coupled Receptor Deorphanizations
2005G protein–coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend.
Yumiko, Saito, Olivier, Civelli
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