Results 271 to 280 of about 851,179 (309)
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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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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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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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G Protein-Coupled Receptor Pharmacogenetics
2008Common G protein-coupled receptor (GPCR) gene variants that encode receptor proteins with a distinct sequence may alter drug efficacy without always resulting in a disease phenotype. GPCR genetic loci harbor numerous variants, such as DNA insertions or deletions and single-nucleotide polymorphisms that alter GPCR expression and function, thereby ...
Miles D, Thompson +2 more
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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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Ubiquitination of G-Protein-Coupled Receptors
2004In this chapter we describe methods for detecting the ubiquitination state of G-protein-coupled receptors (GPCRs). This involves coexpression of a GPCR with an epitope-tagged ubiquitin construct in a heterologous expression system. Modification by ubiquitin of the GPCR resulting from agonist activation is detected by immunoprecipation and subsequent ...
Adriano, Marchese, Jeffrey L, Benovic
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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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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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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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