Results 281 to 290 of about 393,484 (315)

Deorphanization of G-Protein-Coupled Receptors

2007
G-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
openaire   +3 more sources

Fingerprinting G-protein-coupled receptors

"Protein Engineering, Design and Selection", 1994
Recently 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

2008
Common 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, Katherine A, Siminovitch, David E C, Cole   +2 more
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Downregulation of G protein-coupled receptors

Current Opinion in Neurobiology, 2000
Major 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

2004
In 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
openaire   +2 more sources

Oligomerisation of G-protein-coupled receptors

Journal of Cell Science, 2001
ABSTRACT 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 kinases

Cell, 1993
G 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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G Protein‐Coupled Receptor Kinases

Journal of Neurochemistry, 1994
T, Haga, K, Haga, K, Kameyama
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G-Protein-Coupled Receptors

2006
S.B. Liggett, D.W. McGraw
openaire   +1 more source

Dimerization of G-Protein Coupled Receptors

Neuropsychopharmacology, 2000
L A, Devi, L S, Brady
openaire   +2 more sources