Results 231 to 240 of about 356,759 (248)

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
openaire   +2 more sources

Activation of G Protein–Coupled Receptors

2007
G 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
openaire   +2 more sources

Efficacy at g-protein-coupled receptors

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 ...
openaire   +2 more sources

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
openaire   +2 more sources

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.
openaire   +2 more sources

Yeast Assays for G-Protein-Coupled Receptors

Receptors and Channels, 2002
The 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
openaire   +3 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.
openaire   +2 more sources

G‐Protein–Coupled Receptor Deorphanizations

2005
G 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
openaire   +2 more sources

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

Adrenergic Receptors As Models For G Protein-Coupled Receptors

Annual Review of Neuroscience, 1992
Approximately 80% of known hormones and neurotransmitters activate cellular signal transduction mechanisms by activating G protein-coupled receptors (Birnbaumer et al 1990). Studying the structure and function of these receptors has been challenging because they are not naturally abun­ dant proteins and they require a lipid environment to be fully ...
openaire   +2 more sources