Results 311 to 320 of about 396,098 (353)

G Protein-Coupled Receptor Kinases

2005
As the largest family of membrane receptors, G protein-coupled receptors (GPCRs) transduce a large number of extracellular signals from hormones, neurotransmitters, chemokines, and other environmental stimuli to the interior of cells and play fundamental roles in the regulation of cellular functions.
Jingxia Gao, Xiaoqing Chen, Lan Ma
openaire   +2 more sources

Characterization of G protein-coupled receptor kinases

2002
Publisher Summary A basic feature of most cells is the ability to dynamically regulate their responsiveness to extracellular stimuli. Numerous stimuli transmit their signals via interaction with cell surface G protein-coupled receptors (GPCRs). GPCRs are subject to three principal modes of regulation: (1) desensitization, the process by which a ...
Jeffrey L. Benovic, Alexey Pronin, Robert P. Loudon   +2 more
openaire   +3 more sources

G-Protein–coupled receptor kinase expression in hypertension

Clinical Pharmacology & Therapeutics, 1999
In human hypertension we have recently identified an increase in lymphocyte G-protein receptor kinase-2 (GRK-2) protein expression, the key protein regulating the interaction between G-protein-coupled receptors and activation of adenylyl cyclase. However, it was not known whether this increase in GRK-2 protein expression was attributable to regulation ...
Ross D. Feldman, Ross D. Feldman, Robert Gros, Robert Gros, Jozef Chorazyczewski, Jozef Chorazyczewski, Jeffrey L. Benovic, Jeffrey L. Benovic, David J. Kelvin, David J. Kelvin, Christopher M. Tan, Christopher M. Tan   +11 more
openaire   +3 more sources

Pathophysiological roles of G-protein-coupled receptor kinases

Cellular Signalling, 2005
G-protein-coupled receptor kinases (GRKs) interact with the agonist-activated form of G-protein-coupled receptors (GPCRs) to effect receptor phosphorylation and to initiate profound impairment of receptor signalling, or desensitization. GPCRs form the largest family of cell surface receptors known and defects in GRK function have the potential ...
Rémy Perdrisot, Jean-Louis Kraimps, Thierry Métayé, Hélène Gibelin   +3 more
openaire   +3 more sources

Peptide inhibitors of G protein-coupled receptor kinases

Biochemical Pharmacology, 2005
G protein-coupled receptor kinases (GRKs) are regulatory enzymes involved in the modulation of seven-transmembrane-helix receptors. In order to develop specific inhibitors for these kinases, we synthesized and investigated peptide inhibitors derived from the sequence of the first intracellular loop of the beta2-adrenergic receptor.
Hans-Georg Ihlenfeldt, Cornelius Krasel, Günther Jung, Martin J. Lohse, Rainer Winstel   +4 more
openaire   +2 more sources

Regulation of G Protein-Coupled Receptors by Receptor Kinases and Arrestins

1995
Publisher Summary This chapter discusses the regulation of G protein-coupled receptors by receptor kinases and arrestins. Signal transduction through seven-transmembrane domain or serpentine receptors, which is mediated by guanine nucleotide-binding (G) proteins, accounts for a significant fraction of all signaling in the body.
Jeffrey L. Benovic, Rachel Sterne-Marr
openaire   +3 more sources

Tyrosine Kinase Receptor Transactivation Associated to G Protein- Coupled Receptors

Current Drug Targets, 2010
G protein-coupled receptors (GPCRs) comprise a large family of membrane receptors involved in signal transduction. These receptors are linked to a variety of physiological and biological processes such as regulation of neurotransmission, growth, cell differentiation and oncogenesis among others.
Pedro Gascón, Susana García-Recio, Vanessa Almendro   +2 more
openaire   +3 more sources

G-protein coupled receptor kinases and their inhibitors

Expert Opinion on Therapeutic Patents, 2000
G-protein coupled receptors (GPCRs) are regulated by several processes. One is the phosphorylation by G-protein coupled receptor kinases (GRKs) linked to processes like receptor desensitisation, internalisation and downregulation. GRKs also seem to be involved in various processes such as opioid addiction and cardiovascular diseases.
openaire   +2 more sources

Therapeutic potential of G-protein coupled receptor kinases in the heart

Expert Opinion on Investigational Drugs, 1999
The actions of G-protein coupled receptor kinases (GRKs) critically regulate beta-adrenergic receptor (betaAR) signalling. In the cardiovascular system, the betaAR signalling pathway controls important responses of the heart such as the ability to contract (inotropy), the ability to contract faster (chronotropy) and the ability to relax (lusotropy ...
G. Iaccarino, W. J. Koch
openaire   +5 more sources

Endocytosis of G protein-coupled receptors: roles of G protein-coupled receptor kinases and ß-arrestin proteins

Progress in Neurobiology, 2002
Sequestration of G protein-coupled receptors from the cell surface is a commonly observed phenomenon following agonist-stimulation. This process is now believed to be important for receptor resensitization as well as for signal transduction. Over the years, numerous studies have aimed at understanding the molecular mechanisms underlying internalization.
Robert J. Lefkowitz, Stéphane A. Laporte, Audrey Claing, Marc G. Caron   +3 more
openaire   +3 more sources