Results 1 to 10 of about 396,098 (353)
Historical Perspective of the G Protein-Coupled Receptor Kinase Family [PDF]
Agonist activation of G protein-coupled receptors promotes sequential interaction of the receptor with heterotrimeric G proteins, G protein-coupled receptor kinases (GRKs), and arrestins. GRKs play a central role in mediating the switch from G protein to
Jeffrey L. Benovic
doaj +5 more sources
Inhibition of thrombin receptor signaling by a G-protein coupled receptor kinase. Functional specificity among G-protein coupled receptor kinases. [PDF]
The thrombin receptor, a member of the seven membrane-spanning superfamily of G-protein coupled receptors, is activated by an irreversible proteolytic mechanism, but signaling by activated thrombin receptors shuts off soon after receptor activation. This shut-off mechanism is thought to be required for concentration-dependent responses to thrombin and ...
Kenji Ishii+6 more
openalex +3 more sources
G protein-coupled receptor kinase 2 promotes cardiac hypertrophy. [PDF]
The increase in protein activity and upregulation of G-protein coupled receptor kinase 2 (GRK2) is a hallmark of cardiac stress and heart failure. Inhibition of GRK2 improved cardiac function and survival and diminished cardiac remodeling in various ...
Philipp Schlegel+12 more
doaj +2 more sources
G‐protein coupled receptor kinases as modulators of G‐protein signalling
G‐protein coupled receptors (GPCRs) comprise one of the largest classes of signalling molecules. A wide diversity of activating ligands induce the active conformation of GPCRs and lead to signalling via heterotrimeric G‐proteins and downstream effectors.
Moritz Bünemann, Marie Thérèse Hosey
openalex +5 more sources
Insulin signaling inhibits the 5-HT2C receptor in choroid plexus via MAP kinase [PDF]
Background G protein-coupled receptors (GPCRs) interact with heterotrimeric GTP-binding proteins (G proteins) to modulate acute changes in intracellular messenger levels and ion channel activity.
Guan Kunliang+7 more
doaj +5 more sources
The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)
G protein-coupled receptors (GPCRs), which regulate a vast number of eukaryotic processes, are desensitized by various mechanisms but, most importantly, by the GPCR kinases (GRKs).
M. Claire Cato+6 more
doaj +1 more source
Targeting G protein–coupled receptor kinases to G protein–coupled receptors
G protein-coupled receptors (GPCRs) interact with three protein families following agonist binding: heterotrimeric G proteins, G protein-coupled receptor kinases (GRKs) and arrestins. GRK-mediated phosphorylation of GPCRs promotes arrestin binding to uncouple the receptor from G protein, a process called desensitization, and for many GPCRs, arrestin ...
Jeffrey L. Benovic, Sarah M. Sulon
openaire +4 more sources
G PROTEIN–COUPLED RECEPTOR KINASES [PDF]
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.
Robert J. Lefkowitz+2 more
openaire +3 more sources
G-protein-coupled receptor kinases
beta-Adrenergic receptors are prototypes of the many G-protein-coupled receptors. Activation and inactivation of these receptors are regulated by multiple mechanisms which can affect either their function or their expression. The most obvious changes of such receptor systems are induced by activation of the receptors themselves by their respective ...
Federico Mayor+3 more
openaire +4 more sources
G-Protein-Coupled Receptor Kinases in Hypertension [PDF]
[No abstract available]
CARNEVALE, DANIELA, LEMBO, Giuseppe
openaire +4 more sources