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Overexpression of the cardiac beta(2)-adrenergic receptor and expression of a beta-adrenergic receptor kinase-1 (betaARK1) inhibitor both increase myocardial contractility but have differential effects on susceptibility to ischemic injury.
(Circ Res, 1999-11-26)
Cardiac beta(2)-adrenergic receptor (beta(2)AR) overexpression is a potential contractile
therapy for heart failure. Cardiac contractility was elevated in mice overexpressing
beta(2)ARs (TG4s) with no adverse effects under ...
Functionally active targeting domain of the beta-adrenergic receptor kinase: an inhibitor of G beta gamma-mediated stimulation of type II adenylyl cyclase.
(Proc Natl Acad Sci U S A, 1994-04-26)
The beta-adrenergic receptor kinase (beta ARK) phosphorylates its membrane-associated
receptor substrates, such as the beta-adrenergic receptor, triggering events leading
to receptor desensitization. beta ARK activity is ...
Monoclonal antibodies reveal receptor specificity among G-protein-coupled receptor kinases.
(Proc Natl Acad Sci U S A, 1996-07-23)
Guanine nucleotide-binding regulatory protein (G protein)-coupled receptor kinases
(GRKs) constitute a family of serine/threonine kinases that play a major role in the
agonist-induced phosphorylation and desensitization ...
Restoration of beta-adrenergic signaling in failing cardiac ventricular myocytes via adenoviral-mediated gene transfer.
(Proc Natl Acad Sci U S A, 1997-10-28)
Cardiovascular gene therapy is a novel approach to the treatment of diseases such
as congestive heart failure (CHF). Gene transfer to the heart would allow for the
replacement of defective or missing cellular proteins that ...
A beta-adrenergic receptor kinase-like enzyme is involved in olfactory signal termination.
(Proc Natl Acad Sci U S A, 1993-02-15)
We have previously shown that second-messenger-dependent kinases (cAMP-dependent kinase,
protein kinase C) in the olfactory system are essential in terminating second-messenger
signaling in response to odorants. We now document ...
Direct evidence that Gi-coupled receptor stimulation of mitogen-activated protein kinase is mediated by G beta gamma activation of p21ras.
(Proc Natl Acad Sci U S A, 1994-12-20)
Stimulation of Gi-coupled receptors leads to the activation of mitogen-activated protein
kinases (MAP kinases). In several cell types, this appears to be dependent on the
activation of p21ras (Ras). Which G-protein subunit(s) ...
The G-protein-coupled receptor kinases beta ARK1 and beta ARK2 are widely distributed at synapses in rat brain.
(J Neurosci, 1992-10)
The beta-adrenergic receptor kinase (beta ARK) phosphorylates the agonist-occupied
beta-adrenergic receptor to promote rapid receptor uncoupling from Gs, thereby attenuating
adenylyl cyclase activity. Beta ARK-mediated receptor ...
Receptor and G betagamma isoform-specific interactions with G protein-coupled receptor kinases.
(Proc Natl Acad Sci U S A, 1997-03-18)
The G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate and desensitize
agonist-occupied GPCRs. GRK2-mediated receptor phosphorylation is preceded by the
agonist-dependent membrane association of this enzyme. ...
Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice.
(Proc Natl Acad Sci U S A, 1998-06-09)
Heart failure is accompanied by severely impaired beta-adrenergic receptor (betaAR)
function, which includes loss of betaAR density and functional uncoupling of remaining
receptors. An important mechanism for the ...
Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice.
(Proc Natl Acad Sci U S A, 1996-09-03)
Transgenic mice were generated with cardiac-specific overexpression of the G protein-coupled
receptor kinase-5 (GRK5), a serine/threonine kinase most abundantly expressed in the
heart compared with other tissues. Animals ...