• Rapid desensitization of neonatal rat liver beta-adrenergic receptors. (jci.org)
  • Budd , David C. et al "Cross Talk Between m3-Muscarinic and β 2 -Adrenergic Receptors at the Level of Receptor Phosphorylation and Desensitization. (aspetjournals.org)
  • Arrestins mediate phosphorylation-dependent desensitization, internalization, and initiation of signaling cascades for the majority of G protein-coupled receptors (GPCRs). (duke.edu)
  • Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. (cusabio.com)
  • Receptor phosphorylation is a key step in the process of desensitization of the beta-adrenergic and other related receptors. (unich.it)
  • Although GABA activates synaptic (αβγ) GABA A receptors with high efficacy, partial agonist activation of αβγ isoforms and GABA activation of the primary extrasynaptic (αβδ) GABA A receptors are limited to low-efficacy activity, characterized by minimal desensitization and brief openings. (jneurosci.org)
  • Activated receptors directly or indirectly regulate cellular biochemical processes (eg, ion conductance, protein phosphorylation, DNA transcription, enzymatic activity). (msdmanuals.com)
  • Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro . (tocris.com)
  • SER-333 and SER-334 in the carboxyl terminus are involved in agonist-dependent phosphorylation desensitization and internalization of the P2Y4 receptor. (wikipedia.org)
  • CT receptor desensitization, β-arrestin recruitment and internalization are regulated by phosphorylation of carboxyl-terminal serine422/serine425 (pS422/pS425-CT). (7tmantibodies.com)
  • The proposed mechanisms of such rapid receptor desensitization include receptor phosphorylation by either cAMP-dependent protein kinase or the specific beta-adrenergic receptor kinase (BARK), leading to functional uncoupling from adenylyl cyclase and sequestration of the receptors away from the cell surface. (jci.org)
  • Agonist-induced receptor phosphorylation is an initial step in opioid receptor desensitization, a molecular mechanism of opiold tolerance and dependence. (wustl.edu)
  • GRK2-mediated receptor phosphorylation is preceded by the agonist-dependent membrane association of this enzyme. (duke.edu)
  • Moreover, D1 receptor-mediated PKA activation also results in the activation of the extracellular signal-regulated kinases 1/2 (Erk1/2) by two mechanisms: src-Shp2-dependent Erk1/2 phosphorylation and DARPP-32-mediated inhibition of protein phosphatase-1. (7tmantibodies.com)
  • Agonist-induced D2 phosphorylation is primarily mediated by GRK2 and GRK3. (7tmantibodies.com)
  • Coexpression of GRK2 strongly enhanced agonist-stimulated phosphorylation of the wild-type DOR (WT), but Δ15 or mutant DOR (T358A/VT361A/S363G) failed to show any detectable phosphorylation under these conditions. (wustl.edu)
  • In the presence of exogenously expressed GRK2, phosphorylation levels of T358D and S363D mutants were approximately half of that of WT, whereas significant phosphorylation of the T358/S363 double-point mutant was not detected. (wustl.edu)
  • Taken together, we have demonstrated that agonist-induced opioid receptor phosphorylation occurs exclusively at two phosphate acceptor sites (T358 and S363) of GRK2 at the DOR carboxyl terminus. (wustl.edu)
  • Then, our findings further indicate that Hcy significantly downregulates the phosphorylation level of calmodulin-dependent protein kinases 2 (CAMK2A) after ICH, which is associated with neurite outgrowth. (bmj.com)
  • The agonist-liganded GPCR is normally at the mercy of phosphorylation by regulatory kinases (GRK1-6, G protein-coupled receptor kinases). (biotechpatents.org)
  • The current study was carried out to identify the site of DOR phosphorylation during agonist stimulation and the kinases catalyzing this reaction. (wustl.edu)
  • In this study we used phosphorylation of the transcription factor cAMP response element-binding protein as a functional readout to identify cells responding to EGF and FGF-2. (beauty104.com.tw)
  • Since agonist-induced beta ARK translocation is considered the first step involved in beta ARK-mediated homologous desensitization, we screened a number of G-protein-coupled receptor agonists for their ability to induce beta ARK translocation. (unich.it)
  • This interaction precludes the recruitment of G protein and network marketing leads to desensitization of G protein-dependent signaling [31] thus. (biotechpatents.org)
  • D1 desensitization, trafficking and signaling are regulated by phosphorylation of carboxyl-terminal threonine354 (pT354-D1), serine372/serine373 (pS372/pS373-D1). (7tmantibodies.com)
  • Our previous research suggested that agonist-induced δ-opioid receptor (DOR) phosphorylation occurs at the receptor carboxyl terminal domain. (wustl.edu)
  • In agreement with such pattern of desensitization, we have detected (by enzymatic and immunological assays) rapid changes in BARK specific activity in different neonatal rat liver subcellular fractions that take place within the same time frame of BAR uncoupling and sequestration. (jci.org)
  • Thus, chronic administration of opioids modifies neuronal MOR function through a variety of mechanisms including receptor phosphorylation, signaling, multimerization, and trafficking, which may underlie tolerance to morphine. (hindawi.com)
  • Our results provide new evidence on the potential role of BAR desensitization mechanisms in vivo and suggest that they are involved in modulating catecholamines actions at the moment of birth. (jci.org)
  • Tonic inhibition of P2X3 receptor activity by BNP/NPR-A/PKG pathways occurs via two distinct mechanisms: P2X3 serine phosphorylation and receptor redistribution to non-raft membrane compartments. (biomedcentral.com)
  • Anantin application caused preferential P2X3 receptor redistribution to the lipid raft compartment and decreased P2X3 serine phosphorylation, two phenomena that were not interdependent. (biomedcentral.com)
  • These results represent the identification of the GRK phosphorylation site on an opioid receptor for the first time and demonstrate that GRK is the prominent kinase responsible for agonist-induced opioid receptor phosphorylation in vivo. (wustl.edu)
  • item [-] A distinct pathway for Erk phosphorylation is activated, and those cells are anergized for IgE, but not fMLP stim %note here: maybe we want to do pErk/ 63 staining with fMLP stim \item [-] while peroxide effect is thought to be secondary to PTPs, neither lyn, nor syk are activated %should we try to look at fyn? (openwetware.org)
  • D2 desensitization, β-arrestin recruitment and signaling are regulated by phosphorylation of third intracellular loop serine317/threonine318 ( pS317/pT318-D2 ). (7tmantibodies.com)
  • We have detected a rapid, transient uncoupling of liver plasma membrane BARs from adenylyl cyclase (corresponding to a desensitization of approximately 45%) within the first minutes of extrauterine life, followed by a transient sequestration of approximately 40% of the BARs away from the plasma membrane. (jci.org)
  • Thus, we investigated changes in P2X3 receptor distribution in the lipid raft membrane compartment, their phosphorylation state, as well as their function with patch clamping. (biomedcentral.com)
  • Delayed onset of P2X3 desensitization was one mechanism for the anantin-induced enhancement of P2X3 activity. (biomedcentral.com)
  • However, the desensitization mechanism is unknown. (geneticsmr.com)
  • Mann A, Keen AC, Mark H, Dasgupta P, Javitch JA, Canals M, Schulz S, Robert Lane J. New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D2 receptor regulation and signaling. (7tmantibodies.com)
  • In this study, we examined whether H1R desensitization contributes to regulating the decay rate of TRPC6 activity upon receptor stimulation. (mdpi.com)
  • Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner. (cusabio.com)
  • In this study, L-selectin was found to be phosphorylated in lymphoblastoid cell lines, and phosphorylation was enhanced by phorbol ester (phorbol 12-myristate 13-acetate (PMA)) treatment. (upenn.edu)
  • Bone desensitization after mechanical loading is essential for bone to adapt to its mechanical environment. (geneticsmr.com)