• Nicotinic receptors get their name from nicotine which does not stimulate the muscarinic acetylcholine receptors but selectively binds to the nicotinic receptors instead. (wikipedia.org)
  • The muscarinic acetylcholine receptor likewise gets its name from a chemical that selectively attaches to that receptor - muscarine. (wikipedia.org)
  • Acetylcholine itself binds to both muscarinic and nicotinic acetylcholine receptors. (wikipedia.org)
  • Slack, B.E. and Blusztajn, J.K. (2008) Differential regulation of mTOR-dependent S6 phosphorylation by muscarinic acetylcholine receptor subtypes. (bu.edu)
  • Positive allosteric modulators (PAMs) of the M1 muscarinic acetylcholine receptor (M1 mAChR) are a promising strategy for the treatment of the cognitive deficits associated with diseases including Alzheimer's and schizophrenia. (worktribe.com)
  • At the neuromuscular junction, the acetylcholine receptor (AChR) is specifically clustered in the postsynaptic membrane via interactions with rapsyn and other scaffolding proteins. (jneurosci.org)
  • The sequence contains a conserved tyrosine (Y390) whose phosphorylation is induced by agrin and whose mutation abolished clustering of β loop chimeras and their ability to inhibit agrin-induced clustering of the endogenous AChR. (jneurosci.org)
  • Phosphorylation of the AChR β subunit is correlated with increased rapsyn/AChR binding, suggesting that the effect of βY390 phosphorylation on clustering is mediated by rapsyn. (jneurosci.org)
  • Indeed, we found that rapsyn associated with CD4-β loop chimeras in a phosphorylation-dependent manner, and that agrin increased the ratio of rapsyn binding to wild type AChR but not to AChR-β 3F/3F , which lacks β loop tyrosine phosphorylation sites. (jneurosci.org)
  • Together, these findings suggest that agrin-induced phosphorylation of the β subunit motif increases the stoichiometry of rapsyn binding to the AChR, thereby helping to stably cluster the receptor and anchor it at high density in the postsynaptic membrane. (jneurosci.org)
  • Indeed, we have shown previously that mutation of a tyrosine phosphorylation site in the long cytoplasmic loop of the β subunit impairs agrin-induced cytoskeletal anchoring and aggregation of mutant AChR in muscle cells ( Borges and Ferns, 2001 ). (jneurosci.org)
  • Blockade of L-CaChs in muscle cultures inhibited agrin-induced AChR aggregation but not tyrosine phosphorylation of MuSK or AChR beta subunits. (nih.gov)
  • Tyrosine phosphorylation has been implicated as a required early step in AChR aggregation. (thermofisher.com)
  • IgG1-3 MuSK Antibodies Inhibit AChR Cluster Formation, Restored by SHP2 Inhibitor, Despite Normal MuSK, DOK7, or AChR Subunit Phosphorylation. (ox.ac.uk)
  • BACKGROUND AND OBJECTIVES: Up to 50% of patients with myasthenia gravis (MG) without acetylcholine receptor antibodies (AChR-Abs) have antibodies to muscle-specific kinase (MuSK). (ox.ac.uk)
  • RESULTS: IgG1-3 MuSK-Abs impaired AChR clustering without inhibiting agrin-induced MuSK phosphorylation. (ox.ac.uk)
  • Adenosine receptors (ARs) control the cAMP/PKA cascade and cause the functional modulation of neuronal acetylcholine receptor (AChR) through its phosphorylation. (units.it)
  • It is a precursor of membrane phospholipids (e.g., phosphatidylcholine (PC)), the neurotransmitter acetylcholine, and via betaine, the methyl group donor S -adenosylmethionine. (mdpi.com)
  • Acetylcholinesterase (AChE, EC 3.1.1.7) and butyrylcholinesterase (BChE, EC 3.1.1.8) are serine esterases that both hydrolyze the neurotransmitter acetylcholine (ACh) to moderate the cholinergic system (CNS). (cdc.gov)
  • Publications] Y. Watanabe: 'Effect of phosphorylation of inhibitory GTP-binding protein by cyclic AMP-dependent protein kinase on its ADP-ribosylation by pertussis toxin, islet-activating protein. (nii.ac.jp)
  • In this study, we provide multiple lines of evidence showing that the post-translational phosphorylation of MSY3 by Akt kinase modulates the MSY3 repression of myogenin. (biomedcentral.com)
  • MuSK, Downstream of Kinase 7 (DOK7), and βAChR were immunoprecipitated and their phosphorylation levels identified by immunoblotting. (ox.ac.uk)
  • To conclude, the mouse pulmonary endothelial β2-AR is coupled to a Gi/o-Src kinase-PI3K/Akt pathway to promote eNOS phosphorylation at Ser1177 leading to a NO-dependent vasorelaxation. (elsevierpure.com)
  • Caveolin-1 exerts a negative control on this response that is abrogated by its phosphorylation at Tyr14, through a Gi/o-Src kinase pathway. (elsevierpure.com)
  • In healthy individuals, nicotine improves memory impairment caused by sleep deprivation by enhancing the phosphorylation of calmodulin‑dependent protein kinase II, an essential regulator of cell proliferation and synaptic plasticity. (spandidos-publications.com)
  • Identified cell signaling networks have defined many potential mechanisms for initiating smooth muscle contraction with or without myosin regulatory light chain (RLC) phosphorylation by myosin light chain kinase (MLCK). (elsevierpure.com)
  • The kinase knockout also markedly reduced RLC phosphorylation and force development with acetylcholine which activates Ca 2+ -sensitizing signaling pathways. (elsevierpure.com)
  • Here, we define a phosphorylation-dependent binding site on the receptor that mediates agrin-induced clustering. (jneurosci.org)
  • Most MuSK antibodies (MuSK-Abs) are IgG4 and inhibit agrin-induced MuSK phosphorylation, leading to impaired clustering of AChRs at the developing or mature neuromuscular junction. (ox.ac.uk)
  • Biomarkers of OP exposure include: (i) decreased cholinesterase activity, (ii) metabolites associated with the hydrolysis of OPs, (iii) OP-protein adducts resulting from phosphorylation-type modification of serine, threonine or tyrosine amino acids on select proteins, (e. g. alkylphosphorylation of cholinesterase (OP-ChE), (iv) in the case of some pesticides, low levels of free OP that exist in biological matrixes for prolonged periods of time. (cdc.gov)
  • During exposure to organophosphates, AChE and BChE can undergo phosphorylation at their respective active site serine, form OP-ChE adducts and subsequently lose enzyme activity. (cdc.gov)
  • In addition to measuring cAMP and cGMP, detection of downstream GPCR signaling events such as activation of Erk1/2, Akt, Src and Stat3 are routinely assayed using phospho-specific antibodies to distinguish phosphorylation of signaling proteins at specific activating or inactivating serine, threonine, and tyrosine residues. (enzolifesciences.com)
  • Organophosphorus (OP's) results in phosphorylation of serine hydroxyl residue on acetylcholine esterase enzyme, which results in the accumulation of acetylcholine. (ijlr.org)
  • Skeletal muscle and myogenic C2C12 cells were used to study the effects of MSY3 phosphorylation in vivo and in vitro on its sub-cellular localization and activity, by blocking the IGF1/PI3K/Akt pathway, by Akt depletion and over-expression, and by mutating potential MSY3 phosphorylation sites. (biomedcentral.com)
  • Furthermore, forced expression of Akt in adult skeletal muscle induced MSY3 phosphorylation and myogenin derepression. (biomedcentral.com)
  • Acetylcholinesterase inhibition causes acetylcholine to accumulate in synapses, producing continuous stimulation of cholinergic fibers throughout the nervous systems. (drugbank.com)
  • Here we show that methyl-CpG-binding protein 2 (MeCP2) phosphorylation at Ser421 (pMeCP2) is essential for the sustained, but not the rapid, antidepressant effects of ketamine and scopolamine in mice. (nature.com)
  • It is possible that M2 and M2 come from dif-ferent modification of receptor proteins, such as phosphorylation, methylation, association with other protein or polymerization. (nii.ac.jp)
  • Consistently, the thoracic ducts in SHRs showed significantly higher phosphorylation of myosin phosphatase targeting protein-1 than WKY rats. (bvsalud.org)
  • Moreover, folic acid caused a reduction in PTEN (phosphatase and tensin homolog deleted on chromosome 10) expression, an increase in the phosphorylation of endothelial nitric oxide synthase (eNOSSer1177) and AktSer473, and an enhanced interaction of heat shock protein 90 (HSP90) with eNOS in both strains, with greater magnitude observed in +db/+db mice. (edu.hk)
  • The destruction of accumulated acetylcholine can then proceed, and neuromuscular junctions will again function normally. (nih.gov)
  • Analysis of the binding of acetylcholine esterase (AChE) to various organophosphonate pesticides. (nih.gov)
  • AChE inhibition induces an acetylcholine build-up, disrupting signals between nerves and muscles, which in high doses leads to asphyxiation. (cdc.gov)
  • Functional studies (for evaluation of vasorelaxant response), Western blotting (for assessment of eNOS and caveolin-1 phosphorylation) and transmission electron microscopy (for visualization of caveolae) were conducted in pulmonary arteries from wild-type or caveolin-1 knockout mice. (elsevierpure.com)
  • The most active compounds of the 4-phenylpyridin-2-one series exhibited comparable binding affinity to the reference compound, 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (BQCA) (1), but markedly improved positive cooperativity with acetylcholine, and retained exquisite selectivity for the M1 mAChR. (worktribe.com)
  • Moreover, the well-established pathway initiated by MuSK through DOK7, resulting in βAChR phosphorylation, was not impaired by MuSK-IgG1-3 and was agrin-independent. (ox.ac.uk)
  • IPAs from castrated rats exhibited decreased phenylephrine- and electrical field stimulation (EFS)-induced contraction and decreased acetylcholine- and EFS-induced vasodilatation. (gla.ac.uk)
  • Conclusions: MLCK and its phosphorylation of RLC are required physiologically for smooth muscle contraction and are essential for normal gastrointestinal motility. (elsevierpure.com)
  • Unlike procaterol, acetylcholine-induced relaxation was unaffected by PTX, methyl-β-cyclodextrin or caveolin-1 gene deletion. (elsevierpure.com)
  • Acetylcholine-induced relaxation in +db/+db mice was less than that observed in +db/+m mice. (edu.hk)
  • Acetylcholine-induced relaxation (with and without folic acid treatment) was sensitive to NG-nitro-l-arginine methyl ester, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, geldanamycin and triciribine. (edu.hk)
  • In addition, acetylcholine-induced relaxation was attenuated by resistin. (edu.hk)
  • In conclusion, folic acid consumption improved blunted acetylcholine-induced relaxation in +db/+db mice. (edu.hk)
  • Because pralidoxime chloride is less effective in relieving depression of the respiratory center, atropine is always required concomitantly to block the effect of accumulated acetylcholine at this site. (nih.gov)
  • Proteomics and phosphorylation site analysis. (nih.gov)
  • Castration decreased nNOS and α-actin expression and increased collagen expression, p38 (Thr180/Tyr182) phosphorylation, as well as caspase 3 cleavage. (gla.ac.uk)
  • Extracellularly, magnesium ions block neurosynaptic transmission by interfering with the release of acetylcholine. (medscape.com)