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Inositol 1,4,5-Trisphosphate ReceptorsInositol 1,4,5-TrisphosphateInositol PhosphatesReceptors, Cytoplasmic and NuclearCalcium ChannelsInositolCalciumCalcium SignalingSugar PhosphatesMacrocyclic CompoundsBoron CompoundsPhosphatidylinositolsType C PhospholipasesThimerosalRyanodine Receptor Calcium Release ChannelCerebellumOxazolesEndoplasmic ReticulumPhosphatidylinositol PhosphatesThapsigarginPhosphoric Monoester HydrolasesChromogranin BKineticsCytosolCarbacholMicrosomesCell LineSecond Messenger SystemsSignal TransductionPhosphotransferases (Alcohol Group Acceptor)Phytic AcidRyanodineProtein IsoformsCell MembraneMolecular Sequence DataTRPC Cation ChannelsAmino Acid SequenceCyclic ADP-RiboseReceptors, Cell SurfaceCOS CellsEstrenesPhosphatidylinositol 4,5-DiphosphateCells, CulturedEgtazic AcidFura-2Protein BindingCalcium Channel AgonistsIon Channel GatingMicroscopy, ConfocalPyrrolidinonesCaffeinePhosphorylationLithiumCell Membrane PermeabilityCalcium-Transporting ATPasesInosine TriphosphateProtein Structure, TertiaryParotid GlandIonomycinBinding SitesChromograninsAdenosine TriphosphateCalmodulinOocytesIntracellular FluidCyclic GMP-Dependent Protein KinasesPhospholipase C betaEliminative Behavior, AnimalChelating AgentsDose-Response Relationship, DrugOscillometryCyclic AMP-Dependent Protein KinasesHeparinTransfectionTime FactorsAdenosineModels, BiologicalPhospholipase C gammaStrontiumReceptors, MuscarinicEnzyme InhibitorsOvumRecombinant ProteinsDiglyceridesPurkinje CellsEnzyme ActivationOrganothiophosphorus CompoundsLigandsPotassium IodideGTP-Binding ProteinsPatch-Clamp TechniquesCattleProtein Kinase CCholinergic AgonistsBlotting, WesternMembrane PotentialsFertilizationCercopithecus aethiopsPancreasCyclic AMP
PhosphatesIntracellular storesTriphosphateRyanodine receptorsPhosphatidylinositolInsPAntagonistsPhospholipaseMembraneProtein-coupled receptorsInsP3RDiacylglycerolSynapticSerotoninCytoplasmicNeuronsInactivationMicroMPharmacologyCyclicMoleculesKinaseP2X3GlutamatePhospholipidsLife SciencesArachidonic acidGPCRDopamineGeneSuperfamilyAgonistP400High-affinityInhibitionInducesPostsynapticTypeChannelsCaMKIICompounds
Phosphates1
Intracellular stores4
  • The release of Ca 2+ from intracellular stores through the inositol 1,4,5-trisphosphate receptor (InsP 3 R) occurs in both excitable and nonexcitable cells. (jneurosci.org)
  • DAG activates protein kinase C, and InsP3 mobilizes calcium from intracellular stores via the InsP3 receptor. (nih.gov)
  • A broad range of stimuli elevate the cytosolic Ca2ï¼ concentration by promoting a pathway mediated by inositol 1,4,5 trisphosphate (IP3) which causes Ca2ï¼ release from intracellular stores. (bvsalud.org)
  • Adenophostin A, the most potent known agonist of inositol 1,4, 5-trisphosphate (InsP(3)) receptors, stimulated (45)Ca(2+) release from the intracellular stores of permeabilized hepatocytes. (cam.ac.uk)
Triphosphate2
  • Inositol triphosphate receptor represents a dominant second messenger leading to the release of Ca2+ from intracellular store sites. (wikipedia.org)
  • It is subsequently used to reproduce observations on the extent of desensitization and sequestration of the P(2)Y(2) receptor following its activation by uridine triphosphate (UTP). (physiomeproject.org)
Ryanodine receptors2
Phosphatidylinositol6
  • Active PLC hydrolyzes phosphatidylinositol bisphosphate (PIP2) into the two second messengers inositol 1,4,5-trisphosphate (InsP3) and diacyl glycerol (DAG). (nih.gov)
  • ABSTRACT: A mathematical account is given of the processes governing the time courses of calcium ions (Ca2+), inositol 1,4,5-trisphosphate (IP(3)) and phosphatidylinositol 4,5-bisphosphate (PIP(2)) in single cells following the application of external agonist to metabotropic receptors. (physiomeproject.org)
  • PI(16:1(9Z)/18:0) is a phosphatidylinositol. (hmdb.ca)
  • The inositol group that is part of every phosphatidylinositol lipid is covalently linked to the phosphate group that acts as a bridge to the lipid tail. (hmdb.ca)
  • Phosphatidylinositol can be phosphorylated by a number of different kinases that place the phosphate moiety on positions 4 and 5 of the inositol ring, although position 3 can also be phosphorylated by a specific kinase. (hmdb.ca)
  • Seven different isomers are known, but the most important in both quantitative and biological terms are phosphatidylinositol 4-phosphate and phosphatidylinositol 4,5-bisphosphate. (hmdb.ca)
InsP7
  • Our goal is to understand the contribution of the intracellular Ca 2+ release channel, the InsP 3 receptor (InsP 3 R), in the development and function of neural circuitry. (jneurosci.org)
  • The inositol 1,4,5-trisphosphate (InsP 3 ) receptor acts as an InsP 3 -gated Ca 2+ release channel in a variety of cell types. (elsevierpure.com)
  • Type 1 InsP 3 receptor (IP 3 R1) is the major neuronal member of the IP 3 R family in the central nervous system, predominantly enriched in cerebellar Purkinje cells but also concentrated in neurons in the hippocampal CA1 region, caudate-putamen, and cerebral cortex. (elsevierpure.com)
  • The syntheses of four D-myo-inositol 1,4,5-trisphosphate (InsP(3)) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. (ox.ac.uk)
  • The Ca(2+) release evoked by both agonists peaked at the same maximal rate after about 375 ms and the activity of the receptors then decayed to a stable, partially (60%) inactivated state with a half-time (t(1/2)) of 318+/-29 ms for adenophostin A and 321+/-22 ms for InsP(3). (cam.ac.uk)
  • Dissociation rates were measured by recording rates of InsP(3)-receptor channel closure after rapid removal of agonist. (cam.ac.uk)
  • The rate of adenophostin A dissociation (t(1/2), 840+/-195 ms) was only 2-fold slower than that of InsP(3) (t(1/2), 436+/-48 ms). We conclude that slow dissociation of adenophostin A from InsP(3) receptors does not underlie either its high-affinity binding or the reported differences in the Ca(2+) signals evoked by InsP(3) and adenophostin A in intact cells. (cam.ac.uk)
Antagonists2
  • Development of inositol-based antagonists for the D-myo-inositol 1,4,5-trisphosphate receptor. (ox.ac.uk)
  • At the extreme, functionally selective ligands may be both agonists and antagonists at different functions mediated by the same receptor. (aspetjournals.org)
Phospholipase3
  • Phospholipase C (PLC) is the focal point for two major signal transduction pathways: one initiated by G protein-coupled receptors and the other by tyrosine kinase receptors. (nih.gov)
  • The translocation was blocked by inhibiting the phospholipase C/inositol 1,4,5-trisphosphate receptor/Ca 2+ signaling. (aspetjournals.org)
  • Group I metabotropic glutamate receptors (mGluRs) are coupled via Galphaq/11 to the activation of phospholipase Cbeta, which hydrolyzes membrane phospholipids to form inositol 1,4,5 trisphosphate and diacylglycerol. (uwo.ca)
Membrane5
  • Inositol trisphosphate receptor (InsP3R) is a membrane glycoprotein complex acting as a Ca2+ channel activated by inositol trisphosphate (InsP3). (wikipedia.org)
  • The theory predicts the dependence on agonist concentration of the change in the number of receptors in the membrane as well as the time course of disappearance of receptors from the plasmalemma, upon exposure to agonist. (physiomeproject.org)
  • The CXCR1 receptor for IL-8 was expressed only on the apical membrane of Caco-2 BBE cells and differentiated epithelial cells in the human small intestine and colon. (biomedcentral.com)
  • The effect of inositol 1,4,5-trisphosphate and inositol 1,4,5-trisphosphorothioate on calcium release and membrane skeleton organization in the human red blood cell. (ox.ac.uk)
  • Ins (1,4,5)P3 at concentrations between 0.4-5.0 microM releases Ca2+ from RBC plasma membrane with an EC50 of 0.55 microM. (ox.ac.uk)
Protein-coupled receptors1
  • CaSR is a member of sub-family C in the superfamily of G protein-coupled receptors (GPCRs). (biomedcentral.com)
InsP3R1
  • In the mouse, there are three InsP3R genes, and type 1 InsP3R mutants display ataxia and epileptic seizures (Matsumoto et al. (nih.gov)
Diacylglycerol2
  • The synthesis of PI involves CDP-activated 1,2-diacylglycerol condensation with myo-inositol. (hmdb.ca)
  • This signalling system liberates two key second messengers, namely, IP 3 (inositol 1,4,5-trisphosphate) and DAG (diacylglycerol). (shawprize.org)
Synaptic2
  • Concomitant with the synaptic accumulation of α-CaMKII in response to D 4 receptor activation, a D 4 -induced increase in the CaMKII phosphorylation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor glutamate receptor 1 (GluR1) subunits and the amplitude of AMPA receptor-mediated excitatory postsynaptic currents was also observed. (aspetjournals.org)
  • Thus, our results show that D 4 receptor activation induces the synaptic translocation of CaMKII through a mechanism involving Ca 2+ /calmodulin and F-actin, which facilitates the regulation of synaptic targets of CaMKII, such as AMPA receptors. (aspetjournals.org)
Serotonin2
  • Further, voltage-gated Ca2+ channels are activated and release vesicular serotonin (5-HT), norepinephrine (NE) and gamma-aminobutyric acid (GABA). (genome.jp)
  • The dense granules contain proaggregatory factors such as ADP, calcium, and 5-hydroxytryptamine (serotonin). (medscape.com)
Cytoplasmic2
  • Recently, studies performed on PrCa samples have shown that calcium-sensing receptor regulates cytoplasmic calcium levels in relation to extracellular calcium concentrations. (biomedcentral.com)
  • One factor contributing to these contradictory theories is the lack of comprehensive understanding of the molecular mechanisms of calcium intake, serum homeostasis, and cytoplasmic function (Fig. 1 ). (biomedcentral.com)
Neurons4
  • A puzzling case is presented by cerebellar granule cells (GrC), the most numerous neurons of the brain 4 . (nature.com)
  • We found that activation of D 4 receptors, but not D 2 receptors, induced a rapid translocation of α-CaMKII from cytosol to postsynaptic sites in cultured PFC neurons. (aspetjournals.org)
  • ATP-gated P2X3 receptors of sensory ganglion neurons are important transducers of painful stimuli and are modulated by extracellular algogenic substances, via changes in the receptor phosphorylation state. (shengsci.com)
  • Many structures and processes are involved in the development of a seizure, including neurons, ion channels, receptors, glia, and inhibitory and excitatory synapses. (medscape.com)
Inactivation1
  • Rapid activation and partial inactivation of inositol trisphosphate receptors by adenophostin A. (cam.ac.uk)
MicroM2
  • There was more than a 10-fold difference between the ED50 for PGE1 at cyclic AMP formation (70 nM) and its ED50 values at IP accumulation (1 microM), cyclic GMP formation (2 microM), and [Ca2+]i increase (5 microM). (shengsci.com)
  • 1 microM L-Ins(1,4,5)P3 released no more Ca2+ than the control. (ox.ac.uk)
Pharmacology2
  • The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century, yet recent data have revealed that many ligands can differentially activate signaling pathways mediated via a single G protein-coupled receptor in a manner that challenges the traditional definition of intrinsic efficacy. (aspetjournals.org)
  • Developmental Pharmacology and Therapeutics (1991) 16 (1): 22-28. (karger.com)
Cyclic4
  • His interests and those of his research groups have included exploring the mechanisms of ion permeation and selectivity in ion channels, the relationship between the molecular structure and the physiological function of channels, such as those of the inhibitory neurotransmitter receptor glycine channel and the olfactory cyclic nucleotide-gated channel, and investigating the factors that determine their ion permeation, selectivity and conductance. (edu.au)
  • A protein kinase C activator, 4 beta-phorbol 12 beta-myristate 13 alpha-acetate, had opposite effects on PGE1-mediated IP release and cyclic GMP formation (inhibitory) and cyclic AMP formation (stimulatory). (shengsci.com)
  • These data suggest that there may be subtypes of the PGE1 receptor in this clone: a high-affinity receptor mediating cyclic AMP formation, and a low-affinity receptor mediating IP accumulation, cyclic GMP formation, and intracellular calcium mobilization. (shengsci.com)
  • Cyclic compounds with a ring size of approximately 1-4 dozen atoms. (lookformedical.com)
Molecules2
  • The reason is because many immune-related receptors and molecules are extensively produced by these cells, not only during disease but also during physiological processes ( 3 , 9 ). (frontiersin.org)
  • Cellular communication occurs through chemical signals such as hormones, neurotransmitters and nitric oxide, which act via specific receptors or receptive molecules and are linked to diverse intracellular and extracellular signalling pathways. (shawprize.org)
Kinase3
  • One of the important targets of dopamine D 4 receptors in prefrontal cortex (PFC) is the multifunctional Ca 2+ /calmodulindependent protein kinase II (CaMKII). (aspetjournals.org)
  • Calcium/calmodulin-dependent serine protein kinase (CASK) is a new intracellular modulator of P2X3 receptors. (shengsci.com)
  • We show here, that the proline-rich tyrosine kinase 2 (Pyk2) interacts with both mGluR1 and mGluR5 and is precipitated with both receptors from rat brain. (uwo.ca)
P2X31
  • This produces a depolarization that may allow CALMH1 channels to open and release ATP, which serves as a neurotransmitter to activate closely associated nerve afferents expressing P2X2, P2X3 receptors and adjacent type III cells expressing P2Y4 receptors. (genome.jp)
Glutamate3
  • Furthermore, both robust phosphorylation of Homer3 and its dissociation from metabotropic glutamate receptor 1α (mGluR1α) were triggered by depolarization in primary cultured Purkinje cells, and these events were inhibited by CaMKII inhibitor. (jneurosci.org)
  • Pyk2 uncouples metabotropic glutamate receptor G protein signaling but" by Alexander A. Nicodemo, Macarena Pampillo et al. (uwo.ca)
  • Pyk2 uncouples metabotropic glutamate receptor G protein signaling but facilitates ERK1/2 activation. (uwo.ca)
Phospholipids1
  • Phosphatidylinositols are acidic (anionic) phospholipids that consist of a phosphatidic acid backbone, linked via the phosphate group to inositol (hexahydroxycyclohexane). (hmdb.ca)
Life Sciences1
Arachidonic acid1
  • PIs contain almost exclusively stearic acid at carbon 1 and arachidonic acid at carbon 2. (hmdb.ca)
GPCR1
  • IL-8 can signal through two receptors, CXCR1 and CXCR2 both of which are members of the G-protein-coupled receptor (GPCR) family [ 2 ]. (biomedcentral.com)
Dopamine1
  • Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4′-halophenyl)nortropanes: Candidate Radioligands for In Vivo Imaging of the Brain Dopamine Transporter with Positron Emission Tomography. (acs.org)
Gene1
  • Expression of each cluster's gene signatures was validated using multiplex fluorescence in situ hybridization (FISH) co-stained with piwi-1 and largely confirmed the cell clusters revealed by scRNA-seq. (stowers.org)
Superfamily1
  • Tumor necrosis factor receptor-associated factor 6 (TRAF6) is a member of the TRAF family and an important multifunctional intracellular adaptin of the tumor necrosis factor superfamily and toll/IL-1 receptor (TIR) superfamily. (shengsci.com)
Agonist3
  • In addition, the extent of activation and desensitization of the receptor, using the calcium transients in cells initiated by exposure to agonist, is also predicted. (physiomeproject.org)
  • Results of the modelling also reveal the importance of receptor recycling and PIP(2) resupply for maintaining Ca2+ and IP(3) levels during sustained application of agonist. (physiomeproject.org)
  • Pyk2 overexpression in HEK293 results in attenuated basal and agonist-stimulated inositol phosphate formation in mGluR1 expressing cells and involves a mechanism whereby Pyk2 displaces Galphaq/11 from the receptor. (uwo.ca)
P4001
  • The large size of this open reading frame indicated a molecular weight similar to the protein purified biochemically, and soon thereafter it was confirmed that the protein p400 was in fact the inositol trisphosphate receptor. (wikipedia.org)
High-affinity1
  • Trifluoromethoxyl Substituted Phenylethylene Diamines as High Affinity σ Receptor Ligands with Potent Anti-Cocaine Actions. (acs.org)
Inhibition1
  • BMP receptor blockade overcomes extrinsic inhibition of remyelination and restores neurovascular homeostasis. (neurotree.org)
Induces2
  • Transcriptome analyses revealed that Caco-2 BBE cells respond to stimulation with IL-8 supporting the hypothesis that IL-8 induces G protein-coupled receptor signalling. (biomedcentral.com)
  • These results show that IL-8 induces autocrine signalling via an apical CXCR1 in Caco-2 BBE intestinal epithelial cells and that this receptor is also expressed on the apical surface of differentiated human intestinal epithelial cells in vivo , suggesting an autocrine function for IL-8 secreted in the lumen. (biomedcentral.com)
Postsynaptic1
  • Activated CaMKII (Thr 286 phospho-CaMKII) was also redistributed to postsynaptic sites after D 4 receptor stimulation. (aspetjournals.org)
Type4
  • 14 -3-3 proteins and spinocerebellar ataxia type 1: from molecular interaction to human neuropathology. (nih.gov)
  • [ 1 ] These criteria are based on the presence or absence of cancer, the presence of well-characterized paraneoplastic (onconeural) antibodies, and the type of clinical syndrome. (medscape.com)
  • Type II taste cells also secrete acetylcholine (ACh) that appears to stimulate muscarinic receptors, specifically M3, on the same or neighboring Type II cells. (genome.jp)
  • In type III cells, sour taste is initiated when protons enter through apically located proton-selective ion channels: polycystic kidney disease 2-like 1 protein (PKD2L1) and polycystic kidney disease 1-like 3 protein (PKD1L3) channels. (genome.jp)
Channels3
CaMKII3
  • In the present study, we investigated the effect of D 4 receptor activation on subcellular localization of CaMKII. (aspetjournals.org)
  • Point mutation of the calmodulin binding site (Ala 302 ), but not the autophosphorylation site (Thr 286 ), of α-CaMKII prevented the D 4 -induced CaMKII translocation. (aspetjournals.org)
  • Moreover, D 4 receptors failed to induce CaMKII translocation in the presence of an actin stabilizer, and D 4 activation reduced the binding of CaMKII to F-actin. (aspetjournals.org)
Compounds1
  • The shape changes are stereospecific for the D-enantiomer, since L-Ins(1,4,5)P3 and other compounds had no effect. (ox.ac.uk)