• Role of hormone-sensitive low Km cAMP phosphodiesterase in regulation of cAMP-dependent protein kinase and lipolysis in rat adipocytes. (aspetjournals.org)
  • cAMP exerts its effects by activating the cAMP-dependent protein kinase (AMPK), which transduces the signal through phosphorylation of different target proteins. (thermofisher.com)
  • The activated receptor in turn couples to Gq/11 and Gi/o and thus activates phospholipase C and increases the cytosolic Ca2+ concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C. Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases. (wikipedia.org)
  • Clonidine activates another type of adrenergic receptor, designated α 2 . (pharmacology2000.com)
  • Whereas the above two example drugs show α-adrenergic receptor selectivity (α 1 vs. α 2 ), oxymetazoline activates both α 1 and α 2 adrenergic receptors. (pharmacology2000.com)
  • The binding of LPA to an LPAR allosterically activates the heterotrimeric G protein by exchanging GDP for GTP at the G protein's alpha subunit. (smpdb.ca)
  • The main process of this pathway: the growth factor activates the receptor by binding to the tyrosine kinase receptor, and the activated tyrosine kinase receptor activates the Ras protein, then the Ras protein phosphorylates the Raf, and the activated Raf phosphorylates the downstream MEK. (cusabio.com)
  • After a ligand binds to the GPCR, it activates a heterotrimeric G-protein, which is composed of three subunits: a guanine nucleotide binding α-subunit, and a βγ-heterodimer (98). (pancreapedia.org)
  • Concomitant activation of the insulin-like growth factor-1 receptor, Akt, and extracellular signal-regulated protein kinase 1 and 2 as well as increased phosphorylation of Bad also were unique to the hippocampus of APP Sw mice. (jneurosci.org)
  • In T cells, productive antigen stimulation triggers the activation of MAPK including extracellular signal-regulated kinase, p38 and JNK.33 The JNK is activated through the dual phosphorylation of its Thr and Tyr residues by mitogen-activated kinase kinase Pembrolizumab 4 (MKK4) and MKK7. (syksignaling.com)
  • NGF is a neurotrophic factor critical for the survival and maintenance of sympathetic and sensory neurons, and it binds to the high-affinity tyrosine kinase receptor, TrkA, leading to its phosphorylation and the subsequent activation of PI3K/Akt/GSK3β pathways. (biomedcentral.com)
  • It is known to act through protein phosphorylation via PRKA and through the activation of guanine nucleotide exchange factors like EPAC. (plos.org)
  • MAPK is a mitogen-activated protein kinase, a class of protein kinases with dual phosphorylation of serine and tyrosine in the cytosol. (cusabio.com)
  • Agonist stimulation of GABA B receptors enhances the phosphorylation of Akt (Thr-308) and enhances the phosphorylation of GSK-3α (Ser-21)/β (Ser-9) in both HEK-293T cells expressing GABA B receptors and rat hippocampal slices. (biomedcentral.com)
  • The expression of transthyretin, a protein shown to sequester Aβ and prevent amyloid fibril formation in vitro , and several genes in the insulin-signaling pathway, e.g., insulin-like growth factor-2, were increased selectively in the hippocampus of APP Sw mice. (jneurosci.org)
  • Exploring the role of insulin-like growth factor binding protein-1 in identifying idiopathic multicentric Castleman's disease types: Implications for the mTOR signaling pathway. (harvard.edu)
  • The p38 signaling pathway regulates the differentiation direction of stem cells, which may be related to the regulation of the stability of p53 protein [3] [4] . (cusabio.com)
  • There must be 5 molecules of cobra toxin (red) to block the receptor (blue) as each molecule binds with an individual alpha chain on the acetylcholine receptor. (proteopedia.org)
  • It binds the GLP-1 receptor in the pancreas and displays vari. (targetmol.com)
  • Lysophosphatidic acid (LPA) is a water-soluble phospholipid derivative and a potent signalling molecule that binds to six known lysophosphatidic acid receptors (LPARs), named LPA1-LPA6. (smpdb.ca)
  • IP3 diffuses through the cytoplasm to the ER and binds to the inositol 1,4,5-trisphosphate (Ins3P) receptor, releasing calcium from the endoplasmic reticulum into the cytoplasm. (smpdb.ca)
  • In the cytosol, the signal molecule binds to the heme-binding domain of the soluble cyclase. (pancreapedia.org)
  • Desogestrel binds intracellular progesterone receptors in progesterone responsive tissue and the resultant complex interacts with DNA and results in either gene transcription or gene repression. (medindex.am)
  • Pimecrolimus binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. (medindex.am)
  • The α-adrenergic receptor is described by seven α-helical transmembrane (TM) domains which form a 'crevice' for ligand binding. (pharmacology2000.com)
  • The receptor is a transmembrane pentameric glycoprotein. (proteopedia.org)
  • What is the most common activity found intrinsic to transmembrane receptors? (flashcardmachine.com)
  • Sperm intracellular cAMP levels depend on the activity of adenylyl cyclases, mostly SACY, though transmembrane-containing adenylyl cyclases are also present, and on the activity of cyclic nucleotide phosphodiesterases (PDE) whose role is to degrade cAMP into 5'-AMP. (plos.org)
  • One mechanism is the binding of an extracellular ligand to a transmembrane G-protein-coupled receptor (GPCR). (pancreapedia.org)
  • The receptor protein has seven transmembrane α-helices connected by alternating cytosolic and extracellular loops. (pancreapedia.org)
  • Oxymetazoline is an example of a non-selective α-adrenergic receptor agonist. (pharmacology2000.com)
  • Isoproterenol (Isuprel, Isoprenaline) is a classical nonselective β-adrenergic agonist, with prominent actions at β 1 and β 2 receptors. (pharmacology2000.com)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • Oxyntomodulin acetate, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist[1]. (targetmol.com)
  • Glucagon-like peptide 1 (1-37), human acetate is a highly potent the GLP-1 receptor agonist. (targetmol.com)
  • Semaglutide TFA is a agonist of glucagon-like peptide-1 (GLP-1) receptor,with a potential for type 2 diabetes treatment. (targetmol.com)
  • Lixisenatide acetate is a receptor agonist similar to glucagon-like peptide-1 (glp-1) for the treatment of type 2 diabetes mellitus (T2DM). (targetmol.com)
  • Exendin-4 is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). (targetmol.com)
  • Semaglutide is a glucagon-like peptide 1 receptor (GLP-1R) agonist(EC50 of 6.2 pM in a reporter assay using BHK cells expressing the human receptor). (targetmol.com)
  • PF-06882961 Tris is an orally bioavailable glucagon-like peptide-1 receptor (GLP-1R) agonist. (targetmol.com)
  • PF-06882961 is an orally bioavailable glucagon-like peptide-1 receptor (GLP-1R) agonist. (targetmol.com)
  • The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (lookformedical.com)
  • As well, the GABA B receptor agonist, baclofen has been reported to have some efficacy in SCZ patients [ 4 ]. (biomedcentral.com)
  • The α-2 adrenergic receptor (A2AR) inhibits insulin or glucagons release. (proteopedia.org)
  • The Gαi/o subunit inhibits the enzyme adenylyl cyclase (AC) which catalyzes the production of the important secondary messenger 3',5'-cyclic AMP (cAMP) from adenosine triphosphate (ATP). (smpdb.ca)
  • Here we report that activation of GABA B receptors significantly inhibits Akt/GSK-3 signaling in a β-arrestin-dependent pathway. (biomedcentral.com)
  • The AT1 and AT2 receptors share a sequence identity of ~30%, but have a similar affinity for angiotensin II, which is their main ligand. (wikipedia.org)
  • It works as a postsynaptic neurotoxin binding to the receptor as an extracellular ligand by interacting with OH group leaving the acetylcholine channel open which releases ions used in creating an action potential. (proteopedia.org)
  • How is a receptor-ligand binding curve determined? (flashcardmachine.com)
  • Describe the three lines on a receptor-ligand binding curve? (flashcardmachine.com)
  • These receptors function as ligand-dependent transcription factors [2] - [4] , acting either through the transcriptional regulation of genes (genomic pathway) or through membrane and cytoplasmic signaling cascades (non-genomic pathway). (scirp.org)
  • Expression data further support diverse central and peripheral roles, including volume and fluid control, of this ligand/receptor pair. (bvsalud.org)
  • Taking advantage of the diverse γδ TCR repertoire or other ligand-receptor interactions, γδ T cells can recognize a broad spectrum of tumor-associated antigens (TAAs) in a major histocompatibility complex (MHC)-independent manner, thereby activating downstream pleiotropic effects. (explorationpub.com)
  • The ligand-binding site is in the extracellular domain and the cytosolic domain has a heterotrimeric G protein-binding site (127). (pancreapedia.org)
  • Phenylephrine and methoxamine are examples of drugs that selectively activate α 1 -adrenergic receptors (adrenomimetic). (pharmacology2000.com)
  • Dobutamine is an example of a drug that selectively stimulates the heart via β 1 receptors, although dobutamine also has activity at α adrenergic receptors as well. (pharmacology2000.com)
  • that is, of the 182 amino acids defining the TM domains of the human α 2A -adrenergic receptors, about 40% are identical with the human β 2 -adrenergic receptors. (pharmacology2000.com)
  • Phenoxybenzamine (PB) has been used to probe α-adrenergic receptor subtypes. (pharmacology2000.com)
  • Yohimbine is classified as a selective α 2 -adrenergic receptor antagonist. (pharmacology2000.com)
  • adrenergic receptor antagonists i.e. typically propranolol (Inderal) are used in management of hypertrophic obstructive cardiomyopathy. (pharmacology2000.com)
  • adrenergic receptor antagonists have also shown helpful in management of acute dissecting aortic aneurysm due to -blocker-mediated reduction in myocardial contractility and reduced rate of force development . (pharmacology2000.com)
  • The adrenergic receptors are metabolic G protein-coupled receptors. (proteopedia.org)
  • The β-1 adrenergic receptor (B1AR) increases cardiac output and secretion of rennin and ghrelin. (proteopedia.org)
  • The β-2 adrenergic receptor (B2AR) triggers many relaxation reactions. (proteopedia.org)
  • 3D structures in Adrenergic receptor . (proteopedia.org)
  • Isoprenaline, see Beta-1 Adrenergic receptor , 2y03 . (proteopedia.org)
  • The human β2 adrenergic receptor bound to a G-protein ( 3sn6 ) is featured in a scene above, and additional structures are on the Adrenergic receptor page . (proteopedia.org)
  • For G s see Beta2 adrenergic receptor-Gs protein complex updated . (proteopedia.org)
  • Beta 1- and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ventricular myocardium. (aspetjournals.org)
  • Beta-adrenergic desensitization reduces the sensitivity of adenylate cyclase for magnesium in permeabilized lymphocytes. (aspetjournals.org)
  • Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS. (lookformedical.com)
  • Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (lookformedical.com)
  • A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). (lookformedical.com)
  • The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS. (lookformedical.com)
  • One of two major pharmacologically defined classes of adrenergic receptors. (lookformedical.com)
  • The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. (lookformedical.com)
  • Drugs that selectively bind to and activate beta-adrenergic receptors. (lookformedical.com)
  • Stimulation of the receptor results in activation of adenylate cyclase and increased levels of intracellular cAMP. (targetmol.com)
  • Analysis of both spontaneous synchronizations and those driven by high frequency stimulation of individual ARNKISS neurons revealed that the network exhibits semi-random emergent excitation dependent upon glutamate signaling through AMPA receptors. (bvsalud.org)
  • Transcranial magnetic stimulation (TMS) indices of GABA B receptor mediated inhibitory neurotransmission can be altered through antipsychotic treatment. (biomedcentral.com)
  • TOR Serine-Threonine Kinases" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • This graph shows the total number of publications written about "TOR Serine-Threonine Kinases" by people in Harvard Catalyst Profiles by year, and whether "TOR Serine-Threonine Kinases" was a major or minor topic of these publication. (harvard.edu)
  • Below are the most recent publications written about "TOR Serine-Threonine Kinases" by people in Profiles. (harvard.edu)
  • A class of protein-serine-threonine kinases that was originally found as one of the three types of kinases that phosphorylate GLYCOGEN SYNTHASE. (rush.edu)
  • Recent studies have suggested that dopamine D2 receptor antagonists, which are used in the clinical treatment of schizophrenia, modulate protein kinase B (Akt)/glycogen synthase kinase (GSK)-3 signaling. (biomedcentral.com)
  • GSK-3 is a protein kinase originally identified and named for its ability to phosphorylate and inactivate the metabolic enzyme glycogen synthase [ 11 ]. (biomedcentral.com)
  • The relationship between inositol trisphosphate receptor density and calcium release in brain microsomes. (aspetjournals.org)
  • Reversible blockade suggests that the inhibitor dissociates from the receptor relatively easily. (pharmacology2000.com)
  • Since all reactions are, by definition, reversible, those reactions in which the inhibitor and receptor complex is so stable that dissociation is unlikely are described as 'irreversible. (pharmacology2000.com)
  • Consistently, LTD by dopamine + 1 S ,3 R -ACPD coapplication, as well as the two other forms of LTD (LTD by dopamine + tetani and LTD by 1S,3R-ACPD + tetani), was blocked by bath application of MAP-K kinase inhibitor PD98059. (jneurosci.org)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Adenylate Cyclase 5 (ADCY5) in Tissue homogenates, cell lysates and other biological fluids. (therabio.org)
  • Description: A competitive ELISA for quantitative measurement of Human Adenylate cyclase type 5(ADCY5) in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. (therabio.org)
  • In the next series of experiments, coapplication of dopamine and 1 S ,3 R -ACPD, but not application of either drug alone, consistently induced LTD without tetani or even single test stimuli during drug application, suggesting that coactivation of dopamine receptors and the mGluRs is sufficient for LTD induction. (jneurosci.org)
  • Immunoblot analyses with anti-active mitogen-activated protein kinases (MAP-Ks) revealed that D1 receptors, D2 receptors, group I mGluRs, and group II mGluRs all contribute to MAP-K activation in prefrontal cortex, and that combined activation of dopamine receptors and mGluRs synergistically or additively activate MAP-Ks. (jneurosci.org)
  • Our results suggest that dopamine receptors and groups I and II mGluRs cooperate to induce LTD through converging postsynaptic activation of MAP-Ks. (jneurosci.org)
  • Dopamine receptors are a class of metabotropic G protein-coupled receptors that are important in the central nervous system. (proteopedia.org)
  • In contrast to male mice, ongoing tachykinin receptor tone within the slice operated to promote spontaneous synchronizations in females. (bvsalud.org)
  • After receptor activation, the alpha- and beta-gamma-subunits of G protein dissociate to activate diverse downstream pathways resulting in cellular polarization and actin reorganization. (genome.jp)
  • This results in the dissociation of a Gα-GTP monomer and a Gβγ dimer from the receptor which allows both complexes to begin signalling cascades via downstream effectors. (smpdb.ca)
  • Estrogens stimulate the proliferation and the differentiation of breast epithelial cells through the activation of downstream mitogenic signaling pathways, namely via the estrogen receptors ERα and ERβ. (scirp.org)
  • Hsp90 consumer proteins that influence p53 stability include Mdm2, the E3 ligase that right ubiquitylates and promotes the degradation of p53, Chk1, a downstream kinase of Atm that phosphorylates p53 to disrupt its interaction with Mdm2 and Akt that phosphorylates Mdm2 to enhance p53 accumulation. (cd31-signal.com)
  • All six receptors belong to the G protein-coupled receptor (GPCR) superfamily which initiates intracellular signalling cascades via four G protein classes differentiated by their α subunit type: Gαs, Gαi/o, Gαq/11, Gα12/13. (smpdb.ca)
  • Within the GnRH superfamily members, adipokinetic hormone (AKH) and its receptor are well described in ecdysozoans but understudied in other lineages. (bvsalud.org)
  • Other poorly characterized subtypes include the AT3 and AT4 receptors. (wikipedia.org)
  • Evidence suggests that nerve growth factor (NGF) induces neurite outgrowth from PC12 cells by activating the receptor tyrosine kinase, TrkA. (biomedcentral.com)
  • Loss of Pcs impairs Rab11 localization on the trans-side of Golgi units and induces the cytoplasmic accumulation of post-Golgi vesicles bearing rhabdomere proteins, as observed in Rab11-deficiency. (sdbonline.org)
  • What proteins does IRS-1 bind to in order to activate Raf-1? (flashcardmachine.com)
  • Both calcium and DAG activate the kinase activity of protein kinase C beta (PKC). (smpdb.ca)
  • MEK can phosphorylate and activate ERK, which is transferred into the nucleus and regulates gene expression by activating other kinases or transcription factors. (cusabio.com)
  • Depending on which family the G protein is, it goes on to activate (G αs protein subunit) or inhibit (G αi protein subunit) the membrane-bound cyclase. (pancreapedia.org)
  • As in somatic cells, sperm intracellular cAMP concentration is regulated by the opposite action of two enzymes: the adenylyl cyclases (AC), which synthesize cAMP from ATP, and the phosphodiesterases (PDE), which break the phosphodiester bond of cAMP to form 5'-adenosine monophosphate (AMP). (plos.org)
  • AMP-activated protein kinases modify enzymes involved in LIPID METABOLISM, which in turn provide substrates needed to convert AMP into ATP. (rush.edu)
  • Tetanic stimuli to layer I-II afferents in rat prefrontal cortex induced long-term depression (LTD) of layer I-II to layer V pyramidal neuron glutamatergic synapses when tetani were coupled to bath application of dopamine. (jneurosci.org)
  • Activation of this receptor type centrally reduces sympathetic outflow, which is the proposed mechanism that accounts for antihypertensive actions noted following clonidine administration. (pharmacology2000.com)
  • The AT4 receptor is activated by the angiotensin II metabolite angiotensin IV, and may play a role in regulation of the CNS extracellular matrix, as well as modulation of oxytocin release. (wikipedia.org)
  • Intracellular signaling protein kinases that play a signaling role in the regulation of cellular energy metabolism. (rush.edu)
  • 17-DMAG induced an accumulation of p53 protein but not RNA, implicating regulation of p53 turnover. (cd31-signal.com)
  • For instance, familial AD is linked to mutations in the amyloid precursor protein (APP), presenilin 1, and presenilin 2, all of which lead to increased levels of Aβ. (jneurosci.org)
  • By analyzing specific amino acid mutations of the α 2A - receptor with respect to changes in PB binding, certain sites were identified that may serve as the molecular target for phenoxybenzamine-mediated receptor blockade. (pharmacology2000.com)
  • Receptor-interacting protein (RIP) kinases promote the induction of necrotic cell death pathways. (colinsbraincancer.com)
  • Currently, there are 4 known MAPK signaling pathways, including the extracellular signal-regulated kinase ( ERK ), c- Jun N-terminal kinase (JNK, also known as SAPK), p38 and ERK5 pathways. (cusabio.com)
  • Corticosterone increases protein tyrosine kinase activity in the locus coeruleus and other monoaminergic nuclei of rat brain. (aspetjournals.org)
  • Description: A sandwich ELISA kit for detection of Adenylate Cyclase 5 from Human in samples from blood, serum, plasma, cell culture fluid and other biological fluids. (therabio.org)
  • Price TJ, Das V, Dussor G. Adenosine Monophosphate-activated Protein Kinase (AMPK) Activators For the Prevention, Treatment and Potential Reversal of Pathological Pain. (rush.edu)
  • Inhibition of the p38 MARK pathway down-regulates the activity of protein kinase C ( PKC ), which plays an important role in osteogenic differentiation of cells. (cusabio.com)
  • Impaired proteostatic mechanisms other than decreased protein synthesis limit old skeletal muscle recovery after disuse atrophy. (harvard.edu)
  • A cyclase enzyme (lyase) catalyzes the formation of the cyclic nucleotide from its nucleotide triphosphate precursor ( Figure 1 ). (pancreapedia.org)
  • PRKACB is a member of the Ser/Thr protein kinase family and is a catalytic subunit of AMPK. (thermofisher.com)
  • Effects mediated by the AT2 receptor are suggested to include inhibition of cell growth, fetal tissue development, modulation of extracellular matrix, neuronal regeneration, apoptosis, cellular differentiation, and maybe vasodilation and left ventricular hypertrophy. (wikipedia.org)
  • It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS. (lookformedical.com)
  • If viewed from the synaptic cleft, the protein will look like a pseudo-symmetrical rosette shown in the picture below composed of 10 different alpha and 4 different beta subunits. (proteopedia.org)
  • Tg2576 mice overexpress a mutant form of human amyloid precursor protein with the Swedish mutation (APP Sw ), resulting in high β-amyloid (Aβ) levels in the brain. (jneurosci.org)
  • Despite its small genome and limited number of effector proteins, Ehrlichia efficiently establishes an intracellular infection and avoids immune defenses in vertebrate and invertebrate hosts through complex molecular and cellular reprogramming strategies. (frontiersin.org)
  • A serine threonine kinase that controls a wide range of growth-related cellular processes. (harvard.edu)
  • LKB1 is a serine/threonine kinase mutated in Peutz-Jeghers syndrome (PJS), implicated in many cellular processes including energy metabolism, cell polarization and cell cycle arrest and has also been shown to play an essential role as a tumor suppressor gene by negatively regulating the mTOR pathway. (scirp.org)
  • G protein-coupled receptors (GPCRs) as well as heterotrimeric G proteins are also involved in regulating neurite outgrowth. (biomedcentral.com)
  • Altogether, our results demonstrate that βγ subunit of heterotrimeric G proteins play a critical role in neurite outgrowth and differentiation by interacting with MTs and modulating MT rearrangement. (biomedcentral.com)
  • Mechanisms by which E. chaffeensis establishes intracellular infection, and avoids host defenses are not well understood, but involve functionally relevant host-pathogen interactions associated with tandem and ankyrin repeat effector proteins. (frontiersin.org)
  • Because we have shown earlier that prenylation and subsequent methylation/demethylation of γ subunits are required for the Gβγ-MTs interaction in vitro , small-molecule inhibitors (L-28 and L-23) targeting prenylated methylated protein methyl esterase (PMPMEase) were tested in the current study. (biomedcentral.com)
  • The second signaling mechanism involves the binding of a small signaling molecule to a soluble cyclase. (pancreapedia.org)