• A beta-adrenergic receptor kinase-like enzyme is involved in olfactory signal termination. (duke.edu)
  • Bbeta-adrenergic receptor kinase-1 levels in catecholamine-induced myocardial hypertrophy: regulation by beta- but not alpha1-adrenergic stimulation. (duke.edu)
  • beta2-Adrenergic receptor regulation by GIT1, a G protein-coupled receptor kinase-associated ADP ribosylation factor GTPase-activating protein. (duke.edu)
  • Chronic human heart failure is characterized by abnormalities in beta-adrenergic receptor (betaAR) signaling, including increased levels of betaAR kinase 1 (betaARK1), which seems critical to the pathogenesis of the disease. (duke.edu)
  • Direct evidence that Gi-coupled receptor stimulation of mitogen-activated protein kinase is mediated by G beta gamma activation of p21ras. (duke.edu)
  • Essential role of beta-adrenergic receptor kinase 1 in cardiac development and function. (duke.edu)
  • The beta-adrenergic receptor kinase 1 (beta ARK1) is a member of the G protein-coupled receptor kinase (GRK) family that mediates the agonist-dependent phosphorylation and desensitization of G protein-coupled receptors. (duke.edu)
  • Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice. (duke.edu)
  • Functional desensitization of the isolated beta-adrenergic receptor by the beta-adrenergic receptor kinase: potential role of an analog of the retinal protein arrestin (48-kDa protein). (duke.edu)
  • The beta-adrenergic receptor kinase is an enzyme, possibly analogous to rhodopsin kinase, that multiply phosphorylates the beta-adrenergic receptor only when it is occupied by stimulatory agonists. (duke.edu)
  • Functionally active targeting domain of the beta-adrenergic receptor kinase: an inhibitor of G beta gamma-mediated stimulation of type II adenylyl cyclase. (duke.edu)
  • 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. (duke.edu)
  • Chronic/pathologic GPCR signaling elicits the interaction of the G-protein Gbetagamma subunit with GPCR kinase 2 (GRK2), targeting the receptor for internalization, scaffolding to pathologic signals, and receptor degradation. (cusabio.com)
  • The beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G protein-coupled receptors. (utsouthwestern.edu)
  • Overall, the beta adrenergic receptor kinase 2 has 85% amino acid similarity with beta adrenergic receptor kinase 1, with the protein kinase catalytic domain having 95% similarity. (utsouthwestern.edu)
  • High expression of beta-adrenergic receptor kinase in human peripheral blood leukocytes. (unich.it)
  • A selective kinase (called beta-adrenergic receptor kinase, beta ARK) has been identified which phosphorylates the agonist-occupied form of the receptor. (unich.it)
  • Very high levels of beta ARK mRNA and kinase activity were found in peripheral blood leukocytes and in several myeloid and lymphoid leukemia cell lines. (unich.it)
  • 1 Cyclic AMP activates protein kinase A (PKA), which phosphorylates cardiac L-type calcium channels such as Ca v 1.2. (drugbank.com)
  • A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS and a variety of other G-PROTEIN-COUPLED RECEPTORS. (lookformedical.com)
  • Although it is highly homologous to G-PROTEIN-COUPLED RECEPTOR KINASE 2, it is not considered to play an essential role in regulating myocardial contractile response. (lookformedical.com)
  • A G-protein-coupled receptor kinase subtype that is primarily expressed in the MYOCARDIUM and may play a role in the regulation of cardiac functions. (lookformedical.com)
  • We have identified a novel G protein-coupled receptor kinase-interacting protein, GIT1, that is a GTPase-activating protein (GAP) for the ADP ribosylation factor (ARF) family of small GTP-binding proteins. (duke.edu)
  • 2005. Ca2+/calmodulin-dependent protein kinase modulates cardiac ryanodine receptor phosphorylation and sarcoplasmic reticulum Ca2+ leak in heart failure. (badrilla.com)
  • Risk factors for depression initiate an infection-like inflammation in the brain that involves activation microglial Toll-like receptors and glycogen synthase kinase-3β (GSK3β). (mdpi.com)
  • AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity. (bnwax.com)
  • In pathological myocardial remodeling acts downstream of the beta adrenergic receptor signaling cascade to regulate key proteins involved in ECC. (icr.ac.uk)
  • 10 PKA phosphorylates scaffolding proteins and sodium channels, increasing the number of sodium channels on the apical side of alveolar cells and increasing active transport of sodium ions into cells. (drugbank.com)
  • Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors. (lookformedical.com)
  • They are regulatory proteins that play a role in G-protein-coupled receptor densensitization. (lookformedical.com)
  • These results suggest an essential role for ARF proteins in regulating beta2-adrenergic receptor endocytosis. (duke.edu)
  • Recent developments in mass spectrometry-based phosphoproteomics have led to the identification of thousands of differentially phosphorylated proteins and their phosphorylation sites. (molcells.org)
  • However, functional studies of these differentially phosphorylated proteins have not been conducted in a large-scale or high-throughput manner due to a lack of methods capable of revealing the functional relevance of each phosphorylation site. (molcells.org)
  • A pathological cardiac hypertrophy model, junctate-1 transgenic mice and control mice, were analyzed using label-free quantitative phosphoproteomics to identify differentially phosphorylated proteins and sites. (molcells.org)
  • BACKGROUND AND PURPOSE: The cannabinoid CB(1) receptor is primarily thought to be functionally coupled to the G(i) form of G proteins, through which it negatively regulates cAMP accumulation. (bvsalud.org)
  • Our studies provide new insight into the mechanisms governing the coupling of CB(1) receptors to G proteins and cannabinoid-induced tolerance. (bvsalud.org)
  • 2011. Angiotensin receptor blockade improves the net balance of cardiac Ca(2+) handling-related proteins in sympathetic hyperactivity-induced heart failure. (badrilla.com)
  • Epinephrine and norepinephrine through alpha -adrenoreceptors (α1ARs and α2ARs) and beta -adrenoreceptors (β1ARs, β2ARs, β3ARs) bind to proteins in the peripheral nervous system. (nature-nurture.org)
  • In its quiescent state NF-κB is found in the cytoplasm bound to two proteins, IκBα and IκBβ (Inhibitor kappa B alpha and beta) that prevent it from translocating to the cell's nucleus for gene expression (Barnes & Karin, 1997). (nature-nurture.org)
  • This allows for many GPCR combinations created by different receptors being coupled with G proteins comprised of different subunits. (teachmephysiology.com)
  • Receptor-stimulated guanine-nucleotide-triphosphate binding to guanine-nucleotide-binding regulatory proteins. (eurekamag.com)
  • The data thus provide evidence for an essential difference between GTP[S] and p[NH]ppG binding to guanine-nucleotide-binding regulatory proteins and suggest that, in addition to the nucleotide-exchange reaction, a (thio)phosphate-group-transfer process via guanine-nucleotide-binding regulatory protein beta subunits is involved in the receptor-stimulated binding of guanine nucleotide triphosphates to guanine-nucleotide-binding regulatory proteins. (eurekamag.com)
  • In humans, melatonin is a full agonist of melatonin receptor 1 (picomolar binding affinity) and melatonin receptor 2 (nanomolar binding affinity), both of which belong to the class of G-protein coupled receptors (GPCRs). (wikipedia.org)
  • Melatonin receptors 1 and 2 are both Gi/o-coupled GPCRs, although melatonin receptor 1 is also Gq-coupled. (wikipedia.org)
  • We are primarily using cytomegaloviruses to examine how the pathogens alter signaling pathways directed by G-protein coupled receptors (GPCRs) to facilitate robust replication in tissues important for host-host dissemination. (uc.edu)
  • A novel regulatory role of GRK2 was proposed for the ubiquitination of beta-arrestin in the context of the PKC-mediated heterologous regulation of GPCRs. (cusabio.com)
  • Both of these tension hormones signal with their particular GPCRs, beta-adrenergic receptors and CRF1 receptor, that few to Gs protein to improve cAMP amounts in cells [70, 71]. (bio-biz-navi.com)
  • Arrestins are best known for their role in homologous desensitization of G protein-coupled receptors (GPCRs). (bvsalud.org)
  • Arrestins quench G protein activation by binding to activated phosphorylated GPCRs. (bvsalud.org)
  • G-protein coupled receptors (GPCRs) are a diverse family of receptors found in a huge range of tissues throughout the body. (teachmephysiology.com)
  • There are hundreds of GPCRs in the genome and their receptors are activated by many signals such as neurotransmitters , hormones, ions, peptides and even photons in the retina. (teachmephysiology.com)
  • Common examples of GPCRs include adrenoreceptors , muscarinic acetylcholine receptors and opioid receptors. (teachmephysiology.com)
  • These two branches control heart rate by stimulating different G protein-coupled receptors (GPCRs), which in turn activate ion channels that modify the electrical properties of cardiac pacemaker cells ( DiFrancesco, 1993 ). (elifesciences.org)
  • G protein-coupled receptor activation leads to the membrane recruitment and activation of G protein-coupled receptor kinases, which phosphorylate receptors and lead to their inactivation. (duke.edu)
  • Stimulation of Gi-coupled receptors leads to the activation of mitogen-activated protein kinases (MAP kinases). (duke.edu)
  • These data suggest the existence of a family of receptor kinases which may serve broadly to regulate receptor function. (utsouthwestern.edu)
  • A family of serine-threonine kinases that are specific for G-PROTEIN-COUPLED RECEPTORS. (lookformedical.com)
  • Receptor phosphorylation is a key step in the process of desensitization of the beta-adrenergic and other related receptors. (unich.it)
  • May participate in the modulation of skeletal muscle function in response to exercise, by regulating SR Ca(2+) transport through phosphorylation of PLN/PLB and triadin, a ryanodine receptor-coupling factor. (icr.ac.uk)
  • Overexpression of GIT1 leads to reduced beta2-adrenergic receptor signaling and increased receptor phosphorylation, which result from reduced receptor internalization and resensitization. (duke.edu)
  • A cell-based functional assay system measuring hypertrophic cell growth of neonatal rat ventricle cardiomyocytes (NRVMs) following phenylephrine treatment was applied, and changes in phosphorylation of individual differentially phosphorylated sites were induced by incorporation of phosphorylation competition peptides conjugated with cell-penetrating peptides. (molcells.org)
  • Our integrated approach can be used to identify functionally important phosphorylation sites among differentially phosphorylated sites, and unlike conventional approaches, it is easily applicable for large-scale and/or high-throughput analyses. (molcells.org)
  • Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. (joplink.net)
  • 2 Agonism of beta-1 and beta-2 adrenergic receptors causes the alpha subunit of G-protein coupled receptors to exchange GMP for GTP, activating them, and allowing the alpha subunit to dissociate from the beta and gamma subunits. (drugbank.com)
  • The G-protein is heterotrimeric and is made up of three different subunits: alpha ( α ), beta ( β ) and gamma ( γ ). (teachmephysiology.com)
  • Stimulated muscarinic acetylcholine receptors (M2Rs) release Gβγ subunits, which slow heart rate by activating a G protein-gated K + channel (GIRK). (elifesciences.org)
  • Stimulated β2 adrenergic receptors (β2ARs) also release Gβγ subunits, but GIRK is not activated. (elifesciences.org)
  • In the alveoli, agonism of beta-2 adrenergic receptors, activates similar pathways to the heart, however the end result is regulation of sodium channels, the cystic fibrosis transmembrane conductance regulator (CFTR), and sodium potassium ATPase. (drugbank.com)
  • These results could be reproduced by computer modeling of the border zone based on our knowledge of β-adrenergic receptor signaling pathways and their influence on intracellular calcium handling and ion channels. (frontiersin.org)
  • The expression levels of LPL (lipoprotein lipase), HSL (Hormone-sensitive lipase), FAS (fatty acid synthase), and PPARα/PPARγ (peroxisome proliferator-activated receptor alpha/gamma) were significantly changed in the sheep preadipocytes during differentiation for 7 days. (academic-accelerator.com)
  • Longer-term (24 and 48 h) treatment reduced the expression of lipogenic markers (FA synthase and sterol regulatory element-binding protein-1) and increased the expression of lipolytic [hormone-sensitive lipase (HSL) and adipose triglyceride lipase (ATGL)] and mitochondrial (peroxisome proliferator-activated receptor γ coactivator-1α and carnitine palmitoyltransferase 1) markers. (academic-accelerator.com)
  • 05) expression of peroxisome proliferator-activated receptor α (PPARα) and expressions for Ppara and hormone sensitive lipase (HSL) in the liver of IUGR-C rats than the IUGR rats. (academic-accelerator.com)
  • Regulates Ca(2+) influx to myocytes by binding and phosphorylating the L-type Ca(2+) channel subunit beta-2 CACNB2. (icr.ac.uk)
  • Despite the fact that one G-protein coupled receptor only contains one α-subunit, this can interact with several secondary messengers , which can in turn activate multiple enzymes and catalyse many reactions. (teachmephysiology.com)
  • The activated receptor catalyzes removal of GDP from the G protein alpha subunit (Gα i ), which allows intracellular GTP to bind. (elifesciences.org)
  • Using CB(1)/CB(2) chimeric receptors, the second intracellular loop (ICL2) of the CB(1) receptor was identified as primarily responsible for mediating G(s) and G(i) coupling specificity. (bvsalud.org)
  • BACKGROUND AND PURPOSE: We have investigated the effect of deletions of a postsynaptic density, disc large and zo-1 protein (PDZ) motif at the end of the COOH-terminus of the rat A(2B) adenosine receptor on intracellular trafficking following long-term exposure to the agonist 5'-(N-ethylcarboxamido)-adenosine. (bvsalud.org)
  • The intracellular compartment through which the Gln(325)-stop receptor mutant, which lacks the Type II PDZ motif found in the wild type receptor initially trafficked was not the same as the wild type receptor. (bvsalud.org)
  • 2008. Intracellular mechanisms of specific beta-adrenoceptor antagonists involved in improved cardiac function and survival in a genetic model of heart failure. (badrilla.com)
  • Since a recognized function of GRK3 is certainly to phosphorylate and desensitize CRF1 receptor that indicators to activate CREB, up-regulation of GRK3 by CRF1 was hypothesized as a poor feedback regulation to regulate the activation from the receptor [71]. (bio-biz-navi.com)
  • Animal steroid hormones initiate signaling by passive diffusion into cells and binding to their nuclear receptors to regulate gene expression. (biologists.com)
  • beta, gamma-imino]triphosphate, p[NH]ppG, and the regulation of binding by the formyl-peptide-receptor agonist, fMet-Leu-Phe, were studied in membranes of differentiated HL-60 cells. (eurekamag.com)
  • The thiophosphorylation state of this protein was regulated by guanine nucleotides, Mg2+ and, most importantly, by activated formyl-peptide receptors. (eurekamag.com)
  • CONCLUSIONS AND IMPLICATIONS: The ICL2 of CB(1) receptors and in particular Leu-222, which resides within a highly conserved DRY(X)(5) PL motif, played a critical role in G(s) and G(i) protein coupling and specificity. (bvsalud.org)
  • 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)
  • Natural regulators of brown and beige fat include external conditions like cold temperatures, and exercise, as well as internal mechanisms like thyroid hormones, beta-adrenergic hormones, retinoids, PPARγ and PPARα agonists, and the liver X receptor. (mrsupps.com)
  • We hypothesize that the border zone is most vulnerable to alternans, that β-adrenergic receptor stimulation can suppresses this, and investigate the consequences in terms of arrhythmogenic mechanisms. (frontiersin.org)
  • β-Adrenergic receptor stimulation with norepinephrine (1 μmol/L) attenuated alternans by 60 [52-65]% [interquartile range] and this was reversed with metoprolol (10 μmol/L, p = 0.008). (frontiersin.org)
  • Simulations also demonstrated that β-adrenergic receptor stimulation in this specific region reduced the formation of conduction block and the probability of premature ventricular activation propagation. (frontiersin.org)
  • While high levels of overall cardiac sympathetic drive are a negative prognostic indicator of mortality following MI and during heart failure, β-adrenergic receptor stimulation in the infarct border zone reduced spatially heterogeneous alternans, and prevented conduction block and propagation of extrasystoles. (frontiersin.org)
  • Protein phosphatase activity is increased in a rat model of long-term beta-adrenergic stimulation. (badrilla.com)
  • Melatonin also acts as a high-capacity free radical scavenger within mitochondria which also promotes the expression of antioxidant enzymes such as superoxide dismutase, glutathione peroxidase, glutathione reductase, and catalase via signal transduction through melatonin receptors. (wikipedia.org)
  • Via signal transduction through melatonin receptors, melatonin promotes the expression of antioxidant enzymes such as superoxide dismutase, glutathione peroxidase, glutathione reductase, and catalase. (wikipedia.org)
  • binding to the central NMDA receptor may result in amelioration of neuropathic pain. (medindex.am)
  • Alterations in cardiac adrenergic signaling and calcium cycling differentially affect the progression of cardiomyopathy. (duke.edu)
  • Cardiac beta ARK1 inhibition prolongs survival and augments beta blocker therapy in a mouse model of severe heart failure. (duke.edu)
  • Although cardiac hypertrophy is initiated by various receptors at cell membranes sensing biomechanical signals and hormones, it is generally mediated by cellular signaling cascades. (molcells.org)
  • These epub nuclear receptors as molecular targets for cardiometabolic and central nervous system diseases solvay pharmaceuticals bloodletting polypeptides have increased generally generally of cardiac eye and blood response. (siriuspixels.com)
  • It was proposed that beta ARK may be primarily active on synaptic receptors. (unich.it)
  • Alternatively, GRK3 may action through phosphorylating non-GPCR function or substrates being a scaffold protein, as having been proven for various other GRKs, such as for example GRK5 and GRK2 [78C80]. (bio-biz-navi.com)
  • Moreover, they provide a mechanism for integration of receptor activation and endocytosis through regulation of ARF protein activation by GRK-mediated recruitment of the GIT1 ARF GAP to the plasma membrane. (duke.edu)
  • Our results indicate that the lin-4-lin-14 and the lin-28-let-7-lin-41 regulatory circuits control the timing of dendrite arborization through antagonistic regulation of the DMA-1 receptor level on dendrites. (stanford.edu)
  • 2011. Impaired beta-adrenergic responsiveness accentuates dysfunctional excitation-contraction coupling in an ovine model of tachypacing-induced heart failure. (badrilla.com)
  • Results demonstrate that GPR3 signals at the plasma membrane and can be silenced by GRK2/beta-arrestin overexpression. (cusabio.com)
  • In human mononuclear leukocytes, beta-AR agonist isoproterenol and platelet-activating factor were able to induce translocation of beta ARK from cytosol to membrane. (unich.it)
  • 20-min exposure to platelet-activating factor (1 microM) reduced the cytosolic beta ARK activity to 42% of control with concomitant increase in membrane beta ARK activity to 214% of control. (unich.it)
  • Therefore, endocytic removal of polarized receptors that diffuse into the AIS serves as a membrane-clearance mechanism thatis likely to work in conjunction with the known AIS diffusion-barrier mechanism to maintain neuronal polarity on the plasma membrane. (stanford.edu)
  • Prostate-specific membrane antigen cleavage of vitamin B9 stimulates oncogenic signaling through metabotropic glutamate receptors. (bnwax.com)
  • The G-protein then reassociates with the transmembrane receptor, reforming the GPCR for the next ligand binding. (teachmephysiology.com)
  • Phosphorylates phospholamban (PLN/PLB), an endogenous inhibitor of SERCA2A/ATP2A2, contributing to the enhancement of SR Ca(2+) uptake that may be important in frequency-dependent acceleration of relaxation (FDAR) and maintenance of contractile function during acidosis. (icr.ac.uk)
  • 2004. Ouabain treatment is associated with upregulation of phosphatase inhibitor-1 and Na+/Ca2+-exchanger and beta-adrenergic sensitization in rat hearts. (badrilla.com)
  • PHENOTYPE: Animals homozygous for a mutation of this gene appear normal and are fertile, but exhibit a lack of odorant receptor-mediated desensitization in the olfactory epithelium. (utsouthwestern.edu)
  • Overcoming acquired resistance to cetuximab by dual targeting HER family receptors with antibody-based therapy. (bnwax.com)
  • The high levels of beta ARK expression in human peripheral blood leukocytes together with the ability of isoproterenol and platelet-activating factor to induce beta ARK translocation, suggest a role for beta ARK in modulating some receptor-mediated immune functions. (unich.it)
  • In the nucleus, phosphorylates the MEF2 repressor HDAC4, promoting its nuclear export and binding to 14-3-3 protein, and expression of MEF2 and genes involved in the hypertrophic program. (icr.ac.uk)
  • Forcing receptor interaction with the AIS master organizer, ankyrinG, antagonizes receptor endocytosis in the AIS, causes receptor accumulation in the AIS, and leads to polarity deficits with subsequent morphological and behavioural defects. (stanford.edu)
  • A family of G-protein-coupled receptors that was originally identified by its ability to bind N-formyl peptides such as N-FORMYLMETHIONINE LEUCYL-PHENYLALANINE. (lookformedical.com)
  • Since N-formyl peptides are found in MITOCHONDRIA and BACTERIA, this class of receptors is believed to play a role in mediating cellular responses to cellular damage and bacterial invasion. (lookformedical.com)
  • Arrestin quenches G-protein activation by binding to phosphorylated photolyzed rhodopsin. (lookformedical.com)
  • One of the mediators of the positive metabolic effects of endurance exercise is peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α). (mrsupps.com)
  • Apoptosis is programmed cell death triggered by activation of death receptors or cellular stress. (bvsalud.org)
  • An agonist (ligand) is a substance which binds to a receptor and brings about a cellular response. (teachmephysiology.com)
  • 2007. Serotonin increases L-type Ca2+ current and SR Ca2+ content through 5-HT4 receptors in failing rat ventricular cardiomyocytes. (badrilla.com)
  • Endosomes internalize macromolecules bound by receptors on the cell surface. (lookformedical.com)
  • congestive epub nuclear receptors as molecular targets for cardiometabolic: A modification embedded by the enzymatic phenyl that is the Evaluation disease and order Study. (siriuspixels.com)
  • Sirius Pixels UHDe HEVC Encoder also, when the epub nuclear receptors as molecular targets for cardiometabolic and central nervous system diseases solvay pharmaceuticals conferences is not marketed, the code's abnormalities trigger sequentially shown. (siriuspixels.com)
  • This may break while involved acute interested epub nuclear receptors as molecular is well present to a ability in white Bactericidal parent Plasma with caused Propulsive character catheter. (siriuspixels.com)
  • Nonselective beta blocker, you directly into the phenothiazines appear to go to whether these therapies like pulse and primidone. (fireresearch.cn)
  • Funding: william d in costs that its antiarrhythmic effects of beta-blocker used, and treatment of migraines. (fireresearch.cn)
  • 79 years corresponding diminution of regulatory protein should show no follicles and not understand ligand-receptor interactions. (notinovedades.com)
  • Isoprenaline is a catecholamine non-selective beta-adrenergic agonist typically used to treat bradycardia and heart block. (drugbank.com)
  • Isoprenaline is a non-selective beta adrenergic receptor agonist used in a number of indications for the heart, as well as bronchospasm in anesthesia. (drugbank.com)
  • Isoprenaline is a non-selective beta adrenergic receptor agonist. (drugbank.com)
  • CAMK2 is composed of 4 different chains: alpha (CAMK2A), beta (CAMK2B), gamma (CAMK2G), and delta (CAMK2D). (icr.ac.uk)
  • Here, we investigated the dual coupling properties of CB(1) receptors and characterized the structural determinants that mediate selective coupling to G(s) and G(i). (bvsalud.org)
  • CB(1)/CB(2) receptor chimeras and site-directed mutagenesis combined with functional assays and computer modelling were used to determine the structural determinants mediating selective coupling to G(s) and G(i). (bvsalud.org)
  • Many of its effects are through activation of the melatonin receptors, while others are due to its role as an antioxidant. (wikipedia.org)
  • Agonism of beta-2 adrenergic receptors leads to glycogenolysis in the liver, 5 glucagon release from the pancreas, and activation of the renin-angiotensin-aldosterone system. (drugbank.com)
  • Here we demonstrate that arrestin-2 isoform is cleaved by caspases during apoptosis induced via death receptor activation or by DNA damage at evolutionarily conserved sites in the C-terminus. (bvsalud.org)
  • KEY RESULTS: CB(1) receptors could couple to both G(s)-mediated cAMP accumulation and G(i)-induced activation of ERK1/2 and Ca(2+) mobilization, whereas CB(2) receptors selectively coupled to G(i) and inhibited cAMP production. (bvsalud.org)
  • Any positive immunological effect is thought to be the result of melatonin acting on high-affinity receptors (MT1 and MT2) expressed in immunocompetent cells. (wikipedia.org)
  • However, non-formylated peptide ligands have also been found for this receptor class. (lookformedical.com)
  • Ligands bind to the extracellular portion of the G-protein coupled receptor, binding either at the N-terminus or a binding site within the transmembrane region. (teachmephysiology.com)
  • 2009;107:785-96, Smith N, Stoddart L, Devine N, Jenkins L, Milligan G. The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1. (bnwax.com)