• A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). (wikipedia.org)
  • PDE4 hydrolyzes cyclic adenosine monophosphate (cAMP) to inactive adenosine monophosphate (AMP). (wikipedia.org)
  • PDE-4 is a cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase that is predominantly located in inflammatory cells. (medeasy.health)
  • The two well-established cyclic nucleotides are adenosine-3',5'-cyclic monophosphate (cyclic AMP) and guanine-3',5'-cyclic monophosphate (cyclic GMP). (pancreapedia.org)
  • BACKGROUND: ß1AR (beta-1 adrenergic receptor) and ß2AR (beta-2 adrenergic receptor)-mediated cyclic adenosine monophosphate signaling has distinct effects on cardiac function and heart failure progression. (bvsalud.org)
  • The localization pattern is altered post-myocardial infarction, resulting from transverse tubule remodeling, leading to distorted ß2AR-mediated cyclic adenosine monophosphate signaling. (bvsalud.org)
  • This study investigated the effects of cyclic adenosine monophosphate modulating during cumulus-oocyte complexes (COCs) pre-maturation and the role of melatonin on in vitro maturation (IVM) of bovine COCs. (bvsalud.org)
  • 4. Chen X, Wang N, Liu Y, Liu Y, Zhang T, Zhu L, Wang Y, Wu C, Yang J. (2014) Yonkenafil: a novel phosphodiesterase type 5 inhibitor induces neuronal network potentiation by a cGMP-dependent Nogo-R axis in acute experimental stroke. (guidetopharmacology.org)
  • Phosphodiesterase 11A (PDE11A), an enzyme that degrades cyclic nucleotides (cAMP and cGMP), is the only PDE whose mRNA expression in brain is restricted to the hippocampal formation. (frontiersin.org)
  • On the horizon, novel insights into metabolism and energy homeostasis reveal guanosine 3′,5′-cyclic monophosphate (cGMP) signaling circuits as emerging targets for antiobesity pharmacotherapy. (eddoctor24h.com)
  • Cyclic nucleotide phosphodiesterase-mediated integration of cGMP and cAMP signaling in cells of the cardiovascular system. (bardonreorg.hu)
  • 2005 ). cAMP and cGMP are hydrolyzed by phosphodiesterase (PDE) enzymes, and inhibitors of PDEs (PDE-Is) produce cognition-enhancing effects in animal models of cognition. (springer.com)
  • It inhibits PDE4 to the greatest extent, but also shows significant inhibition of other PDE subtypes, and so acts as a selective PDE4 inhibitor or a non-selective phosphodiesterase inhibitor, depending on the dose. (wikipedia.org)
  • Apemilast 10 mg is a novel, orally available small molecule inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4). (medeasy.health)
  • The interaction with the non-selective PDE (cyclic nucleotide phosphodiesterase) inhibitor 3-isobutyl-1-methylxanthine (IBMX) was tested after three days. (scirp.org)
  • BRL 50481 is a selective, substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (K i = 180 nM). (tocris.com)
  • [6] Another class of inhibitor proteins is the ribonuclease inhibitors , which bind to ribonucleases in one of the tightest known protein-protein interactions . (wikipedia.org)
  • In human ASM cells, these constituents decreased phosphorylation of 17-kD protein kinase C-potentiated inhibitory protein of type 1 protein phosphatase and 8-gingerol decreased myosin light chain phosphorylation. (nih.gov)
  • 2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. (axonmedchem.com)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • Chen, Z.S., Lee, K. and Kruh, G.D. (2001) Transport of Cyclic Nucleotides and Estradiol 17-Beta-d-glucuronide by Multidrug Resistance Protein 4. (scirp.org)
  • 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)
  • These cyclic nucleotides in turn activate a series of kinases that phosphorylate the transcription factors cAMP response element binding protein ( CREB ) and serum response factor ( SRF ), leading to the expression of plasticity-related genes. (nootropicsexpert.com)
  • Garg, U.C. and Hassid, A. (1989) Nitric Oxide-Generating Vasodilators and 8-Bromo-cyclic Guanosine Monophosphate Inhibit Mitogenesis and Proliferation of Cultured Rat Vascular Smooth Muscle Cells. (scirp.org)
  • Purified phosphodiesterase (PDE) 4D or phospholipase C β enzyme was used to assess inhibitory activity of ginger components using fluorescent assays. (nih.gov)
  • A cyclase enzyme (lyase) catalyzes the formation of the cyclic nucleotide from its nucleotide triphosphate precursor ( Figure 1 ). (pancreapedia.org)
  • Reversible inhibitors produce different types of inhibition depending on whether they bind to the enzyme, the enzyme-substrate complex, or both. (wikipedia.org)
  • Hence the discovery and refinement of enzyme inhibitors is an active area of research in biochemistry and pharmacology . (wikipedia.org)
  • Together with β-agonists, 6-gingerol, 8-gingerol, or 6-shogaol may augment existing asthma therapy, resulting in relief of symptoms through complementary intracellular pathways. (nih.gov)
  • Transformation of znuA mutant with a shuttle vector pBBR1MCS-4 containing znuA gene restored the growth in zinc chelated medium and intracellular replication in HeLa cells and macrophages to a level comparable to that of wild-type strain. (go.jp)
  • This editorial highlights the relevance of interfering in cancer cell progression through the pharmacological manipulation on the cell metabolism of cyclic nucleotides such as cAMP, and on the intracellular Ca2+ signaling, which may avail the reduction of toxic effects promoted by chemotherapy, radiotherapy and immunotherapy, thus decreasing the incidence of interruption in antitumoral treatment. (researchgate.net)
  • The combination synergistically suppresses release of proinflammatory mediators, including tumour necrosis factor-α, IL-6, chemokine (C-C motif) ligand 5 (RANTES), matrix metalloproteinase-9, and others, from human peripheral blood mononuclear cells and mouse macrophages. (biomedcentral.com)
  • Given its ability to transport important intra- and intercellular mediators such as cyclic nucleotides and eicosanoids, the physiological repertoire of MRP4 is thought to cover platelet aggregation, cell migration and proliferation, angiogenesis, and cardiomyocyte contraction. (solvobiotech.com)
  • Considering that IBMX had not an additional effect to potentiate inhibition of meiotic resumption, a combination of C-type natriuretic peptide and forskolin was chosen. (bvsalud.org)
  • Selective phosphodiesterase (PDE) inhibitors improve the formation of hippocampus-dependent memories in several rodent models of cognition. (springer.com)
  • 1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. (axonmedchem.com)
  • 29. T ljedal I-B: Glucose-6-phosphatase in pancreatic -cell metabolism. (taljedal.se)
  • In addition, increases in GPX, SOD3, G6PD, HK, and PFK at proteomic and transcriptomic levels suggested elevation of glycolysis and pentose phosphate pathway, synthesis of glutathione and nucleotides, and antioxidative pathway activity, whereas oxidative phosphorylation, TCA and mitochondrial energy metabolism were reduced. (frontiersin.org)
  • 6-Gingerol, 8-gingerol, or 6-shogaol significantly inhibited PDE4D, whereas 8-gingerol and 6-shogaol also inhibited phospholipase C β activity. (nih.gov)
  • There are two types of nitrogenous bases: purines (adenine and guanine) and pyrimidines (cytosine, uracil and thymine). (pancreapedia.org)
  • The non-canonical cyclic nucleotides include the purines inosine-3',5'-cyclic monophosphate (cyclic IMP), xanthosine-3',5'-cyclic monophosphate (cyclic XMP) and the pyrimidines cytidine-3',5'-cyclic monophosphate (cyclic cCMP), uridine-3',5'-cyclic monophosphate (cyclic UMP), and thymidine-3',5'-cyclic monophosphate (cTMP) (145). (pancreapedia.org)
  • They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. (axonmedchem.com)
  • Considerably higher resistance against cyclic nucleotide phosphodiesterases compared to dibutyryl- or 8-Br-cAMP (Cat. (biolog.de)
  • Elks, M. L. & Manganiello, V. C. Antilipolytic action of insulin: role of cAMP phosphodiesterase activation. (nature.com)
  • This cyclic conformation allows cyclic nucleotides to bind to proteins to which other nucleotides cannot. (pancreapedia.org)
  • Induced EndoMT cells exhibited up-regulation of mesenchymal markers, including collagen type I and α-smooth muscle actin, and a reduction in endothelial cell and junctional proteins, including von Willebrand factor, CD31, occludin, and vascular endothelial-cadherin. (surrey.ac.uk)
  • Interestingly, we found that isolation-induced decreases in membrane PDE11A4 correlated with increased expression of interleukin-6 (IL-6) in the soluble fraction, suggesting pro-inflammatory signaling for this cytokine. (frontiersin.org)
  • In rat models of acute lipopolysaccharide-induced endotoxemia and delayed-type hypersensitivity, and in chronic models of collagen-induced and adjuvant-induced arthritis, the combination produced anti-inflammatory activity that required only a subtherapeutic dose of prednisolone. (biomedcentral.com)
  • MATERIALS AND METHODS: Mining chemical ingredients reported in LCDD, 144 compounds covering all herbs were selected and screened against inflammatory-, immunity- and respiratory-related GPCRs including GPR35, H1, CB2, B2, M3 and ß2-adrenoceptor receptor using a label-free integrative pharmacology method. (bvsalud.org)
  • Intravenous injection induced significant hepatic injury based on pathological inspection and increased the levels of AST/ALT and the inflammatory factors IL-6, IL-1β and TNF-a. (frontiersin.org)
  • On the other hand, oral administration of MSNs disturbed inflammatory factors and metabolites of ribose-5-phosphate, 6-phosphogluconate, GSSG, and NADP+ associated with the pentose phosphate pathway, glutathione synthesis and oxidative stress albeit to a lesser extent than intravenous injection despite the administration of a ten-fold greater dose. (frontiersin.org)
  • Translation tags are based on the publication type and the MeSH terms NLM assigns to the publication. (viictr.org)
  • The his- Bariatric surgery reduces the size of the stomach, increases tory of dietary supplements is full of success stories in terms the feeling of fullness, and reduces the amount of food intake.8 of efficacy, but this success is matched by tragedy with regard Different types of bariatric surgery include the following: to safety. (eddoctor24h.com)
  • Tissues were relaxed dose dependently with β-agonist, isoproterenol, in the presence of vehicle, 6-gingerol, 8-gingerol, or 6-shogaol (100 μM). (nih.gov)
  • 6-Shogaol showed the largest shift in isoproterenol half-maximal effective concentration. (nih.gov)
  • In experiment one, COCs were pre-matured for 8 h in control medium or with 3-isobutyl-1-methylxanthine (IBMX) and forskolin, IBMX and C-type natriuretic peptide, c-type natriuretic peptide and forskolin or IBMX, forskolin and c-type natriuretic peptide. (bvsalud.org)
  • In experiment 1, COCs pre-matured with both C-type natriuretic peptide and forskolin or C-type natriuretic peptide, forskolin and IBMX had lower meiotic resumption rate when compared to control. (bvsalud.org)
  • If its negative charge is not reduced, the nucleotide triphosphate cannot be approached by a nucleophile, which is, in this reaction, the 3' hydroxyl group of the ribose (183). (pancreapedia.org)
  • The end products of this catalytic reaction are a cyclic nucleotide (cyclic AMP or cyclic GMP) and a pyrophosphate group. (pancreapedia.org)
  • 16. T ljedal I-B: Some aspects of the apparent glucose-6-phsophatase activity in the pancreatic islets of mammals. (taljedal.se)
  • Some aspects of the apparent glucose-6-phosphatase activity in obese-hyperglycemice mice and guinea-pigs. (taljedal.se)
  • 27. T ljedal I-B: Presence, inducation and possible role of glucose 6-phosphatase in mammalian pancreatic islets. (taljedal.se)
  • 28. T ljedal I-B: Kinetics of glucose 6-phosphatase in pancreatic islets as revealed by staining histochemistry. (taljedal.se)
  • Following the 5-day titration, the recommended maintenance dosage is 30 mg twice daily taken orally starting on Day 6. (medeasy.health)
  • This study was undertaken to explore the contribution of PDCs and type I IFNs to RA pathogenesis using various animal models of PDC depletion and to monitor the effect of localized PDC recruitment and activation on joint inflammation and bone damage. (cnrs.fr)
  • CONCLUSION: The therapeutic effects of imiquimod on joint inflammation and bone destruction are dependent on TLR-7 sensing by PDCs and type I IFN signaling. (cnrs.fr)
  • Bacterial internalization into HeLa cells and macrophages and co-localization with either late endosomes or lysosomes of znuA mutant were not different from those of wild-type strain. (go.jp)
  • Cyclic GMP was able to mimic the antiproliferative effect of SNP on HEK293 cells. (scirp.org)
  • In the liver, choroid plexus, prostatic acinar cells, and the GIT, MRP4 is expressed at the basolateral membrane, while in the brain capillary endothelium and renal proximal tubule cells it is expressed at the apical membrane [2-6]. (solvobiotech.com)
  • OBJECTIVE: The role of plasmacytoid dendritic cells (PDCs) and type I interferons (IFNs) in rheumatoid arthritis (RA) remains a subject of controversy. (cnrs.fr)
  • advance online publication 13 Nov CliniCal PHarMaCOlOGy & THeraPeuTiCs VOLUME 95 NUMBER 1 JANUARy 2014 state art however, the overall rates of overweight adults and children SAFETY ISSUES WITH WEIGHT-LOSS DRUGS remain stubbornly large.7 Drugs can be very effective in inducing weight loss. (eddoctor24h.com)
  • 6. Hellman B, Jacobsson L & T ljedal I-B: Endocrine activity of the testis in obese-hyperglycemic mice. (taljedal.se)
  • Clopidogrel use is associated with an increased risk of bleeding and may cause haematological adverse effects, such as thrombotic thrombocytopenic purpura, haemolytic uremic syndrome, and bone-marrow suppression, manifesting with aplastic anaemia, thrombocytopenia [ 5 ], and neutropenia [ 6 , 7 ]. (hindawi.com)
  • [6] caffeine paralyzes and kills certain insects feeding upon the plant. (wikidoc.org)
  • 6-Shogaol alone inhibited Ras homolog gene family member A activation. (nih.gov)
  • This effect on IL-6 is consistent with the fact that PDE11A deletion increased microglia activation, although it left astrocytes unchanged. (frontiersin.org)
  • Omics data suggested intravenous administration of MSNs perturbed the following metabolites: succinate, hypoxanthine, GSSG, NADP+, NADPH and 6-phosphogluconic acid. (frontiersin.org)