• 7] Ghiadoni L, Versari D, Taddei S. Phosphodiesterase 5 inhibition in essential hypertension. (degruyter.com)
  • Here we address for the first time preclinical topics crucial for translation, most importantly 1) the comparison of 2 long-term PLX5622 applications (prevention and treatment) vs. 1 treatment alone, 2) the correlation of catatonic signs and executive dysfunction, 3) the phenotype of leftover microglia evading depletion, and 4) the role of intercellular interactions for efficient CSF1R inhibition. (mpg.de)
  • Importantly, 2 extended rounds of CSF1R inhibition are not superior to 1 treatment regarding any readout investigated (magnetic resonance imaging and magnetic resonance spectroscopy, behavior, immunohistochemistry). (mpg.de)
  • Woolson, H. D. , Thomson, V. S. , Rutherford, C. , Yarwood, S. J. and Palmer, T. M. (2009) Selective inhibition of cytokine-activated extracellular signal-regulated kinase by cyclic amp via Epac1-dependent induction of suppressor of cytokine signalling-3. (gla.ac.uk)
  • The inhibitory effect of cAMP could not be reversed by inhibition of cAMP-dependent protein kinase (PKA) but was blocked by depletion of the alternative intracellular cAMP sensor exchange protein activated by cAMP 1 (Epac1), which is also required to observe SOCS-3 accumulation in response to cAMP. (gla.ac.uk)
  • Together, these observations suggest that while SOCS-3 induction and subsequent inhibition of cytokine-mediated phosphorylation of ERK1,2 and STAT3 in response to cAMP require Epac1 and a transient PKA-independent activation of the ERK pathway, these two events are controlled by distinct mechanisms. (gla.ac.uk)
  • 2′,3′-Cyclic-nucleotide 3'-phosphodiesterase (EC 3.1.4.37, CNPase, systematic name nucleoside-2′,3′-cyclic-phosphate 2′-nucleotidohydrolase) is an enzyme that in humans is encoded by the CNP gene. (wikipedia.org)
  • CNPase catalyzes the following reaction: nucleoside 2′,3′-cyclic phosphate + H2O ⇌ {\displaystyle \rightleftharpoons } nucleoside 2′-phosphate CNPase is a myelin-associated enzyme that makes up 4% of total CNS myelin protein, and is thought to undergo significant age-associated changes. (wikipedia.org)
  • Nucleoside-2',3'-cyclic phosphate nucleotidohydrolase. (rush.edu)
  • Enzymes that catalyze the hydrolysis of the 2'- or 3'- phosphate bonds of 2',3'-cyclic nucleotides. (rush.edu)
  • 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)
  • Cyclic nucleotide phosphodiesterases: pharmacology, biochemistry and function. (urologi.or.id)
  • 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)
  • J Cell Biol (2001) 155 (2): 271-278. (rupress.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)
  • The interaction with the non-selective PDE (cyclic nucleotide phosphodiesterase) inhibitor 3-isobutyl-1-methylxanthine (IBMX) was tested after three days. (scirp.org)
  • 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)
  • Eli Lilly, Indianapolis, IN, USA), both of which are phosphodiesterase-5 (PDE5) inhibitors, are currently in Phase III clinical trials and could prove more potent, and produce fewer side effects, than sildenafil. (health.am)
  • It is named for its ability to catalyze the phosphodiester hydrolysis of 2',3'-cyclic nucleotides to 2'-nucleotides, though a cohesive understanding of its specific physiologic functions are still ambiguous. (wikipedia.org)
  • The more frequent side effects of sildenafil, such as facial flushing, headache, nasal congestion and dyspepsia [3], have been assumed to be caused by vasodilation produced as a consequence of blocking PDE5 in other areas of the body. (health.am)
  • Schwann Cells Metabolize Extracellular 2',3'-cAMP to 2'-AMP. (antikoerper-online.de)
  • A combination of outlier and cluster analyses identified putative new members of the PhoP regulon, namely, yfkN (2′,3′ cyclic nucleotide 2′-phosphodiesterase), yurI (RNase), yjdB (unknown), and vpr (extracellular serine protease). (sunderland.ac.uk)
  • The inhibitory effects of cAMP on sIL-6Ra/IL-6-stimulated phosphorylation of ERK1,2 and STAT3 were abolished by either short interfering (si) RNA-mediated knockdown or genetic ablation of suppressor of cytokine signalling-3 (SOCS-3). (gla.ac.uk)
  • Furthermore, this increase in cGMP degradation is paralleled by the phosphorylation of phosphodiesterase type 5 at Ser-92. (rupress.org)
  • Thus, our data suggest that NO-induced desensitization of the cGMP response is caused by the phosphorylation and subsequent activity increase of phosphodiesterase type 5. (rupress.org)
  • They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. (axonmedchem.com)
  • We therefore immunized young female Cnp −/− mice lacking the structural myelin protein 2′-3′-cyclic nucleotide 3′-phosphodiesterase (Cnp) with a "cocktail" of NMDAR1 peptides. (nature.com)
  • Reduced expression of 2′-3′-cyclic nucleotide 3′-phosphodiesterase (Cnp) in humans and mice causes white matter inflammation and catatonic signs. (mpg.de)
  • Most of the effects of the signaling molecule nitric oxide (NO) are mediated by cGMP, which is synthesized by soluble guanylyl cyclase and degraded by phosphodiesterases. (rupress.org)
  • Using a mouse model of genetic copper misregulation, in combination with pharmacological alterations in copper status and imaging studies in a 3T3-L1 white adipocyte model, we found that copper regulates lipolysis at the level of the second messenger, cyclic AMP (cAMP), by altering the activity of the cAMP-degrading phosphodiesterase PDE3B. (nih.gov)
  • The effects of 3, 3', 4, 4', 5-pentachlorobiphenyl (PCB-126), which is the most toxic congener of coplanar polychlorinated biphenyls (Co-PCBs), on intracellular accumulation and transepithelial transport of vinblastine were examined in porcine kidney cells, LLC-PK1, and its transformant cells expressing human P-glycoprotein (LLC-MDR1). (go.jp)
  • Exosomal 2',3'-CNP from mesenchymal stem cells promotes hippocampus CA1 neurogenesis/neuritogenesis and contributes to rescue of cognition/learning deficiencies of damaged brain. (antikoerper-online.de)
  • Blood tests revealed severe leukopenia (white cells 1 × 10 3 / μ L) with marked neutropenia (neutrophils 3%), anaemia (haemoglobin 9.9 g/dL), and an important rise in inflammatory markers (C-reactive protein 122 mg/dL). (hindawi.com)
  • Cyclic GMP was able to mimic the antiproliferative effect of SNP on HEK293 cells. (scirp.org)
  • Here we demonstrate that elevation of cyclic AMP (cAMP) levels in human umbilical vein endothelial cells (HUVECs) specifically attenuates ERK1,2 activation in response to either leptin or a soluble interleukin IL-6 receptor-α/IL-6 (sIL-6R-α/IL-6) trans-signalling complex but not protein kinase C activator phorbol 12-myristate 13-acetate. (gla.ac.uk)
  • Considerably higher resistance against cyclic nucleotide phosphodiesterases compared to dibutyryl- or 8-Br-cAMP (Cat. (biolog.de)
  • We have identified neuron-glia antigen 2 (NG2) as a unique molecular marker of S100β+ PSCs in skeletal muscle. (elifesciences.org)
  • 1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. (axonmedchem.com)
  • The proposed mechanism of CNPases phosphodiesterase catalytic activity is similar to the second step of the reaction mechanism for RNase A. CNPase is expressed exclusively by oligodendrocytes in the CNS, and the appearance of CNPase seems to be one of the earliest events of oligodendrocyte differentiation. (wikipedia.org)
  • YurI is thought to be responsible for the nonspecific degradation of RNA, while the activity of YfkN on various nucleotide phosphates suggests that it could act on substrates liberated by YurI, which produces 3′ or 5′ phosphoribonucleotides. (sunderland.ac.uk)
  • However, when intact platelets were incubated with NO and then lysed, enhanced activity of phosphodiesterase type 5 was detected in the cytosol. (rupress.org)
  • This study was designed to investigate the effects of Hunteria umbellata (HU) seeds and Cylicodiscus gabunensis (CG) stem barks aqueous extracts on key enzymes relevant to erectile dysfunction (phosphodiesterase-5 and arginase) and type-2 diabetes (α-amylase and α-glucosidase). (degruyter.com)
  • In ascertaining the erectogenic and antidiabetic properties of the extracts, the effects of the extracts on activities of some enzymes relevant to erectile dysfunction (arginase and phosphodiesterase-5) and type-2 diabetes (α-amylase and α-glucosidase) were determined. (degruyter.com)
  • The ability of samples' extract to inhibit some of key enzymes relevant to erectile dysfunction and type-2 diabetes could render them cheap, natural and alternative therapy with erectogenic and antidiabetic potentials. (degruyter.com)
  • 2016 Jul 2;11(7):482-8. (lu.se)
  • Cyclic nucleotide phosphodiesterases: relating structure and function. (degruyter.com)
  • 2011) c 0.86 2.08 2:1 HR 8799 e 7-10 14.5 Goździewski and Migaszewski Glutamate dehydrogenase (2009), Marois et al. (survivinpathway.com)
  • Catalpol Protects Pre-Myelinating Oligodendrocytes against Ischemia-induced Oxidative Injury through ERK1/2 Signaling Pathway. (antikoerper-online.de)
  • However, siRNA depletion and immunoblotting experiments revealed that neither Epac1 nor Epac2 contributed to the PKA-independent activation of ERK1,2 observed following cAMP elevation. (gla.ac.uk)
  • Clopidogrel exerts its antiplatelet effect by inhibiting the binding of adenosine diphosphate (ADP) to its receptor (P2Y12) and consequent ADP-mediated platelet activation [ 3 ]. (hindawi.com)
  • A Syntenic Cross Species Aneuploidy Genetic Screen Links RCAN1 Expression to β-Cell Mitochondrial Dysfunction in Type 2 Diabetes. (lu.se)
  • Moreover, this dose is 5-10 times higher than the dose necessary to stimulate the caudate nucleus (extrapyramidal motor system) and the neural structures regulating the sleep-wake cycle, the 2 functions that are most sensitive to caffeine. (medscape.com)
  • 2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. (axonmedchem.com)
  • 2',3'-Cyclic-Nucleotide Phosphodiesterases" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (rush.edu)
  • The levels of mRNAs were (1) down‐regulated to basal levels (PO and MBP mRNAs), (2) down‐regulated to undetectable levels (myelin‐associated glycoprotein mRNAs), (3) upregulated (mRNAs encoding 2′3′‐cyclic nucleotide phosphodiesterase and β‐actin), or (4) not stringently controlled by the removal of Schwann cell‐axonal contact (proteolipid protein mRNAs). (elsevierpure.com)
  • Arterial blood gas levels (through an indwelling line [eg, umbilical arterial catheter or preductal peripheral arterial line]): To assess the pH, partial pressure of carbon dioxide (PaCO 2 ) and the partial pressure of oxygen (PaO 2 ) which might be higher in the preductal arterial line. (medscape.com)