Cyclic Nucleotide Phosphodiesterases, Type 1
A CALCIUM and CALMODULIN-dependent cyclic nucleotide phosphodiesterase subfamily. The three members of this family are referred to as type 1A, type 1B, and type 1C and are each product of a distinct gene. In addition, multiple enzyme variants of each subtype can be produced due to multiple alternative mRNA splicing. Although the type 1 enzymes are classified as 3',5'-cyclic-AMP phosphodiesterases (EC 3.1.4.17), some members of this class have additional specificity for CYCLIC GMP.
3',5'-Cyclic-AMP Phosphodiesterases
Enzymes that catalyze the hydrolysis of CYCLIC AMP to form adenosine 5'-phosphate. The enzymes are widely distributed in animal tissue and control the level of intracellular cyclic AMP. Many specific enzymes classified under this heading demonstrate additional spcificity for 3',5'-cyclic IMP and CYCLIC GMP.
Cyclic Nucleotide Phosphodiesterases, Type 4
A cyclic nucleotide phosphodiesterase subfamily that is found predominantly in inflammatory cells and may play a role in the regulation of CELL-MEDIATED IMMUNITY. The enzyme family includes over twenty different variants that occur due to multiple ALTERNATIVE SPLICING of the mRNA of at least four different genes.
Cyclic Nucleotide Phosphodiesterases, Type 3
A cyclic nucleotide phosphodiesterase subfamily that is inhibited by the binding of CYCLIC GMP to an allosteric domain found on the enzyme and through phosphorylation by regulatory kinases such as PROTEIN KINASE A and PROTEIN KINASE B. The two members of this family are referred to as type 3A, and type 3B, and are each product of a distinct gene. In addition multiple enzyme variants of each subtype can be produced due to multiple alternative mRNA splicing.
Cyclic Nucleotide Phosphodiesterases, Type 2
A cyclic nucleotide phosphodiesterase subfamily that is activated by the binding of CYCLIC GMP to an allosteric domain found on the enzyme. Multiple enzyme variants of this subtype can be produced due to multiple alternative mRNA splicing. The subfamily is expressed in a broad variety of tissues and may play a role in mediating cross-talk between CYCLIC GMP and CYCLIC CMP pathways. Although the type 2 enzymes are classified as 3',5'-cyclic-AMP phosphodiesterases (EC 3.1.4.17), members of this class have additional specificity for CYCLIC GMP.
Phosphoric Diester Hydrolases
2',3'-Cyclic-Nucleotide Phosphodiesterases
Phosphodiesterase Inhibitors
3',5'-Cyclic-GMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 5
Cyclic GMP
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
Cyclic Nucleotide Phosphodiesterases, Type 7
Cyclic AMP
1-Methyl-3-isobutylxanthine
Isoenzymes
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Calmodulin
A heat-stable, low-molecular-weight activator protein found mainly in the brain and heart. The binding of calcium ions to this protein allows this protein to bind to cyclic nucleotide phosphodiesterases and to adenyl cyclase with subsequent activation. Thereby this protein modulates cyclic AMP and cyclic GMP levels.
Amino Acid Sequence
Cyclic Nucleotide Phosphodiesterases, Type 6
A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. It is found predominantly in the outer segment PHOTORECEPTOR CELLS of the RETINA. It is comprised of two catalytic subunits, referred to as alpha and beta, that form a dimer. In addition two regulatory subunits, referred to as gamma and delta, modulate the activity and localization of the enzyme.
Nucleotides
Dibutyryl Cyclic GMP
Theophylline
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
Phosphodiesterase I
Cyclic Nucleotide-Gated Cation Channels
Phosphorus-Oxygen Lyases
Milrinone
Bucladesine
Pyrrolidinones
Cyclic AMP-Dependent Protein Kinases
Cyclic GMP-Dependent Protein Kinases
Adenylate Cyclase
Second Messenger Systems
Systems in which an intracellular signal is generated in response to an intercellular primary messenger such as a hormone or neurotransmitter. They are intermediate signals in cellular processes such as metabolism, secretion, contraction, phototransduction, and cell growth. Examples of second messenger systems are the adenyl cyclase-cyclic AMP system, the phosphatidylinositol diphosphate-inositol triphosphate system, and the cyclic GMP system.
Papaverine
An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.
Cyclic IMP
Base Sequence
Colforsin
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
Guanylate Cyclase
Cloning, Molecular
Polymorphism, Single Nucleotide
8-Bromo Cyclic Adenosine Monophosphate
Calcium
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Cattle
Isoproterenol
Binding Sites
Catalytic Domain
Signal Transduction
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Vinca Alkaloids
Enzyme Activation
Substrate Specificity
IL-3 and IL-4 activate cyclic nucleotide phosphodiesterases 3 (PDE3) and 4 (PDE4) by different mechanisms in FDCP2 myeloid cells. (1/326)
In FDCP2 myeloid cells, IL-4 activated cyclic nucleotide phosphodiesterases PDE3 and PDE4, whereas IL-3, granulocyte-macrophage CSF (GM-CSF), and phorbol ester (PMA) selectively activated PDE4. IL-4 (not IL-3 or GM-CSF) induced tyrosine phosphorylation of insulin-receptor substrate-2 (IRS-2) and its association with phosphatidylinositol 3-kinase (PI3-K). TNF-alpha, AG-490 (Janus kinase inhibitor), and wortmannin (PI3-K inhibitor) inhibited activation of PDE3 and PDE4 by IL-4. TNF-alpha also blocked IL-4-induced tyrosine phosphorylation of IRS-2, but not of STAT6. AG-490 and wortmannin, not TNF-alpha, inhibited activation of PDE4 by IL-3. These results suggested that IL-4-induced activation of PDE3 and PDE4 was downstream of IRS-2/PI3-K, not STAT6, and that inhibition of tyrosine phosphorylation of IRS molecules might be one mechnism whereby TNF-alpha could selectively regulate activities of cytokines that utilized IRS proteins as signal transducers. RO31-7549 (protein kinase C (PKC) inhibitor) inhibited activation of PDE4 by PMA. IL-4, IL-3, and GM-CSF activated mitogen-activated protein (MAP) kinase and protein kinase B via PI3-K signals; PMA activated only MAP kinase via PKC signals. The MAP kinase kinase (MEK-1) inhibitor PD98059 inhibited IL-4-, IL-3-, and PMA-induced activation of MAP kinase and PDE4, but not IL-4-induced activation of PDE3. In FDCP2 cells transfected with constitutively activated MEK, MAP kinase and PDE4, not PDE3, were activated. Thus, in FDCP2 cells, PDE4 can be activated by overlapping MAP kinase-dependent pathways involving PI3-K (IL-4, IL-3, GM-CSF) or PKC (PMA), but selective activation of PDE3 by IL-4 is MAP kinase independent (but perhaps IRS-2/PI3-K dependent). (+info)Characterization of the cyclic nucleotide phosphodiesterase subtypes involved in the regulation of the L-type Ca2+ current in rat ventricular myocytes. (2/326)
The effects of several phosphodiesterase (PDE) inhibitors on the L-type Ca current (I(Ca)) and intracellular cyclic AMP concentration ([cAMP]i) were examined in isolated rat ventricular myocytes. The presence of mRNA transcripts encoding for the different cardiac PDE subtypes was confirmed by RT-PCR. IBMX (100 microM), a broad-spectrum PDE inhibitor, increased basal I(Ca) by 120% and [cAMP]i by 70%, similarly to a saturating concentration of the beta-adrenoceptor agonist isoprenaline (1 microM). However, MIMX (1 microM), a PDE1 inhibitor, EHNA (10 microM), a PDE2 inhibitor, cilostamide (0.1 microM), a PDE3 inhibitor, or Ro20-1724 (0.1 microM), a PDE4 inhibitor, had no effect on basal I(Ca) and little stimulatory effects on [cAMP]i (20-30%). Each selective PDE inhibitor was then tested in the presence of another inhibitor to examine whether a concomitant inhibition of two PDE subtypes had any effect on I(Ca) or [cAMP]i. While all combinations tested significantly increased [cAMP]i (40-50%), only cilostamide (0.1 microM)+ Ro20-1724 (0.1 microM) produced a significant stimulation of I(Ca) (50%). Addition of EHNA (10 microM) to this mix increased I(Ca) to 110% and [cAMP]i to 70% above basal, i.e. to similar levels as obtained with IBMX (100 microM) or isoprenaline (1 microM). When tested on top of a sub-maximal concentration of isoprenaline (1 nM), which increased I(Ca) by (approximately 40% and had negligible effect on [cAMP]i, each selective PDE inhibitor induced a clear stimulation of [cAMP]i and an additional increase in I(Ca). Maximal effects on I(Ca) were approximately 8% for MIMX (3 microM), approximately 20% for EHNA (1-3 microM), approximately 30% for cilostamide (0.3-1 microM) and approximately 50% for Ro20-1724 (0.1 microM). Our results demonstrate that PDE1-4 subtypes regulate I(Ca) in rat ventricular myocytes. While PDE3 and PDE4 are the dominant PDE subtypes involved in the regulation of basal I(Ca), all four PDE subtypes determine the response of I(Ca) to a stimulus activating cyclic AMP production, with the rank order of potency PDE4>PDE3>PDE2>PDE1. (+info)Mechanisms involved in the regulation of free fatty acid release from isolated human fat cells by acylation-stimulating protein and insulin. (3/326)
The effects of acylation-stimulating protein (ASP) and insulin on free fatty acid (FFA) release from isolated human fat cells and the signal transduction pathways to induce these effects were studied. ASP and insulin inhibited basal and norepinephrine-induced FFA release by stimulating fractional FFA re-esterification (both to the same extent) and by inhibiting FFA produced during lipolysis (ASP to a lesser extent than insulin). Protein kinase C inhibition influenced none of the effects of ASP or insulin. Phosphatidylinositol 3-kinase inhibition counteracted the effects of insulin but not of ASP. Phosphodiesterase 3 (PDE3) activity was stimulated by ASP and insulin, whereas PDE4 activity was slightly increased by ASP only. Selective PDE3 inhibition reversed the effects of both ASP and insulin on fractional FFA re-esterification and lipolysis. Selective PDE4 inhibition slightly counteracted the ASP but not the effect of insulin on fractional FFA re-esterification and did not prevent the action of ASP or insulin on lipolysis. Thus, ASP and insulin play a major role in regulating FFA release from fat cells as follows: insulin by stimulating fractional FFA re-esterification and inhibiting lipolysis and ASP mainly by stimulating fractional FFA re-esterification. For both ASP and insulin these effects on FFA release are mediated by PDE3, and for ASP PDE4 might also be involved. The signaling pathway preceding PDE is not known for ASP but involves phosphatidylinositol 3-kinase for insulin. (+info)Inhibition of phosphodiesterase III with milrinone increases renin secretion in human subjects. (4/326)
One of the major signaling molecules involved in the regulation of renin secretion is cyclic AMP (cAMP). The concentration of cAMP in cells is determined in part by the rate of cAMP hydrolysis by several families of phosphodiesterases, especially the phosphodiesterase III family, but little is known about the roles of these enzymes in the control of renin secretion, particularly in humans. The aim of the present study was to investigate the effect of the phosphodiesterase III inhibitor milrinone on renin secretion in human subjects. Milrinone was infused i.v. in eight healthy normotensive subjects in a dose of 100 microgram/kg. Immediately after the infusion, there was a transient increase in systolic pressure from 107 +/- 5 to 116 +/- 5 mm Hg (p <.01), but no significant change in diastolic or mean arterial pressure. Heart rate increased from 67 +/- 2 to 86 +/- 4 beats/min (p <.01) and remained elevated. Plasma renin activity increased in all subjects, the mean value increasing from 3.0 +/- 0.5 to 6.0 +/- 1.1 ng/ml/h at 15 min (p <.01). These results demonstrate that milrinone increases renin secretion in human subjects, thus providing evidence that phosphodiesterase III family participates in the control of renin secretion in humans. The increase in renin secretion does not appear to be mediated by major mechanisms that control renin secretion, and likely results from an increase in cAMP concentration in the juxtaglomerular cells. (+info)Phosphorylation and activation of phosphodiesterase type 3B (PDE3B) in adipocytes in response to serine/threonine phosphatase inhibitors: deactivation of PDE3B in vitro by protein phosphatase type 2A. (5/326)
Phosphodiesterase type 3B (PDE3B) has been shown to be activated and phosphorylated in response to insulin and hormones that increase cAMP. In order to study serine/threonine protein phosphatases involved in the regulation of rat adipocyte PDE3B, we investigated the phosphorylation and activation of PDE3B in vivo in response to phosphatase inhibitors and the dephosphorylation and deactivation of PDE3B in vitro by phosphatases purified from rat adipocyte homogenates. Okadaic acid and calyculin A induced dose- and time-dependent activation of PDE3B. Maximal effects were obtained after 30 min using 1 microM okadaic acid (1.8-fold activation) and 300 nM calyculin A (4-fold activation), respectively. Tautomycin and cyclosporin A did not induce activation of PDE3B. Incubation of adipocytes with 300 nM calyculin A inhibited protein phosphatase (PP) 1 and PP2A completely. Okadaic acid (1 microM) reduced PP2A activity by approx. 50% but did not affect PP1 activity, and 1 microM tautomycin reduced PP1 activity by approx. 60% but PP2A activity by only 11%. This indicates an important role for PP2A in the regulation of PDE3B. Furthermore, rat adipocyte PDE3B phosphatase activity co-purified with PP2A but not with PP1 during MonoQ chromatography. As compared with insulin, okadaic acid and calyculin A induced phosphorylation of PDE3B by 2.8- and 14-fold respectively, whereas tautomycin and cyclosporin A had no effect. Both calyculin A and okadaic acid induced phosphorylation on serine 302, the site known to be phosphorylated on PDE3B in response to insulin and isoproterenol (isoprenaline), as well as on sites not identified previously. In summary, PP2A seems to be involved in the regulation of PDE3B in vivo and can act as a PDE3B phosphatase in vitro. In comparison with insulin, calyculin A induced a dramatic activation of PDE3B and both calyculin A and okadaic acid induced phosphorylation on additional sites, which could have a role in signalling pathways not yet identified. (+info)Beta-adrenergic receptor agonists and cyclic nucleotide phosphodiesterase inhibitors: shifting the focus from inotropy to cyclic adenosine monophosphate. (6/326)
Clinical trials of beta-adrenergic receptor agonists and cyclic nucleotide phosphodiesterase inhibitors in heart failure have demonstrated a reduction in survival in treated patients despite initial inotropic responses. These findings have led many to infer that activation of the mechanisms through which contractility is increased has deleterious effects on failing myocardium. It should be remembered, however, that these agents act proximately by raising intracellular cyclic adenosine monophosphate (cAMP) content and stimulating protein phosphorylation by cAMP-dependent protein kinase, and that the proteins whose phosphorylation contributes to the inotropic responses may be different from the proteins whose phosphorylation contributes to the reduction in survival. Evidence in support of the latter interpretation is presented, and potential therapeutic approaches through which the phosphorylation of different proteins might be selectively affected are considered. (+info)(-)-Enantiomer EMD 57439 antagonizes the Ca2+ sensitizing effect of (+)-enantiomer EMD 57033 on diastolic function but not on systolic function in rabbit ventricular cardiomyocytes. (7/326)
EMD 53998 (5-[1-(3,4-dimethoxybenzoyl)-1,2,3,4-tetrahydro-6-quinolyl]-6-meth yl-3,6-dihydro-2H-1,3,4-thiadiazin-2-one), the racemic mixture of (+)-enantiomer EMD 57033 and (-)-enantiomer EMD 57439, is a prototype of Ca2+ sensitizers that act via a central and/or down-stream mechanism in cardiac E-C coupling. In rabbit ventricular cardiomyocytes loaded with indo-1/AM, EMD 53998 and EMD 57033 shifted the relationship between Ca2+ transients and cell shortening (systolic function) to the left to the same extent as compared with that of elevation of [Ca2+]o. EMD 57439 did not elicit a positive inotropic effect (PIE). The PIE of EMD 57033 was associated with a more pronounced decrease in the diastolic cell length than that of EMD 53998, whereas the systolic effects of these compounds were equivalent. These results indicate that weak phosphodiesterase (PDE) III inhibition may exert a differential action on diastolic and systolic function. Thus, EMD 57439 antagonizes the Ca2+-sensitizing effect of EMD 57033 on diastolic function with no effect on systolic function, which may lead to a decrease in diastolic cell length of a lesser extent with the racemate EMD 53998 compared with (+)-enantiomer EMD 57033. (+info)Insulin-induced phosphorylation and activation of cyclic nucleotide phosphodiesterase 3B by the serine-threonine kinase Akt. (8/326)
Cyclic nucleotide phosphodiesterase (PDE) is an important regulator of the cellular concentrations of the second messengers cyclic AMP (cAMP) and cGMP. Insulin activates the 3B isoform of PDE in adipocytes in a phosphoinositide 3-kinase-dependent manner; however, downstream effectors that mediate signaling to PDE3B remain unknown. Insulin-induced phosphorylation and activation of endogenous or recombinant PDE3B in 3T3-L1 adipocytes have now been shown to be inhibited by a dominant-negative mutant of the serine-threonine kinase Akt, suggesting that Akt is necessary for insulin-induced phosphorylation and activation of PDE3B. Serine-273 of mouse PDE3B is located within a motif (RXRXXS) that is preferentially phosphorylated by Akt. A mutant PDE3B in which serine-273 was replaced by alanine was not phosphorylated either in response to insulin in intact cells or by purified Akt in vitro. In contrast, PDE3B mutants in which alanine was substituted for either serine-296 or serine-421, each of which lies within a sequence (RRXS) preferentially phosphorylated by cAMP-dependent protein kinase, were phosphorylated by Akt in vitro or in response to insulin in intact cells. Moreover, the serine-273 mutant of PDE3B was not activated by insulin when expressed in adipocytes. These results suggest that PDE3B is a physiological substrate of Akt and that Akt-mediated phosphorylation of PDE3B on serine-273 is important for insulin-induced activation of PDE3B. (+info)
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Oligodendrocyte
... phosphodiesterase (CNPase) List of human cell types derived from the germ layers Carlson, Neil (2010). Physiology of Behavior. ... Cyclic-nucleotide 3'- ... Oligodendrocytes are a type of glial cell. They arise during ... They are the last cell type to be generated in the CNS. Oligodendrocytes were discovered by Pío del Río Hortega. ... Oligodendrocytes (from Greek 'cells with a few branches'), or oligodendroglia, are a type of neuroglia whose main functions are ...
Neuronal calcium sensor-1
... cyclic nucleotide phosphodiesterases ARF1 (ADP Ribosylation factor 1) A type (Kv4.3; Shal-related subfamily, member 3) voltage- ... The designation 'NCS-1' came from the assumption that the protein was expressed only in neuronal cell types, which is not the ... type III phosphatidylinositol 4-kinase β) IP3 receptor (this activity is inhibited by lithium - a drug used for the treatment ... 8 (3): 182-193. doi:10.1038/nrn2093. PMC 1887812. PMID 17311005. Burgoyne RD, O'Callaghan DW, Hasdemir B, Haynes LP, Tepikin AV ...
EHNA
"Isozyme selective inhibition of cGMP-stimulated cyclic nucleotide phosphodiesterases by erythro-9-(2-hydroxy-3-nonyl) adenine ... which also acts as a phosphodiesterase inhibitor that selectively inhibits phosphodiesterase type 2 (PDE2). "Sigma Aldrich". ... adenine inhibits cyclic GMP-stimulated phosphodiesterase in isolated cardiac myocytes". Molecular Pharmacology. 48 (1): 121-30 ... Méry PF, Pavoine C, Pecker F, Fischmeister R (July 1995). "Erythro-9-(2-hydroxy-3-nonyl) ...
Oligodendrocyte
Cyclic-nucleotide 3'-phosphodiesterase (CNPase). *List of human cell types derived from the germ layers ... Oligodendrocytes are a type of glial cell. They arise during development from oligodendrocyte precursor cells (OPCs),[7] which ... Oligodendrocytes (from Greek 'cells with a few branches'), or oligodendroglia, are a type of neuroglia whose main functions are ... Precursors and both mature types are typically identified by their expression of the transcription factor OLIG2.[10] ...
PDE1C
2007). "Cyclic nucleotide phosphodiesterase PDE1C1 in human cardiac myocytes". J. Biol. Chem. 282 (45): 32749-57. doi:10.1074/ ... 2006). "Subcellular localization and regulation of type-1C and type-5 phosphodiesterases". Biochem. Biophys. Res. Commun. 341 ( ... Rybalkin SD, Rybalkina I, Beavo JA, Bornfeldt KE (2002). "Cyclic nucleotide phosphodiesterase 1C promotes human arterial smooth ... cyclic nucleotide phosphodiesterase 1C is an enzyme that in humans is encoded by the PDE1C gene. GRCh38: Ensembl release 89: ...
P19 cell
Cyclic-nucleotide 3'-phosphodiesterase. Moreover, oligodendrocytes also developed and migrated into fiber bundles in mice when ... The cell line is pluripotent and can differentiate into cell types of all three germ layers. Also, it is the most characterized ... At concentration of 0.5-1% DMSO induced P19 cells to aggregate and process mesodermal and endodermal cell types. The cellular ... 560 (1-3): 192-8. doi:10.1016/S0014-5793(04)00086-9. PMID 14988021. Tan, Y; Xie, Z; Ding, M; Wang, Z; Yu, Q; Meng, L; Zhu, H; ...
CNP
Cyclic-nucleotide 3'-phosphodiesterase, a myelin-associated enzyme that makes up 4% of total CNS myelin protein Chronic ... nonbacterial prostatitis, a pelvic pain condition affecting men c-type Natriuretic Peptide, a vasoactive hormone Certified ...
3',5'-Ciklični-AMP fosfodiestaraza
Johner, A., Kunz, S., Linder, M., Shakur, Y. and Seebeck, T. (2006). "Cyclic nucleotide specific phosphodiesterases of ... http://www.garlandscience.com/textbooks/0815323042.asp?type=reviews. *Irwin H. Segel. Enzyme Kinetics: Behavior and Analysis of ... B enzm: 1.1/2/3/4/5/6/7/8/10/11/13/14/15-18, 2.1/2/3/4/5/6/7/8, 2.7.10, 2.7.11-12, 3.1/2/3/4/5/6/7, 3.1.3.48, 3.4.21/22/23/24, ... B enzm: 1.1/2/3/4/5/6/7/8/10/11/13/14/15-18, 2.1/2/3/4/5/6/7/8, 2.7.10, 2.7.11-12, 3.1/2/3/4/5/6/7, 3.1.3.48, 3.4.21/22/23/24, ...
Phosphodiesterase 3
September 2003). "Cyclic nucleotide phosphodiesterase activity, expression, and targeting in cells of the cardiovascular system ... PDE3A can be either membrane-associated or cytosolic, depending on the variant and the cell type it is expressed in. PDE3A and ... Lugnier C (March 2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific ... WO 03012030, Movsesian M, "Isoform-Selective Inhibitors and Activators of PDE3 Cyclic Nucleotide Phosphodiesterases", published ...
Cyclic nucleotide
Cyclic nucleotides can be found in many different types of eukaryotic cells, including photo-receptor rods and cones, smooth ... cAMP's role in this process terminates upon hydrolysis to AMP by phosphodiesterase. Cyclic nucleotides are well-suited to act ... The two most well-studied cyclic nucleotides are cyclic AMP (cAMP) and cyclic GMP (cGMP), while cyclic CMP (cCMP) and cyclic ... A cyclic nucleotide (cNMP) is a single-phosphate nucleotide with a cyclic bond arrangement between the sugar and phosphate ...
Benjamin Weiss (scientist)
He is best known for his work with cyclic nucleotide phosphodiesterases. He was the first to propose, based on his experimental ... He showed that a single cell type may contain more than one form of phosphodiesterase [6,7] and that different forms of ... one on the potential therapeutic application of cyclic nucleotides: (Weiss, Benjamin, ed., Cyclic Nucleotides in Disease[1]), ... Cyclic Nucleotide Phosphodiesterases: Weiss and co-workers developed rapid phosphodiesterease assays [3, 4], separated ...
PDE4B
This gene is a member of the type IV, cyclic AMP (cAMP)-specific, cyclic nucleotide phosphodiesterase (PDE) family. Cyclic ... The cyclic nucleotide phosphodiesterases (PDEs) regulate the cellular concentrations of cyclic nucleotides and thereby play a ... "Pivotal role of cyclic nucleoside phosphodiesterase 4 in Tat-mediated CD4+ T cell hyperactivation and HIV type 1 replication". ... "Entrez Gene: PDE4B phosphodiesterase 4B, cAMP-specific (phosphodiesterase E4 dunce homolog, Drosophila)". Swerdlow, Neal R. ( ...
ABCC5
This export contributes to the degradation of phosphodiesterases and possibly an elimination pathway for cyclic nucleotides. ... "cDNA cloning of a short type of multidrug resistance protein homologue, SMRP, from a human lung cancer cell line". Biochemical ... This protein functions in the cellular export of its substrate, cyclic nucleotides. ... a transporter for cyclic nucleotides, in human placenta and cultured human trophoblasts: effects of gestational age and ...
CGMP-specific phosphodiesterase type 5
"Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Advances in Cyclic ... Fertel R, Weiss B (July 1976). "Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung" ( ... cGMP-specific phosphodiesterase type 5 is an enzyme (EC 3.1.4.17) from the phosphodiesterase class. It is found in various ... Weiss B, Hait WN (1977). "Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annual ...
PDE9A
1998). "Identification and characterization of a novel cyclic nucleotide phosphodiesterase gene (PDE9A) that maps to 21q22.3: ... "Identification and characterization of a new human type 9 cGMP-specific phosphodiesterase splice variant (PDE9A5). Differential ... cyclic phosphodiesterase 9A is an enzyme that in humans is encoded by the PDE9A gene. The protein encoded by this gene ... "Entrez Gene: PDE9A phosphodiesterase 9A". Verhoest PR, Fonseca KR, Hou X, et al. (2012). "Design and discovery of 6-[(3S,4S)-4- ...
Bucladesine
... is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor. ... The effect of bucladesine as a cAMP analog has been studied on the pentylenetetrazol-induced seizure in the wild-type mice. The ... Bucladesine (50-100nM/mouse) showed significant attenuation in the morphine withdrawal syndrome in the wild-type mice. In ... 670 (2-3): 464-70. doi:10.1016/j.ejphar.2011.09.026. PMID 21946102. Seyedi SY, Salehi F, Payandemehr B, Hossein S, Hosseini- ...
Myelin basic protein
Cyclic-nucleotide 3'-phosphodiesterase and multiple molecules of the Immune system. GRCh38: Ensembl release 89: ENSG00000197971 ... In general, the major form of MBP is a protein of about 18.5 Kd (170 residues). In melanocytic cell types, MBP gene expression ... 3: 96-9. doi:10.4024/18SH03R.jbpc.03.03. This article incorporates text from the United States National Library of Medicine, ... The Golli mRNAs contain 3 exons unique to Golli-MBP, spliced in-frame to 1 or more MBP exons. They encode hybrid proteins that ...
PDE6B
"Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... Journal of Cyclic Nucleotide Research. 2 (3): 139-48. PMID 6493. Keeler, CE (20 March 1928). "The Geotropic Reaction of Rodless ... "Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... cyclic phosphodiesterase subunit beta is the beta subunit of the protein complex PDE6 that is encoded by the PDE6B gene. PDE6 ...
Caffeine-induced anxiety disorder
Methylxanthines such as caffeine inhibit the action of cyclic nucleotide phosphodiesterase, which normally acts to break down ... Symptoms must also not have a more likely clinical cause, such as another type of anxiety disorder, come before the ingestion ... Cyclic adenosine monophosphate, or cAMP, is a second messenger important in many cellular processes and is a critical factor in ... Adenosine acts on A1 receptors to decrease opening of N-type Ca2+ channels in some hippocampal neurons, and therefore decrease ...
CGAS-STING cytosolic DNA sensing pathway
Sun L, Wu J, Du F, Chen X, Chen ZJ (February 2013). "Cyclic GMP-AMP synthase is a cytosolic DNA sensor that activates the type ... cGAMP was found to be much more potent than other cyclic di-nucleotides (c-di-GMP and c-di-AMP). cGAMP was shown to ... phosphodiesterases. Other advantages of the unique 2'-5' linkage may be that cGAMP is able to bind multiple allelic variants of ... Cyclic GMP-AMP (cGAMP) is a cyclic dinucleotide (CDN) and the first to be found in metazoans. Other CDNs (c-di-GMP and c-di-AMP ...
PDE4A
The protein encoded by this gene belongs to the cyclic nucleotide phosphodiesterase (PDE) family, and PDE4 subfamily. This PDE ... "Pivotal role of cyclic nucleoside phosphodiesterase 4 in Tat-mediated CD4+ T cell hyperactivation and HIV type 1 replication". ... Zhou L, Thompson WJ, Potter DE (Jul 1999). "Multiple cyclic nucleotide phosphodiesterases in human trabecular meshwork cells" ( ... of a human cytosolic type-IVA, cyclic AMP specific phosphodiesterase (hPDE-IVA-h6.1)". Cellular Signalling. 6 (7): 793-812. doi ...
Phosphodiesterase-4 inhibitor
"Functional and biochemical evidence for diazepam as a cyclic nucleotide phosphodiesterase type 4 inhibitor". British Journal of ... A phosphodiesterase type 4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action ... Barad M, Bourtchouladze R, Winder DG, Golan H, Kandel E (1998). "Rolipram, a type IV-specific phosphodiesterase inhibitor, ... Dinter, H (February 2000). "Phosphodiesterase type 4 inhibitors: potential in the treatment of multiple sclerosis?". BioDrugs. ...
Cyclic nucleotide phosphodiesterase
"Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... 3'5'-cyclic nucleotide phosphodiesterases are a family of phosphodiesterases. Generally, these enzymes hydrolyze some ... "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacological Reviews. 58 (3): 488-520. doi: ... nucleotide phosphodiesterase, cyclic 3',5'-phosphodiesterase, 3',5'-nucleotide phosphodiesterase, 3':5'-cyclic nucleotide 5'- ...
Phosphodiesterase
"Biochemistry and physiology of cyclic nucleotide phosphodiesterases: essential components in cyclic nucleotide signaling". ... Phosphodiesterase enzymes have been shown to be different in different types of cells, including normal and leukemic ... Usually, phosphodiesterase refers to cyclic nucleotide phosphodiesterases, which have great clinical significance and are ... "Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Advances in Cyclic ...
List of EC numbers (EC 3)
... cyclic-nucleotide phosphodiesterase EC 3.1.4.18: now EC 3.1.16.1 EC 3.1.4.19: now EC 3.1.13.3 EC 3.1.4.20: now EC 3.1.13.1 EC ... type I site-specific deoxyribonuclease EC 3.1.21.4: type II site-specific deoxyribonuclease EC 3.1.21.5: type III site-specific ... CMP-N-acylneuraminate phosphodiesterase EC 3.1.4.41: sphingomyelin phosphodiesterase D EC 3.1.4.42: glycerol-1,2-cyclic- ... glucose-1-phospho-D-mannosylglycoprotein phosphodiesterase EC 3.1.4.52: cyclic-guanylate-specific phosphodiesterase EC 3.1.4.53 ...
Pharmacology of antidepressants
... by adenylyl cyclase and metabolized by cyclic nucleotide phosphodiesterases (PDEs). One manifestation of depression is an ... 5-cyclic adenosine monophosphate (cAMP) system induced by different types of chronic but not acute antidepressant treatment, ... a type of glutamate receptor - produces rapid (within 2 hours), robust and sustained (lasting for up to a fortnight) ... "Interaction between the antidepressant-like behavioral effects of beta adrenergic agonists and the cyclic AMP PDE inhibitor ...
Phosphodiesterase inhibitor
2001). "Cyclic nucleotide phosphodiesterases". The Journal of Allergy and Clinical Immunology. 108 (5): 671-80. doi:10.1067/mai ... Jan 2012). "Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental ... Fertel R, Weiss B (1976). "Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung". Mol. ... Weiss B (1975). "Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Adv. ...
Paraxanthine
Essayan DM (November 2001). "Cyclic nucleotide phosphodiesterases". The Journal of Allergy and Clinical Immunology. 108 (5): ... Paraxanthine is a phosphodiesterase type 9 (PDE9) inhibitor and it is sold as a research molecule for this same purpose. ... Paraxanthine is a selective inhibitor of cGMP-preferring phosphodiesterase (PDE9) activity and is hypothesized to increase ... Paraxanthine is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits ...
Phosphodiesterase 2
"Biologic regulation through opposing influences of cyclic GMP and cyclic AMP: the Yin Yang hypothesis". Adv Cyclic Nucleotide ... As different PDE types may affect different cAMP pools, the different PDEs may regulate different processes in the cell. PDE2 ... June 1997). "cGMP-stimulated cyclic nucleotide phosphodiesterase regulates the basal calcium current in human atrial myocytes ... Bender AT, Beavo JA (September 2006). "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacol. ...
PDE1
Lugnier C (March 2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific ... PDE1 (phosphodiesterase type 1) is a phosphodiesterase enzyme also known as calcium- and calmodulin-dependent phosphodiesterase ... Kakkar R, Raju RV, Sharma RK (July 1999). "Calmodulin-dependent cyclic nucleotide phosphodiesterase (PDE1)". Cell. Mol. Life ... Bender AT, Beavo JA (September 2006). "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacol. ...
Photoreceptor cell
Unstimulated (in the dark), cyclic-nucleotide gated channels in the outer segment are open because cyclic GMP (cGMP) is bound ... One type of photosensitive pigment Three types of photosensitive pigment in humans ... Each transducin then activates the enzyme cGMP-specific phosphodiesterase (PDE).. *PDE then catalyzes the hydrolysis of cGMP to ... resulting in the closure of cyclic nucleotide-gated Na+ ion channels located in the photoreceptor outer segment membrane. ...
Retina
... resulting in the closing of Na+ cyclic nucleotide-gated ion channels (CNGs). Thus the cell is hyperpolarised. The amount of ... A third type of light-sensing cell, the photosensitive ganglion cell, is important for entrainment of circadian rhythms and ... This in turn causes the Ga-subunit of the protein to activate a phosphodiesterase (PDE6), which degrades cGMP, ... There are two types of centre-surround structures in the retina - on-centres and off-centres. On-centres have a positively ...
Hormone-sensitive lipase
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... LIPE, AOMS4, FPLD6, HSL, LHS, lipase E, hormone sensitive type. External IDs. OMIM: 151750 MGI: 96790 HomoloGene: 3912 ... which is necessary for lipid mobilization in response to cyclic AMP, which itself is provided by the activation of Gs protein- ... 130 (3): 697-705. PMC 1174508. PMID 4664927.. *^ de Meijer J (1998-05-01). "Hormone sensitive lipase: structure, function and ...
GNB1
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 is a protein that in humans is encoded by the GNB1 gene.[5] ... type 1 angiotensin receptor binding. • protein complex binding. • signal transducer activity. • protein binding. • GTPase ... alkylglycerophosphoethanolamine phosphodiesterase activity. • macromolecular complex binding. Cellular component. • ... retina development in camera-type eye. • Ras protein signal transduction. • cell proliferation. • cellular response to hypoxia ...
Glucose 6-phosphatase
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... The third type of glucose 6-phosphatase deficiency, glucose 6-phosphatase-β deficiency, is characterized by a congenital ... 1993). "Glycogen Storage Disease Type I". PMID 20301489.. Cite journal requires ,journal=. (help). ... Chou JY, Matern D, Mansfield BC, Chen YT (March 2002). "Type I glycogen storage diseases: disorders of the glucose-6- ...
G protein
Types of G protein signaling[edit]. G protein can refer to two distinct families of proteins. Heterotrimeric G proteins, ... Gαs activates the cAMP-dependent pathway by stimulating the production of cyclic AMP (cAMP) from ATP. This is accomplished by ... G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside ... An example is adenylate cyclase, which produces the second messenger cyclic AMP.[6] For this discovery, they won the 1994 Nobel ...
Retinitis pigmentosa GTPase regulator
... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... guanyl-nucleotide exchange factor activity. • RNA binding. Cellular component. • cytoplasm. • ciliary basal body. • centrosome ... "Analysis of the RPGR gene in 11 pedigrees with the retinitis pigmentosa type 3 genotype: paucity of mutations in the coding ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ...
PETase
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... It is suggested that 57 enzymes fall into the type I category whereas the rest fall into the type II group, including the ... and there are two classifications of these enzymes including type I and type II. ... Other types of PET degrading hydrolases have been known before this discovery.[2] These include hydrolases such as: lipases, ...
G protein-coupled receptor
Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was ... Involved in growth and metastasis of some types of tumors.[24]. *Used in the endocrine system for peptide and amino-acid ... When a ligand binds to the GPCR it causes a conformational change in the GPCR, which allows it to act as a guanine nucleotide ... These signals then can be terminated by cAMP phosphodiesterase, which is an enzyme that degrades cAMP to 5'-AMP and inactivates ...
Guanylate cyclase
Because RETGC-1 produces cGMP, which keeps cyclic nucleotide-gated channels open allowing the influx of calcium, this mutation ... Types[edit]. There are membrane-bound (type 1, guanylate cyclase-coupled receptor) and soluble (type 2, soluble guanylate ... Once formed, cGMP can be degraded by phosphodiesterases, which themselves are under different forms of regulation, depending on ... Depending on cell type, it can drive adaptive/developmental changes requiring protein synthesis. In smooth muscle, cGMP is the ...
PDE5 inhibitor
"Differential Activation and Inhibition of the Multiple Forms of Cyclic Nucleotide Phosphodiesterase". Advances in Cyclic ... is a drug used to block the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth ... Weiss, B; Hait, W N (1977). "Selective Cyclic Nucleotide Phosphodiesterase Inhibitors as Potential Therapeutic Agents". Annual ... Fertel, Richard; Weiss, Benjamin (1976). "Properties and Drug Responsiveness of Cyclic Nucleotide Phosphodiesterases of Rat ...
RNA splicing
Yeast tRNA cyclic phosphodiesterase cleaves the cyclic phosphodiester group to form a 2'-phosphorylated 3' end. Yeast tRNA ... exon then performs a nucleophilic attack at the first nucleotide following the last nucleotide of the intron at the 3' splice ... This type of splicing is termed canonical splicing or termed the lariat pathway, which accounts for more than 99% of splicing. ... Splicing occurs in all the kingdoms or domains of life, however, the extent and types of splicing can be very different between ...
Phosphoserine phosphatase
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Types. *EC1 Oxidoreductases (list). *EC2 Transferases (list). *EC3 Hydrolases (list). *EC4 Lyases (list) ...
cGMP-specifična fosfodiesteraza, tip 5
Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Adv Cyclic Nucleotide Res ... http://www.garlandscience.com/textbooks/0815323042.asp?type=reviews. *Irwin H. Segel. Enzyme Kinetics: Behavior and Analysis of ... Fertel R, Weiss B (1976). „Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung" (abstract). ... Weiss B, Hait WN (1977). „Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annu. Rev ...
cAMP-dependent pathway
Kaupp UB, Seifert R (July 2002). "Cyclic nucleotide-gated ion channels". Physiol. Rev. 82 (3): 769-824. CiteSeerX 10.1.1.319. ... cAMP phosphodiesterase converts cAMP into AMP by breaking the phosphodiester bond, in turn reducing the cAMP levels ... which vary based on the type of cell. ... cyclic nucleotide-gated ion channels[9]. *exchange proteins ... caffeine and theophylline inhibit cAMP phosphodiesterase, which degrades cAMP - thus enabling higher levels of cAMP than would ...
Enzyme inhibitor
This compound is a potent inhibitor of cGMP specific phosphodiesterase type 5, the enzyme that degrades the signalling molecule ... This block of nucleotide biosynthesis is more toxic to rapidly growing cells than non-dividing cells, since a rapidly growing ... cyclic guanosine monophosphate.[40] This signalling molecule triggers smooth muscle relaxation and allows blood flow into the ... Although it is possible for mixed-type inhibitors to bind in the active site, this type of inhibition generally results from an ...
Luteinizing hormone/choriogonadotropin receptor
The cyclic AMP-regulatory dimers are degraded by phosphodiesterase and release 5'AMP. DNA in the cell nucleus binds to ... G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger. • activation of adenylate cyclase ... LHCGR have been found in many types of extragonadal tissues, and the physiologic role of some has remained largely unexplored. ... Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was ...
Achromatopsia
Known genetic causes of this are mutations in the cone cell cyclic nucleotide-gated ion channels CNGA3 (ACHM2) and CNGB3 (ACHM3 ... This α-subunit then activates a phosphodiesterase that catalyzes the conversion of cGMP to GMP, thereby reducing current ... though in some cases the truncated proteins may be able to coassemble with wild-type channels in a dominant negative fashion. ... There are at least four genetic causes of congenital ACHM, two of which involve cyclic nucleotide-gated ion channels (ACHM2/ ...
PDE11
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Phosphodiesterase type 11 (PDE11) is a type of phosphodiesterase enzyme. An inhibitor is BC11-38. ...
PLCG1
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... "Demonstration of functionally different interactions between phospholipase C-gamma and the two types of platelet-derived growth ... For example, when activated by SRC, the encoded protein causes the Ras guanine nucleotide exchange factor RASGRP1 to ... 240 (3): 635-9. doi:10.1006/bbrc.1997.7719. PMID 9398617.. *^ Ueno E, Haruta T, Uno T, Usui I, Iwata M, Takano A, Kawahara J, ...
Eosinophil-derived neurotoxin
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... 1994). "New type of linkage between a carbohydrate and a protein: C-glycosylation of a specific tryptophan residue in human ... 111 (3): 325-30. doi:10.1093/oxfordjournals.jbchem.a123757. PMID 1587793.. *. Hamann KJ, Ten RM, Loegering DA, et al. (1990). " ... 97 (3): 923-34. doi:10.1093/oxfordjournals.jbchem.a135134. PMID 3926759.. *. de Beer T, Vliegenthart JF, Löffler A, Hofsteenge ...
Vinpocetine
... acts as a phosphodiesterase (PDE) type-1 inhibitor in isolated rabbit aorta,[12] Independent of vinpocetine's ... Hagiwara M, Endo T, Hidaka H (February 1984). "Effects of vinpocetine on cyclic nucleotide metabolism in vascular smooth muscle ... 7 (3): 240-3. June 2002. PMID 12126465.. *^ Shimizu Y, Saitoh K, Nakayama M, Suto K, Raikohara R, Nemoto T. "Agranulocytosis ... Schmitt, Rick (February 3, 2017). "Dubious doses". Newsweek. Retrieved September 24, 2017.. ...
Deoxyribonuclease II
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Types. *EC1 Oxidoreductases (list). *EC2 Transferases (list). *EC3 Hydrolases (list). *EC4 Lyases (list) ... Deoxyribonuclease II (EC 3.1.22.1, DNase II, pancreatic DNase II, deoxyribonucleate 3'-nucleotidohydrolase, pancreatic DNase II ... yielding products with 3'-phosphates. As the name implies, it is more effective at acid pH. ...
Purinergic signalling
Single-nucleotide polymorphisms (SNPs) in the P2RX7 receptor gene are associated with an increased risk of bone fracture. The ... There are two types of NTs: Concentrative nucleoside transporters (CNTs): Na+-dependent symporters Equilibrative nucleoside ... the ectonucleotide pyrophosphatase/phosphodiesterases (E-NPPs) and alkaline phosphatases (APs). Extracellular AMP is hydrolyzed ... for sustained platelet aggregation through the inhibition of adenylate cyclase and a corresponding decrease in cyclic adenosine ...
Phosphodiesterase 2
"Biologic regulation through opposing influences of cyclic GMP and cyclic AMP: the Yin Yang hypothesis". Adv Cyclic Nucleotide ... As different PDE types may affect different cAMP pools, the different PDEs may regulate different processes in the cell.[9]. ... cyclic nucleotide phosphodiesterase (PDE2) on guinea pig left atria in eu- and hyperthyroidism" (PDF). Gen Physiol Biophys. 22 ... "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacol. Rev. 58 (3): 488-520. doi:10.1124/pr. ...
Restriction enzyme
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Type II[edit]. Type II site-specific deoxyribonuclease. Structure of the homodimeric restriction enzyme EcoRI (cyan and green ... Type V[edit]. Type V restriction enzymes (e.g., the cas9-gRNA complex from CRISPRs[43]) utilize guide RNAs to target specific ... Type l[edit]. Type I restriction enzymes were the first to be identified and were first identified in two different strains (K- ...
Cyclic Nucleotide Phosphodiesterases, Type 3 | Profiles RNS
Cyclic-AMP Phosphodiesterases [D08.811.277.352.640.150]. *Cyclic Nucleotide Phosphodiesterases, Type 3 [D08.811.277.352.640.150 ... "Cyclic Nucleotide Phosphodiesterases, Type 3" is a descriptor in the National Library of Medicines controlled vocabulary ... Cyclic Nucleotide Phosphodiesterases, Type 1. *Cyclic Nucleotide Phosphodiesterases, Type 2. *Cyclic Nucleotide ... Cyclic Nucleotide Phosphodiesterases, Type 4. *Cyclic Nucleotide Phosphodiesterases, Type 5. *Cyclic Nucleotide ...
3',5'-cyclic nucleotide phosphodiesterase 11A: localization in human tissues
Cyclic nucleotide phosphodiesterase 11 (PDE11) is the most recently discovered family of human 3,5-cyclic nucleotide ... phosphodiesterases (PDEs). This family contains one gene, PDE11A, with four splice variants (PDE11A1-PDE11A4). The ... cyclic nucleotide phosphodiesterase 11A: localization in human tissues Int J Impot Res. Jul-Aug 2005;17(4):320-5. doi: 10.1038/ ... Publication types * Research Support, Non-U.S. Govt MeSH terms * Adolescent * Adult ...
Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease
... act by increasing intracellular concentrations of cyclic AMP, which has a broad range of anti-inflammatory effects on various ... Cyclic-AMP Phosphodiesterases * Cyclic Nucleotide Phosphodiesterases, Type 3 * Cyclic Nucleotide Phosphodiesterases, Type 4 ... Inhibitors of phosphodiesterase type 4 (PDE4) act by increasing intracellular concentrations of cyclic AMP, which has a broad ... Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease Lancet. 2005 Jan 8-14;365(9454):167-75. doi ...
2',3'-cyclic nucleotide 3' phosphodiesterase ELISA Kits | Biocompare.com
... cyclic nucleotide 3 phosphodiesterase ELISA Kits from leading suppliers on Biocompare. View specifications, prices, citations ... cyclic nucleotide 3 phosphodiesterase ELISA Kits. The ELISA (enzyme-linked immunosorbent assay) is a well-established antibody ... cyclic nucleotide 3 phosphodiesterase ELISA ELISA Kit across 10 suppliers. ... C-Type Natriuretic Peptide ELISA Kit *. Detection Target: C-Type Natriuretic Peptide ...
3',5' Cyclic nucleotide phosphodiesterases class III: members, structure, and catalytic mechanism. - PubMed - NCBI
2002 Feb 15;46(3):278-86. Research Support, Non-U.S. Govt; Research Support, U.S. Govt, P.H.S. ... Publication types, MeSH terms, Substance, Grant support. Publication types. *Research Support, Non-U.S. Govt ... Cyclic nucleotide phosphodiesterases (PDEs) comprise a superfamily of enzymes that were previously divided by their primary ... Cyclic nucleotide phosphodiesterases class III: members, structure, and catalytic mechanism.. Richter W1. ...
Cyclic Nucleotide Phosphodiesterases, Type 5 | Harvard Catalyst Profiles | Harvard Catalyst
Cyclic-AMP Phosphodiesterases [D08.811.277.352.640.150]. *Cyclic Nucleotide Phosphodiesterases, Type 5 [D08.811.277.352.640.150 ... Cyclic-GMP Phosphodiesterases [D08.811.277.352.640.155]. *Cyclic Nucleotide Phosphodiesterases, Type 5 [D08.811.277.352.640.155 ... "Cyclic Nucleotide Phosphodiesterases, Type 5" by people in Harvard Catalyst Profiles by year, and whether "Cyclic Nucleotide ... "Cyclic Nucleotide Phosphodiesterases, Type 5" by people in Profiles.. * Are Phosphodiesterase-5 Inhibitors a New Frontier for ...
EMD 60263
Summary Report | CureHunter
07/01/2000 - "The effects of a novel Ca(2+)-sensitizer (EMD 60263, 10 microM, group 1) were compared with a phosphodiesterase ( ... Type 3 Cyclic Nucleotide Phosphodiesterases 2. 1,2,3,4-tetrahydroquinoline 3. zatebradine ... a Ca2+ sensitizer without phosphodiesterase III inhibitory properties, increased contractility more profoundly in stunned than ... sensitizing agent with negligible phosphodiesterase III inhibitory activity, on diastolic function of regionally stunned ...
Lipoatrophic Diabetes Mellitus
Summary Report | CureHunter
A type of diabetes mellitus that is characterized by severe INSULIN RESISTANCE and LIPODYSTROPHY. The latter may be generalized ... 07/01/2000 - "This study investigated the association between glutamic acid decarboxylase antibodies (GAD-AB) and Type 1, Type ... 11/01/2001 - "We screened for mutations in the gene of insulin-sensitive phosphodiesterase 3B (PDE3B), which regulates ... antilipolytic actions of insulin via reduction of intracellular cyclic AMP levels, in Japanese patients with type 2 diabetes ...
Cyclic GMP-Dependent Protein Kinases and the Cardiovascular System | Circulation Research
Cyclic nucleotide research: still expanding after half a century. Nat Rev Mol Cell Biol. 2002; 3: 710-718. ... Cyclic GMP phosphodiesterases and regulation of smooth muscle function. Circ Res. 2003; 93: 280-291. ... cAK indicates cAMP-dependent protein kinase; cGK(I/II), cGMP-dependent protein kinase (type I/II); cGMP, cyclic guanosine-3′,5 ... Cyclic AMP- and cyclic GMP-dependent protein kinases differ in their regulation of cyclic AMP response element-dependent gene ...
Human Metabolome Database: Showing Protein Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C ...
Protein Type. Unknown. Biological Properties. General Function. Involved in catalytic activity. Specific Function. Cyclic ... cyclic nucleotide phosphodiesterase 1C (HMDBP00605). IdentificationBiological propertiesGene propertiesProtein properties ... cyclic nucleotide phosphodiesterases. J Biol Chem. 1996 Jan 12;271(2):796-806. [PubMed:8557689 ] ... nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many ...
Cyclic nucleotide phosphodiesterases (PDE) 3 and 4 in normal, malignant, and HTLV-I transformed human lymphocytes
type. Contribution to journal publication status. published. subject. *Endocrinology and Diabetes. keywords. human lymphocytes ... Intracellular cyclic AMP, determined in part by cyclic nucleotide phosphodiesterases (PDEs), regulates proliferation and immune ... Intracellular cyclic AMP, determined in part by cyclic nucleotide phosphodiesterases (PDEs), regulates proliferation and immune ... Cyclic nucleotide phosphodiesterases (PDE) 3 and 4 in normal, malignant, and HTLV-I transformed human lymphocytes. Ekholm, Dag ...
Two types of detergent-insoluble, glycosphingolipid/cholesterol-rich membrane domains from isolated myelin - Arvanitis - 2005 -...
... cyclic nucleotide 3′-phosphodiesterase modulates cell morphology. J. Neurosci. Res. 39, 386 - 397. *Wiley Online Library , ... phosphodiesterase isoform 2 and identification of specifically phosphorylated serine residues. J. Neurochem. 74, 540 - 546. * ... cyclic nucleotide 3′-phosphodiesterase (CNP), myelin/OL basic protein and the tight junction protein claudin-11 (formerly ... Other cell types have also been found to have several different microdomains of different composition (Madore et al. 1999; ...
JCI Insight -
Blocking MHC class II on human endothelium mitigates acute rejection
Functional regulatory T cells produced by inhibiting cyclic nucleotide phosphodiesterase type 3 prevent allograft rejection. ... If development into CTL occurs within the graft, the question arises as to which types of graft cells stimulate this process. ... Immunocompetent T-cells with a memory-like phenotype are the dominant cell type following antibody-mediated T-cell depletion. ... or type III (transmural arteritis) (44). The presence and degree of such vascular lesions is reported to correlate with the ...
Restoration of Neuronal Plasticity by a Phosphodiesterase Type 1 Inhibitor in a Model of Fetal Alcohol Exposure | Journal of...
Kakkar R, Raju RVS, Sharma RK (1999) Calmodulin-dependent cyclic nucleotide phosphodiesterase (PDE1). Cell Mol Life Sci 55: ... Restoration of Neuronal Plasticity by a Phosphodiesterase Type 1 Inhibitor in a Model of Fetal Alcohol Exposure. Alexandre E. ... Restoration of Neuronal Plasticity by a Phosphodiesterase Type 1 Inhibitor in a Model of Fetal Alcohol Exposure ... Restoration of Neuronal Plasticity by a Phosphodiesterase Type 1 Inhibitor in a Model of Fetal Alcohol Exposure ...
Natriuretic Peptide, Pro, C-Type, aa30-50 (pro-CNP) Antibody
... cyclic nucleotide 3 phosphodiesterase. Locus17q21.2. Discovery year1991-07-15 ... Alternative name2 Natriuretic Peptide, Pro, C-Type, aa30-50 (pro-CNP) Alternative name3 Natriuretic Peptide, Pro, C-Type, aa30- ... Alternative name4 Natriuretic Peptide, Pro, C-Type, aa30-50 Alternative name5 Anti -Natriuretic Peptide, Pro, C-Type, aa30-50 ( ... MBS621328 , Natriuretic Peptide, Pro, C-Type, aa30-50 (pro-CNP) Antibody size: 100ul , 1,149.25 USD Catalog number MBS621328 ...
Pde1c - Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C - Mus musculus (Mouse) - Pde1c gene & protein
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators ... Type I PDE are activated by the binding of calmodulin in the presence of Ca2+. ... calmodulin-dependent cyclic-nucleotide phosphodiesterase activity Source: MGIInferred from sequence orthologyi*7568196 ... Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators ...
Engineered Biosynthesis of 5/5/6 Type Polycyclic Tetramate Macrolactams in an Ikarugamycin (5/6/5 Type)-Producing Chassis.
Combinatorial biosynthesis of 5/5/6 type polycyclic tetramate macrolactams (PoTeMs) was achieved in an engineered ikarugamycin ... Cyclic Nucleotide Phosphodiesterases, Type 1. A CALCIUM and CALMODULIN-dependent cyclic nucleotide phosphodiesterase subfamily ... type II (intermediate form), and type III (Kugelberg-Welander disease). Type I is fatal in infancy, type II has a late ... The three members of this family are referred to as type 1A, type 1B, and type 1C and are each product of a distinct gene. In ...
Oligodendrocyte - Wikipedia
... phosphodiesterase (CNPase) List of human cell types derived from the germ layers Carlson, Neil (2010). Physiology of Behavior. ... Cyclic-nucleotide 3- ... Oligodendrocytes are a type of glial cell. They arise during ... They are the last cell type to be generated in the CNS. Oligodendrocytes were discovered by Pío del Río Hortega. ... Oligodendrocytes (from Greek cells with a few branches), or oligodendroglia, are a type of neuroglia whose main functions are ...
WikiGenes - Ro 201724 - 4-[(3-butoxy-4-methoxy...
Papaverine and Ro 20-1724 inhibit cyclic nucleotide phosphodiesterase activity and increase cyclic AMP levels in psoriatic ... Treatment with the type IV phosphodiesterase inhibitor Ro 20-1724 protects renal and mesenteric blood flow in endotoxemic rats ... Papaverine and Ro 20-1724 inhibit cyclic nucleotide phosphodiesterase activity and increase cyclic AMP levels in psoriatic ... Cyclic AMP-mediated regulation of vascular smooth muscle cell cyclic AMP phosphodiesterase activity. Rose, R.J., Liu, H., ...
3'5'-cyclic nucleotide phosphodiesterase, catalytic domain superfamily (IPR036971) | InterPro | EMBL-EBI
Type 3 phosphodiesterase inhibitors may be protective against cerebrovascular events in patients with claudication.. null 17 ... The cyclic nucleotide phosphodiesterases (PDE) comprise a group of enzymes that degrade the phosphodiester bond in the second ... 35-cyclic nucleotide phosphodiesterase, catalytic domain superfamily (IPR036971). Short name: PDEase_catalytic_dom_sf ... They regulate the localisation, duration and amplitude of cyclic nucleotide signalling within subcellular domains. PDEs are ...
ORM-3819 promotes cardiac contractility through Ca<sup>2+</sup> sensitization in combination with selective PDE III inhibition,...
keywords = "Ca sensitization, Levosimendan, Myocardial stunning, ORM-3819, Phosphodiesterase III inhibition, Positive inotropic ... and a selective inhibition of the phosphodiesterase III (PDE III) isozyme (IC50=3.88±0.3 nM) was revealed during in vitro ... and a selective inhibition of the phosphodiesterase III (PDE III) isozyme (IC50=3.88±0.3 nM) was revealed during in vitro ... and a selective inhibition of the phosphodiesterase III (PDE III) isozyme (IC50=3.88±0.3 nM) was revealed during in vitro ...
Table of Contents - May 01, 2014, 459 (3) | Biochemical Journal
The upstream conserved regions (UCRs) mediate homo- and hetero-oligomerization of type 4 cyclic nucleotide phosphodiesterases ( ... Chitinase-3-like protein 1 protects skeletal muscle from TNFα-induced inflammation and insulin resistance Sven W. Görgens, ... Biochemical Journal May 01, 2014, 459 (3) 551-564; DOI: https://doi.org/10.1042/BJ20131363 ... Biochemical Journal May 01, 2014, 459 (3) 427-439; DOI: https://doi.org/10.1042/BJ20130172 ...
Quantification of Cilostazol and Telmisartan in Combination Using Risk Profile and Uncertainty Contour: A Contemporary...
... a dual inhibitor of cyclic nucleotide phosphodiesterase type 3 and adenosine uptake. Cardiovasc Drug Rev 19: 369-386. ... Sample mass has three types of uncertainty sources sensitivity, linearity, and repeatability. Mass of the sample was expressed ... quinolinone and is a quinolinone derivative that inhibits cellular phosphodiesterase III, and is used for the inhibition of ... J. PharmTech Res 3: 763-769.. *Jose K,Jaysekhar P, Jinu J (2014) HPTLC Determination of Cilostazol in Pharmaceutical Dosage ...
Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using...
Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ... Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ... Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ... Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ...
The role of the cyclic GMP-inhibited cyclic AMP-specific phosphodiesterase (PDE3) in regulating clonal BRIN-BD11 insulin...
... cyclic nucleotide phosphodiesterases, type 3, insulin, insulin-like growth factor I, islets of langerhans, mitogen-activated ... We report here that the cyclic GMP-inhibited cyclic AMP specific phosphodiesterase (PDE3B) is expressed as a membrane-bound ... The role of the cyclic GMP-inhibited cyclic AMP-specific phosphodiesterase (PDE3) in regulating clonal BRIN-BD11 insulin ... The role of the cyclic GMP-inhibited cyclic AMP-specific phosphodiesterase (PDE3) in regulating clonal BRIN-BD11 insulin ...
Potential L-Type Voltage-Operated Calcium Channel Blocking Effect of Drotaverine on Functional Models | Journal of Pharmacology...
1981) Effects of cyclic AMP- and cyclic GMP- phosphodiesterase inhibitors on immunological release of histamine and on lung ... nucleotide-phosphodiesterase as a possible mode of action of papaverine and similarly acting drugs. Naunyn Schmiedebergs Arch ... 1970) Cyclic phosphodiesterase activity and the action of papaverine. Biochem Biophys Res Commun 40:64-69. ... L-type voltage-operated calcium channel. PDE. phosphodiesterase receptor-operated calcium channels. ...
Neuronal calcium sensor-1 - Wikipedia
... cyclic nucleotide phosphodiesterases ARF1 (ADP Ribosylation factor 1) A type (Kv4.3; Shal-related subfamily, member 3) voltage- ... The designation NCS-1 came from the assumption that the protein was expressed only in neuronal cell types, which is not the ... type III phosphatidylinositol 4-kinase β) IP3 receptor (this activity is inhibited by lithium - a drug used for the treatment ... 8 (3): 182-193. doi:10.1038/nrn2093. PMC 1887812. PMID 17311005. Burgoyne RD, OCallaghan DW, Hasdemir B, Haynes LP, Tepikin AV ...
Patente US7660631 - Methods and systems for electrical and/or drug stimulation as a therapy for ... - Google Patentes
Cyclic nucleotide phosphodiesterases, specifically Type 5, break down cGMP to GMP by catalyzing a reaction that breaks the ... on the Relaxation of Human Corpus Cavernosum Tissue in Vitro and on the Activities of Cyclic Nucleotide Phosphodiesterase ... Carter, et al., "Effect of the Selective Phosphodiesterase Type Inhibitor Sildenafil on Erectile Function in the Anesthetized ... "Sildenafil, a Novel Inhibitor of Phosphodiesterase Type 5 in Human Corpus Cavernosum Smooth Muscle Cells", Life Sciences 62 ( ...
PDE - Esterases (Phosphodi-) - Hydrolases - Enzymes - Products
Phosphodiesterases listed: PDE, PLC, PLD. [1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases ... They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. Roughly, the sub-types can ... No less than eleven sub-types of the enzyme family of phosphodiesterases (PDE; EC 3.1.4.-) are known to date, many of which ... 2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug ...
Plus it
... phosphodiesterase (CNPase) in the corpus callosum of the wild-type and Act1-deficient mice. As shown in Figure 1E, cuprizone ... cyclic nucleotide 3′- ... 4A) than wild-type controls. Cuprizone-induced PDGFR-α+ cell ... IL-17 is produced by varied cell types, including CD8+ T cells, γδT, and NK cells as well as CD4+ Th17 cells. Interestingly, we ... To determine the role of the IL-17A-Act1 axis in cuprizone-induced demyelination, we fed age- and sex-matched wild-type, IL-17A ...
InhibitorsPDEsInhibitorPDE4GeneProteinsAdenosine monophosphateProtein KinasesInhibitionHydrolysisPDE3AbstractSecond messenger cyclicEnzymesSignal TransductionCharacterization of the cyclicPDE3AIntracellular cyclicInsulin resistanceGuanylyl CyclaseSubfamilyMeSHRegulatesCardiacMitogen-activaPhosphateSpecificityRegulateSingle nucleotide2002PathwaysAdipocytesIschemicReceptorTherapeuticActivity
Inhibitors13
- Inhibitors of phosphodiesterase type 4 (PDE4) act by increasing intracellular concentrations of cyclic AMP, which has a broad range of anti-inflammatory effects on various key effector cells involved in asthma and chronic obstructive pulmonary disease (COPD). (nih.gov)
- Ultimately, clinicians will want to know whether PDE4 inhibitors are anything more than expensive "designer" theophylline, the archetypal non-selective phosphodiesterase inhibitor. (nih.gov)
- Are Phosphodiesterase-5 Inhibitors a New Frontier for Prevention of Colorectal Cancer? (harvard.edu)
- Although some studies showed the efficacy of phosphodiesterase (PDE) inhibitors as neuronal plasticity enhancers, little is known about the effectiveness of these drugs to improve plasticity in cases of mental retardation. (jneurosci.org)
- Type 3 phosphodiesterase inhibitors may be protective against cerebrovascular events in patients with claudication. (ebi.ac.uk)
- Theophylline and 3-isobutyl-1-methylxanthine, two cyclic nucleotide phosphodiesterase inhibitors, when fed to wild-type Drosophila adults, cause the rapid decay of learning index after training in a shock-odor learning paradigm. (springer.com)
- The CO-induced increase in I Ba was blocked when cells were pretreated with 1H-[1,2,4]- oxadiazolo[4,3-a]quinoxalin-1-one (10 μM) or inhibitors of NO synthase (NOS). (elsevier.com)
- Inhibitors and activators were used to characterize the involvement of nitric oxide, soluble guanylate cyclase, cyclic GMP, protein kinase G and BKCa channel. (ufl.edu)
- Aim and Objective: Human full-length cyclic nucleotide phosphodiesterase isozyme 4B2 (hPDE4B2) as the target for screening and characterizing inhibitors suffers from low activity yield and the coexistence of two conformational states bearing different affinities for (R)-rolipram. (eurekaselect.com)
- Rodent studies have consistently shown upregulation of the 3, 5-cyclic adenosine monophosphate (cAMP) system induced by different types of chronic but not acute antidepressant treatment including serotonin and norepinephrine uptake inhibitors, monoamine oxidase inhibitors, tricyclic antidepressants, lithium and electroconvulsions. (clinicaltrials.gov)
- In addition, induction of PAI was enhanced by isobutyl-methylxanthine, a phosphodiesterase inhibitor, but not, however, by other phosphodiesterase inhibitors, or by forskolin or N(G)-nitro-L-arginine, suggesting an effect of isobutyl-methylxanthine other than through cyclic nucleotides. (tudelft.nl)
- The paper describes the discovery and characterization of a polymorphism in the promoter region of the phosphodiesterase 3A (PDE3A) gene, which encodes the target of Type 3 phosphodiesterase inhibitors (PDE3Is). (yahoo.com)
- Phosphodiesterase inhibitors, pentoxifylline and rolipram, increase bone mass mainly by promoting bone formation in normal mice. (naver.com)
PDEs15
- 3',5'-Cyclic nucleotide phosphodiesterase 11 (PDE11) is the most recently discovered family of human 3',5'-cyclic nucleotide phosphodiesterases (PDEs). (nih.gov)
- 3',5' Cyclic nucleotide phosphodiesterases (PDEs) comprise a superfamily of enzymes that were previously divided by their primary structure into two major classes: PDE class I and II. (nih.gov)
- The 3',5' cyclic AMP phosphodiesterase from Escherichia coli encoded by the cpdA gene does not show any homology to either PDE class I or class II enzymes and, therefore, represents a new, third class of PDEs. (nih.gov)
- 2,3 Cyclic GMP is degraded by cGMP-hydrolyzing phosphodiesterases (PDEs). (ahajournals.org)
- 6 Like NO, cGMP can affect multiple signaling pathways ( Figure 1 A). 1,5,6 To date, three classes of cGMP receptor proteins have been identified: cyclic nucleotide-gated (CNG) cation channels, cGMP-regulated PDEs, which hydrolyze cAMP and/or cGMP, and cGMP-dependent protein kinases (cGKs). (ahajournals.org)
- Intracellular cyclic AMP, determined in part by cyclic nucleotide phosphodiesterases (PDEs), regulates proliferation and immune functions in lymphoid cells. (lu.se)
- This project aims to unite global efforts to target the highly druggable class of enzymes called cyclic nucleotide phosphodiesterases (PDEs) in the fight for neglected parasitic diseases (NPD). (europa.eu)
- Phosphodiesterases (PDEs) are a family of phosphohydrolyases that catalyze the hydrolysis of 3' cyclic phosphate bonds in adenosine and/or guanine 3',5' cyclic monophosphate (cAMP and/or cGMP). (genecards.org)
- cAMP is synthesized from adenosine 5-triphosphate (ATP) by adenylyl cyclase and metabolized by cyclic nucleotide phosphodiesterases (PDEs). (clinicaltrials.gov)
- Cyclic nucleotide PDEs have been categorized into 11 families and are encoded by at least 21 genes. (aspetjournals.org)
- Specific functions for different cyclic nucleotide phosphodiesterases (PDEs) have not yet been identified in most cell types. (pnas.org)
- The findings further suggest that the approach of using selective, inhibitor-dependent phosphoproteome analysis can provide a generalized methodology for understanding the roles of different PDEs in the regulation of cyclic nucleotide signaling. (pnas.org)
- Phosphodiesterases (PDEs) provide the sole route for degrading cAMP in cells and are thus poised to regulate intracellular cAMP gradients. (ox.ac.uk)
- A large family of enzymes named cyclic nucleotide phosphodiesterases (PDEs) inactivate cAMP and cGMP through their hydrolysis ( 11 - 14 ). (diabetesjournals.org)
- Cyclic nucleotide hydrolyzing phosphodiesterases (PDEs), which comprise a large superfamily of 11 families termed PDE1-PDE11 ( 13 , 14 ), play a fundamental role in regulating T cell signaling. (jimmunol.org)
Inhibitor30
- Preimplant Phosphodiesterase-5 Inhibitor Use Is Associated With Higher Rates of Severe Early Right Heart Failure After Left Ventricular Assist Device Implantation. (harvard.edu)
- Analysis of short-term treatment with the phosphodiesterase type 5 inhibitor tadalafil on long bone development in young rats. (harvard.edu)
- The effects of a novel Ca(2+)-sensitizer (EMD 60263, 10 microM, group 1) were compared with a phosphodiesterase (PDE) III-inhibitor (enoximon, 20 microM, group 2) on 14 isolated, blood-perfused rabbit hearts during reperfusion after a global ischemia of 20 min. (curehunter.com)
- Using a combination of electrophysiological and optical imaging techniques, we show here that vinpocetine, a PDE type I inhibitor, restores ocular dominance plasticity in the ferret model of fetal alcohol exposure. (jneurosci.org)
- Here, we try to restore ocular dominance plasticity in alcohol-exposed ferrets using the PDE type 1 inhibitor vinpocetine. (jneurosci.org)
- This was shown using SKF94836 (PDE3 inhibitor) which maximally inhibited membrane-bound cyclic AMP PDE activity by approximately 25-30% and by RT-PCR. (strath.ac.uk)
- A selective phosphodiesterase 3 inhibitor rescues low PO2-induced ATP release from erythrocytes of humans with type 2 diabetes: implication for vascular control. (nih.gov)
- Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity. (nih.gov)
- Amrinone, a selective phosphodiesterase (PDE) III inhibitor, is a newly developed agent that possesses a combination of positive inotropic and vasodilating properties as a result of preventing the degradation of cAMP and it has recently been licensed for treatment of heart failure alone. (elsevier.com)
- The PKA inhibitor KT-5720 (0.5 μM) and milrinone (3 μM), a phosphodiesterase (PDE) III inhibitor, blocked the effect of CO on I Ba . (elsevier.com)
- Among components of the cAMP pathway, PDE4 appears to be critical for antidepressant effects because an inhibitor of PDE4, 4-[3-(cyclopenotoxyl)-4-methoxyphenyl]-2-pyrrolidone (rolipram), showed antidepressant effects both in animals and humans, and various forms of antidepressant treatment induced increase in PDE4 in rodents. (clinicaltrials.gov)
- The nonselective PDE inhibitor 3-isobutyl-1-methylxanthine (IBMX) potentiated the ability of NMDA to increase cAMP and cGMP. (aspetjournals.org)
- In contrast, only the PDE2 inhibitor erythro -9-(2-hydroxy-3-nonyl) adenine (EHNA) enhanced the ability of NMDA to increase cGMP. (aspetjournals.org)
- Amrinone , a specific inhibitor of phosphodiesterase 3, has an antioxidant activity against PMNs. (bvsalud.org)
- Pharmacological modulation of the in vivo induction of plasminogen activator inhibitor type-1 (PAI-1) synthesis was studied in rats using the induction of PAI-1 by endotoxin as a model system. (tudelft.nl)
- Roflumilast, type 4 phosphodiesterase inhibitor, attenuates inflammation in rats with ulcerative. (deepdyve.com)
- El-Adawy, Samar A. 2018-03-01 00:00:00 BackgroundRoflumilast (Rof), a phosphodiesterase 4 (PDE4) inhibitor, has been shown to be an effective agent in inflammatory diseases and marketed for chronic obstructive pulmonary disease. (deepdyve.com)
- RVT-501 (E6005) is a selective phosphodiesterase 4 (PDE4PDE4) inhibitor with an IC50 of 2.8 nM. (abmole.com)
- competitive nonselective phosphodiesterase inhibitor and nonselective adenosine receptor antagonist. (abmole.com)
- Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5. (abmole.com)
- Sildenafil is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM. (abmole.com)
- Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake. (abmole.com)
- Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist. (abmole.com)
- Vardenafil hydrochloride Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. (abmole.com)
- Milrinone is a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE. (abmole.com)
- Piclamilast (RP 73401) is a potent and selective inhibitor of phosphodiesterase (PDE) 4. (abmole.com)
- Roflumilast (trade names Daxas, Daliresp) is a novel and selective, long-acting inhibitor of phosphodiesterase 4 (PDE-4). (abmole.com)
- GSK256066 is a selective phosphodiesterase 4 (PDE4)inhibitor with an IC50 of 3.2 pM. (abmole.com)
- Short-term or long-term treatments with a phosphodiesterase-4 (PDE4) inhibitor result in opposing agonist-induced Ca 2+ responses in endothelial cells. (unistra.fr)
- Bucladesine is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor. (wikipedia.org)
PDE44
- Type 4 PDE (PDE4) is selective to cAMP in the brain. (clinicaltrials.gov)
- VSMC cAMP hydrolysis is catalyzed by members of the phosphodiesterase 3 (PDE3) and PDE4 families ( 12 ), whereas VSMC cGMP is inactivated by PDE1 or PDE5 enzymes ( 15 ). (diabetesjournals.org)
- S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer. (abmole.com)
- Type 4 phosphodiesterases (PDE4) are critical regulators in TCR signaling by attenuating the negative constraint of cAMP. (jimmunol.org)
Gene17
- A cyclic nucleotide phosphodiesterase subfamily that is inhibited by the binding of CYCLIC GMP to an allosteric domain found on the enzyme and through phosphorylation by regulatory kinases such as PROTEIN KINASE A and PROTEIN KINASE B. The two members of this family are referred to as type 3A, and type 3B, and are each product of a distinct gene. (uams.edu)
- The present study shows by computational analysis that the enzyme encoded by the E. coli cpdA gene belongs to a family of phosphodiesterases that closely resembles the catalytic machinery known from purple acid phosphatases and several other dimetallophosphoesterases. (nih.gov)
- Furthermore, the known biochemical properties of the bacterial phosphodiesterase encoded by the cpdA gene, such as the requirement of iron ions and a reductant for maintaining its catalytic activity, support this hypothesis developed by computational analysis. (nih.gov)
- Systematic search for single nucleotide polymorphisms in the 5' flanking region of the human phosphodiesterase 3B gene: absence of evidence for major effects of identified polymorphisms on susceptibility to Japanese type 2 diabetes. (nih.gov)
- PDE3B (Phosphodiesterase 3B) is a Protein Coding gene. (genecards.org)
- Gene Ontology (GO) annotations related to this gene include 3',5'-cyclic-nucleotide phosphodiesterase activity and cGMP-inhibited cyclic-nucleotide phosphodiesterase activity . (genecards.org)
- Recently published studies from different populations provide apparently conflicting evidence on the association between the phosphodiesterase 4D (PDE4D) gene and ischemic stroke. (bvsalud.org)
- We selected and genotyped a PDE4D single nucleotide polymorphism (SNP 41, rs152312) as a candidate marker for susceptibility to ischemic stroke because SNP 41 has shown the most significant association with stroke in both a meta-analysis and the original Icelandic study of the PDE4D gene. (bvsalud.org)
- Prominent interferon (IFN) inducible gene signatures in TB patients and animal models of Mycobacterium tuberculosis infection have drawn significant attention to the roles of type I IFNs in the host response to mycobacterial infections. (frontiersin.org)
- Recently described gene signatures in blood of patients with active TB disease ( 3 - 9 ) are being explored extensively for their utility as biomarkers for the reliable diagnosis of active TB, tracking of at-risk individuals, and monitoring of treatment outcome. (frontiersin.org)
- Additionally, the discovery of IFN-related gene signatures in patients with active TB disease ( 3 - 9 ) has created significant momentum behind investigation of the innate immune pathways and pathophysiological consequences of type I IFN expression during M. tuberculosis infection. (frontiersin.org)
- Context Convergent data make 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNP) a candidate gene for schizophrenia. (cf.ac.uk)
- The protein encoded by this gene belongs to the cyclic nucleotide phosphodiesterase (PDE) family, and PDE7 subfamily. (mybiosource.com)
- Development of decompensated dilated cardiomyopathy is associated with decreased gene expression and activity of the milrinone-sensitive cAMP phosphodiesterase PDE3A. (semanticscholar.org)
- Distinctive anatomical patterns of gene expression for cGMP-inhibited cyclic nucleotide phosphodiesterases. (semanticscholar.org)
- Association between a variation in the phosphodiesterase 4D gene and bone mineral density. (naver.com)
- High-throughput development and characterization of a genomewide collection of gene-based single nucleotide polymorphism markers by chip-based matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. (naver.com)
Proteins5
- In addition, the availability of atomic coordinates for several purple acid phosphatases and related proteins allowed the generation of a three-dimensional model for class III cyclic nucleotide phosphodiesterases. (nih.gov)
- The gel can be used for affinity chromatography of various cyclic nucleotide-responsive proteins such as protein kinases, phosphodiesterases and others. (biolog.de)
- Several other proteins such as cyclic nucleotide gated ion channels ( 1 ), phosphodiesterases (PDE) ( 2 ), and guanine nucleotide exchange factors (Epac) ( 3 ) bind cAMP. (mcponline.org)
- When combined with electrophysiology, mouse genetics provides unmatched power in elucidating the in vivo functions of key phototransduction proteins, most of which have been knocked out, overexpressed or mutated in rods, yielding a rich body of information on the mechanisms underlying the amplification, recovery and adaptation of rod/cone photoresponses (Table 1, Figures 2 & 3). (utah.edu)
- The discs carry the visual pigment (rhodopsin in rods and cone pigment in cones) and other transduction components either as transmembrane or peripheral membrane proteins (Figure 3). (utah.edu)
Adenosine monophosphate2
- We hypothesized that β 2 -adrenergic receptor (AR)-coupled PI3K constrains increases in cardiac inotropy through cyclic adenosine monophosphate (cAMP)-dependent phosphodiesterase (PDE) activation. (elsevier.com)
- The 29 nucleotide (nt) insertion/deletion (indel) polymorphism is 2214 nts upstream from the PDE3A1 translation start site that regulates transcriptional activity in response to cyclic adenosine monophosphate (cAMP) levels, with the insertion (INS) allele having a frequency of 0.41. (yahoo.com)
Protein Kinases1
- cAMP coordinates the regulation of these cellular responses by activating cAMP-dependent protein kinases (PKAs) ( 4 ), specific guanine nucleotide exchange factors (EPACs) ( 5 ), and cyclic nucleotide-gated ion channels ( 6 ). (pnas.org)
Inhibition8
- Phosphodiesterase 5 Inhibition Limits Doxorubicin-induced Heart Failure by Attenuating Protein Kinase G Ia Oxidation. (harvard.edu)
- It is well established that inhibition of dipeptidyl peptidase (DPP)-IV reduces glucose levels and preserves pancreatic beta cell function in patients with type 2 diabetes. (bioportfolio.com)
- Phosphodiesterase 5 inhibition in essential hypertension. (ebi.ac.uk)
- ORM-3819 binding to cardiac troponin C (cTnC) was confirmed by nuclear magnetic resonance spectroscopy, and a selective inhibition of the phosphodiesterase III (PDE III) isozyme (IC 50 =3.88±0.3 nM) was revealed during in vitro enzyme assays. (elsevier.com)
- Biochemical characterization of the inhibition of the two major phosphodiesterase isoenzymes in Drosophila by theophylline predicts only a slight inhibition of these enzymes in vivo , in accordance with the unchanged level of cAMP in wild-type fly heads during drug feeding. (springer.com)
- Is inhibition of PDE3B a possible target for treatment of obesity or type 2 diabetes mellitus? (nih.gov)
- Inhibition of human phosphodiesterase 4A expressed in yeast cell GL62 by theophylline, rolipram, and acetamide-45. (illumina.com)
- The second messenger cAMP has been recognized as an important mediator of such inhibitory signaling mechanisms by activation of the cAMP-protein kinase A (PKA), 3 with PKA functioning as a gatekeeper of tonic inhibition in T cells ( 5 , 6 , 7 , 8 , 9 , 10 ). (jimmunol.org)
Hydrolysis3
- This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP. (uniprot.org)
- An enzyme that catalyzes the hydrolysis of cyclic AMP to form adenosine 5'-phosphate. (termsciences.fr)
- Experiments were carried out to determine which phosphodiesterase (PDE) families are involved in the hydrolysis of the cyclic nucleotides formed via this mechanism, using primary neuronal cultures prepared from rat cerebral cortex and hippocampus. (aspetjournals.org)
PDE31
- Similarly, insulin, IGF-1, or leptin activates PDE3 by a protein kinase B (PKB)-mediated, phosphatidylinositol 3-kinase (PI3K)-dependent phosphorylation reaction. (diabetesjournals.org)
Abstract1
- abstract = "This study is the first pharmacological characterization of the novel chemical entity, ORM-3819 (L-6-{4-[N'-(4-Hydroxi-3-methoxy-2-nitro-benzylidene)-hydrazino]-phenyl}-5-methyl-4,5-dihydro-2 H-pyridazin-3-one), focusing primarily on its cardiotonic effects. (elsevier.com)
Second messenger cyclic2
- The second messenger cyclic AMP immobilized on agarose by an aminohexylamino spacer attached to position 8 of the ligand. (biolog.de)
- The second messenger cyclic AMP (cAMP) has a central role in cell signalling in the ovary and its degradation is carried out by the phosphodiesterase (PDE) enzyme family. (ulaval.ca)
Enzymes2
- The cyclic nucleotide phosphodiesterases (PDE) comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. (ebi.ac.uk)
- 1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. (axonmedchem.com)
Signal Transduction3
- Retinal 3',5'-cGMP phosphodiesterase is located in photoreceptor outer segments: it is light activated, playing a pivotal role in signal transduction. (ebi.ac.uk)
- Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. (uniprot.org)
- The encoded protein plays a role in signal transduction by regulating the intracellular concentration of these cyclic nucleotides. (abnova.com)
Characterization of the cyclic2
- A partial characterization of the cyclic nucleotide phosphodiesterases of Drosophila melanogaster. (springer.com)
- Cloning and characterization of the cyclic guanosine monophosphate-inhibited phosphodiesterase PDE3A expressed in mouse oocyte. (semanticscholar.org)
PDE3A4
- Recently, we found that expression of cAMP hydrolyzing phosphodiesterase 3A (PDE3A) was significantly reduced in human failing hearts, accompanied by up-regulation of inducible cAMP early repressor (ICER) expression. (montclair.edu)
- With respect to Ang II, the initiation of the PDE3A-ICER feedback loop depends on activation of Ang II type 1 receptor (AT1R), classical PKC(s), and CREB (cAMP response element binding protein). (montclair.edu)
- Isoforms of cyclic nucleotide phosphodiesterase PDE3A in cardiac myocytes. (semanticscholar.org)
- PDE3A cyclic nucleotide phosphodiesterases regulate cAMP- and cGMP-mediated intracellular signaling in cardiac myocytes. (semanticscholar.org)
Intracellular cyclic2
- We propose that the deregulation of the PI3K/PDE3B pathway might result in increased intracellular cyclic AMP accumulation, which promotes apoptosis. (strath.ac.uk)
- The enzyme is widely distributed in animal tissue and controls the level of intracellular cyclic AMP. (termsciences.fr)
Insulin resistance3
- A type of diabetes mellitus that is characterized by severe INSULIN RESISTANCE and LIPODYSTROPHY. (curehunter.com)
- Of the many animal models used in the study of non-insulin-dependent (type 2) diabetes, the JCR:LA-cp rat is unique in that it develops insulin resistance in the presence of obesity and manifests both peripheral and coronary vasculopathies. (diabetesjournals.org)
- In this context, epidemiological evidence consistent with an increased risk of atherosclerosis in diabetes is mounting, with a possible role for 1 ) insulin resistance and its associated hyperinsulinemia, 2 ) poor glycemic control leading to elevated levels of advanced glycosylated end products, or 3 ) elevated circulating leptin levels associated with increased adipose mass ( 1 - 5 ). (diabetesjournals.org)
Guanylyl Cyclase3
- 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)
- Here we show that in platelets and aortic tissue, NO led to a biphasic response characterized by a tremendous increase in cGMP (up to 100-fold) in less than 30 s and a rapid decline, reflecting the tightly controlled balance of guanylyl cyclase and phosphodiesterase activities. (rupress.org)
- The influx of Ca 2+ also stimulates Ca 2+ -calmodulin-dependent nitric-oxide (NO) synthase (NOS) type to produce NO, which stimulates guanylyl cyclase to produce cGMP (for review, see Garthwaite, 1991 ). (aspetjournals.org)
Subfamily2
- A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. (harvard.edu)
- Shal-related subfamily, member 3) voltage-gated potassium channels Nitric oxide synthase TRPC5 channel Ric8a Frq modulates Ca2+ entry through a functional interaction with the α1 voltage-gated Ca2+-channel subunit. (wikipedia.org)
MeSH1
- Cyclic Nucleotide Phosphodiesterases, Type 3" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uams.edu)
Regulates2
- Phosphodiesterase type 3A regulates basal myocardial contractility through interacting with sarcoplasmic reticulum calcium ATPase type 2a signaling complexes in mouse heart. (semanticscholar.org)
- Cyclic GMP from the surrounding somatic cells regulates cyclic AMP and meiosis in the mouse oocyte. (semanticscholar.org)
Cardiac1
- Fluorescence resonance energy transfer-based analysis of cAMP dynamics in live neonatal rat cardiac myocytes reveals distinct functions of compartmentalized phosphodiesterases. (ox.ac.uk)
Mitogen-activa1
- We therefore evaluated the role of phosphoinositide 3-kinase (PI3K) and p42/p44 mitogen-activated protein kinase (p42/p44 MAPK) pathways in regulating this enzyme. (strath.ac.uk)
Phosphate2
- Two different types of low-density detergent-insoluble glycosphingolipid-enriched membrane domain (DIG) fractions were isolated from myelin by extraction with Triton X-100 (TX-100) in 50 mM sodium phosphate buffer at room temperature (20°C) (procedure 1), in contrast to a single low-density fraction obtained by extraction with TX-100 in Tris buffer containing 150 mM NaCl and 5 mM EDTA at 4°C (procedure 2). (wiley.com)
- Nucleoside 3',5'-cyclic phosphate + H 2 O = nucleoside 5'-phosphate. (uniprot.org)
Specificity1
- Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. (hmdb.ca)
Regulate2
Single nucleotide2
- Data indicate that genome-wide significant associations were found both at age 6 and 14 with single nucleotide polymorphisms (SNPs) on chromosome 11p15 in phosphodiesterase 3B, cGMP-inhibited protein PDE3B/cytochrome P-450 CYP2R1 genes. (nih.gov)
- A study of alveolar rhabdomyosarcoma copy number alterations by single nucleotide polymorphism analysis. (cancerindex.org)
20021
- 2002 Feb 15;46(3):278-86. (nih.gov)
Pathways2
- Here, we review recent developments in the understanding of the innate immune pathways that drive type I IFN responses in mycobacteria-infected host cells and the functional consequences for the host defense against M. tuberculosis , with a view that such insights might be exploited for the development of targeted host-directed immunotherapies and development of reliable biomarkers. (frontiersin.org)
- Nitric oxide sustains long-term skeletal muscle regeneration by regulating fate of satellite cells via signaling pathways requiring Vangl2 and cyclic GMP. (optistem.org)
Adipocytes1
- Phosphodiesterase (PDE) 3B, a major isoform of PDE in adipocytes, mediates the antilipolytic action of insulin. (elsevier.com)
Ischemic1
- In an in vivo dog model of myocardial stunning, ORM-3819 restored the depressed LV+dP/dt max and improved % segmental shortening (%SS) in the ischemic area (to 18.8±3), which was reduced after the ischaemia-reperfusion insult (from 24.1±2.1 to 11.0±2.4). (elsevier.com)
Receptor5
- however, published receptor binding data also support the potential L-type voltage- operated calcium channel (L-VOCC) blocking effect of drotaverine. (aspetjournals.org)
- We found that mice deficient in IL-17A, IL-17 receptor C (IL-17RC), and adaptor protein Act1 (of IL-17R) all had reduced demyelination accompanied by lessened microglial and polydendrocyte cellular reactivity compared with that in wild-type mice in response to cuprizone feeding, demonstrating the essential role of IL-17-induced Act1-mediated signaling in cuprizone-induced demyelination. (jneurosci.org)
- 8-Phenyltheophylline, an adenosine receptor antagonist in mammals, slightly retards memory decay in the wild-type. (springer.com)
- In the brain, two types of high‐affinity receptors bind glucocorticoids, the type I, mineralocorticoid receptor and the type II, glucocorticoid receptor (GR). Both receptor types are expressed by many types of neurons. (deepdyve.com)
- All known type I IFNs signal through a common receptor, IFNAR, which consists of the low-affinity IFNAR1 and the high-affinity IFNAR2 ( 11 , 12 ). (frontiersin.org)
Therapeutic2
- 2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. (axonmedchem.com)
- Zhang, K.Y. Keynote review: Phosphodiesterase-4 as a therapeutic target. (eurekaselect.com)
Activity6
- A quantitative model for the kinetics of cAMP-dependent protein kinase (type II) activity. (springer.com)
- However, when intact platelets were incubated with NO and then lysed, enhanced activity of phosphodiesterase type 5 was detected in the cytosol. (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)
- littermates, display an " activated" phenotype in vitro and in vivo and have an elevated level of cAMP phosphodiesterase (PDE) activity. (diabetesjournals.org)
- The activity of phosphodiesterase (PDE)3A requires divalent cations. (semanticscholar.org)
- In vitro, has a metal-dependent phosphodiesterase activity against 2',3'- cAMP and 2',3'-cGMP. (string-db.org)