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Cyclic Nucleotide Phosphodiesterases, Type 13',5'-Cyclic-AMP PhosphodiesterasesCyclic Nucleotide Phosphodiesterases, Type 4Cyclic Nucleotide Phosphodiesterases, Type 3Cyclic Nucleotide Phosphodiesterases, Type 2Phosphoric Diester Hydrolases2',3'-Cyclic-Nucleotide PhosphodiesterasesNucleotides, CyclicPhosphodiesterase Inhibitors3',5'-Cyclic-GMP PhosphodiesterasesCyclic Nucleotide Phosphodiesterases, Type 5Cyclic GMPCyclic Nucleotide Phosphodiesterases, Type 7Cyclic AMPRolipram1-Methyl-3-isobutylxanthinePurinonesIsoenzymesMolecular Sequence DataCalmodulinAmino Acid SequenceKineticsCyclic Nucleotide Phosphodiesterases, Type 6NucleotidesPhosphodiesterase 3 InhibitorsPhosphodiesterase 4 Inhibitors4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinoneDibutyryl Cyclic GMPTheophyllinePhosphodiesterase ICyclic Nucleotide-Gated Cation ChannelsPhosphorus-Oxygen LyasesMilrinoneBucladesinePyrrolidinonesAdenine NucleotidesCyclic AMP-Dependent Protein KinasesCyclic GMP-Dependent Protein KinasesAdenylate CyclaseSecond Messenger SystemsPapaverineCyclic IMPBase SequenceColforsinGuanylate CyclaseCloning, MolecularPolymorphism, Single NucleotidePhosphodiesterase 5 Inhibitors8-Bromo Cyclic Adenosine MonophosphateCalciumGuanine NucleotidesCattleHydrolysisIsoproterenolXanthinesBinding SitesCatalytic DomainSignal TransductionVinca AlkaloidsCyclic P-OxidesEnzyme ActivationSubstrate SpecificitySequence Homology, Amino Acid
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
A class of enzymes that catalyze the hydrolysis of one of the two ester bonds in a phosphodiester compound. EC 3.1.4.
2',3'-Cyclic-Nucleotide Phosphodiesterases
Nucleoside-2',3'-cyclic phosphate nucleotidohydrolase. Enzymes that catalyze the hydrolysis of the 2'- or 3'- phosphate bonds of 2',3'-cyclic nucleotides. Also hydrolyzes nucleoside monophosphates. Includes EC 3.1.4.16 and EC 3.1.4.37. EC 3.1.4.-.
Nucleotides, Cyclic
Phosphodiesterase Inhibitors
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
3',5'-Cyclic-GMP Phosphodiesterases
Enzymes that catalyze the hydrolysis of cyclic GMP to yield guanosine-5'-phosphate.
Cyclic Nucleotide Phosphodiesterases, Type 5
A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. It is found predominantly in vascular tissue and plays an important role in regulating VASCULAR SMOOTH MUSCLE contraction.
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
A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type exist, each with its own tissue localization. The isoforms are encoded by at least two genes and are a product of multiple alternative splicing of their mRNAs.
Cyclic AMP
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
Rolipram
A phosphodiesterase 4 inhibitor with antidepressant properties.
1-Methyl-3-isobutylxanthine
A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES
Purinones
Isoenzymes
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
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
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Kinetics
The rate dynamics in chemical or physical systems.
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
The monomeric units from which DNA or RNA polymers are constructed. They consist of a purine or pyrimidine base, a pentose sugar, and a phosphate group. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
Phosphodiesterase 3 Inhibitors
Compounds that specifically inhibit PHOSPHODIESTERASE 3.
Phosphodiesterase 4 Inhibitors
Compounds that specifically inhibit PHOSPHODIESTERASE 4.
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
Inhibitor of phosphodiesterases.
Dibutyryl Cyclic GMP
N-(1-Oxobutyl)-cyclic 3',5'-(hydrogen phosphate)-2'-butanoate guanosine. A derivative of cyclic GMP. It has a higher resistance to extracellular and intracellular phosphodiesterase than 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
A phosphoric diester hydrolase that removes 5'-nucleotides from the 3'-hydroxy termini of 3'-hydroxy-terminated OLIGONUCLEOTIDES. It has low activity towards POLYNUCLEOTIDES and the presence of 3'-phosphate terminus on the substrate may inhibit hydrolysis.
Cyclic Nucleotide-Gated Cation Channels
A subgroup of cyclic nucleotide-regulated ION CHANNELS within the superfamily of pore-loop cation channels. They are expressed in OLFACTORY NERVE cilia and in PHOTORECEPTOR CELLS and some PLANTS.
Phosphorus-Oxygen Lyases
Enzymes that catalyze the cleavage of a phosphorus-oxygen bond by means other than hydrolysis or oxidation. EC 4.6.
Milrinone
A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase type 3 activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the inotropic potency of amrinone.
Bucladesine
A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
Pyrrolidinones
A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed)
Adenine Nucleotides
Cyclic AMP-Dependent Protein Kinases
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
Cyclic GMP-Dependent Protein Kinases
A group of cyclic GMP-dependent enzymes that catalyze the phosphorylation of SERINE or THREONINE residues of proteins.
Adenylate Cyclase
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
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
Inosine cyclic 3',5'-(hydrogen phosphate). An inosine nucleotide which acts as a mild inhibitor of the hydrolysis of cyclic AMP and cyclic GMP and as an inhibitor of cat heart cyclic AMP phosphodiesterase.
Base Sequence
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide 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
An enzyme that catalyzes the conversion of GTP to 3',5'-cyclic GMP and pyrophosphate. It also acts on ITP and dGTP. (From Enzyme Nomenclature, 1992) EC 4.6.1.2.
Cloning, Molecular
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Polymorphism, Single Nucleotide
A single nucleotide variation in a genetic sequence that occurs at appreciable frequency in the population.
Phosphodiesterase 5 Inhibitors
Compounds that specifically inhibit PHOSPHODIESTERASE 5.
8-Bromo Cyclic Adenosine Monophosphate
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
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.
Guanine Nucleotides
Cattle
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
Hydrolysis
The process of cleaving a chemical compound by the addition of a molecule of water.
Isoproterenol
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
Xanthines
Purine bases found in body tissues and fluids and in some plants.
Binding Sites
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Catalytic Domain
The region of an enzyme that interacts with its substrate to cause the enzymatic reaction.
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
A group of indole-indoline dimers which are ALKALOIDS obtained from the VINCA genus of plants. They inhibit polymerization of TUBULIN into MICROTUBULES thus blocking spindle formation and arresting cells in METAPHASE. They are some of the most useful ANTINEOPLASTIC AGENTS.
Cyclic P-Oxides
Enzyme Activation
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
Substrate Specificity
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
Sequence Homology, Amino Acid
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.

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)

Role of cGMP-inhibited phosphodiesterase and sarcoplasmic calcium in mediating the increase in basal heart rate with nitric...
Nitric oxide (NO) donors increase heart rate (HR) through a guanylyl cyclase-dependent stimulation of the pacemaker current I(f), without affecting basal I(Ca-L). The activity of I(f)is known to be enhanced by cyclic nucleotides and by an increase in cytosolic Ca(2+). We examined the role of cGMP-dependent signaling pathways and intracellular Ca(2+)stores in mediating the positive chronotropic effect of NO donors. In isolated guinea pig atria, the increase in HR in response to 1-100 micromol/l 3-morpholino-sydnonimine (SIN-1; with superoxide dismutase, n=6) or diethylamine-NO (DEA-NO, n=8) was significantly attenuated by blockers of the cGMP-inhibited phosphodiesterase (PDE3; trequinsin, milrinone or Ro-13-6438, n=22). In addition, the rate response to DEA-NO or sodium nitroprusside (SNP) was significantly reduced following inhibition of PKA (KT5720 or H-89, n=15) but not PKG (KT5728 or Rp-8-pCPT-cGMPs, n=16). Suppression of sarcoplasmic (SR) Ca(2+)release by pretreatment of isolated atria with
https://www.camsoxford.ox.ac.uk/coi-publications/publications/104881
Oral Dosage Form Containing A PDE 4 Inhibitor As An Active Ingredient And Polyvinylpyrrolidone As Excipient - Patent...Oral Dosage Form Containing A PDE 4 Inhibitor As An Active Ingredient And Polyvinylpyrrolidone As Excipient - Patent...
0139] The dosage forms of the invention can be employed for the treatment and prevention of all diseases regarded as treatable or preventable through the use of PDE 4 inhibitors. Selective cyclic nucleotide phosphodiesterase (PDE) inhibitors (specifically of type 4) are suitable on the one hand as bronchial therapeutic agents (for the treatment of airway obstructions owing to their dilating effect but also owing to their effect increasing the respiratory rate and respiratory drive) and for eliminating erectile dysfunction owing to the vasodilating effect, but on the other hand especially for the treatment of disorders, especially of an inflammatory nature, e.g. of the airways (asthma prophylaxis), of the skin, of the central nervous system, of the intestine, of the eyes and of the joints, which are promoted by mediators such as histamine, PAF (platelet-activating factor), arachidonic acid derivatives such as leukotrienes and prostaglandins, cytokines, interleukins, chemokines, alpha-, beta- and ...
http://www.patentsencyclopedia.com/app/20110251244
Phosphodiesterases in neuronal function (Homo sapiens) - WikiPathwaysPhosphodiesterases in neuronal function (Homo sapiens) - WikiPathways
Minami N, Suzuki Y, Yamamoto M, Kihira H, Imai E, Wada H, Kimura Y, Ikeda Y, Shiku H, Nishikawa M.; Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo.; Life Sci. , 1997 PubMed Europe PMC ...
https://www.wikipathways.org/index.php?title=Pathway:WP4222&direction=prev&oldid=96808
Single-step affinity purification, partial structure and properties of human platelet cGMP inhibited cAMP phosphodiesterase |...Single-step affinity purification, partial structure and properties of human platelet cGMP inhibited cAMP phosphodiesterase |...
The human platelet cilostamide- and cGMP-inhibited cAMP phosphodiesterase (cGI-PDE) was rapidly purified approximately 19,000-fold to apparent homogeneity using single step affinity chromatography on the isothiocyanate derivative of cilostamide coupled to aminoethyl agarose. Within 24 h, 30 micrograms of enzyme protein was obtained from 20 ml of packed platelets. Vmax for cAMP and cGMP was 6.1 and 0.9 mumol/min per mg protein, respectively. Several polypeptides (110/105, 79, 62, 55/53 kDa) were identified after SDS-PAGE, all of which were immunologically related to cGI-PDE and represented approx. 5, 20, 50 and 20% of the total protein, respectively. Limited proteolysis of the cGI-PDE with chymotrypsin produced a major fragment of approximately 47 kDa (and at least two smaller peptides) with catalytic activity and sensitivity to cGMP and OPC 3911 similar to controls. Phosphorylation of the cGI-PDE by cAMP-dependent protein kinase (A-kinase) resulted in maximal incorporation of 0.6-1.8 mol of ...
https://www.ludc.lu.se/eva-degerman-pi/publication/39c35772-631e-4a60-a666-f89be7efcdf2
Intracellular cAMP levels are higher in LDLR-/−p110γ | Open-iIntracellular cAMP levels are higher in LDLR-/−p110γ | Open-i
Intracellular cAMP levels are higher in LDLR-/−p110γ−/− than in LDLR−/−p110γ+/−macrophages.LDLR−/−p110γ+/− and LDLR−/−p110γ−/− BMM
https://openi.nlm.nih.gov/detailedresult.php?img=PMC3750002_pone.0072674.g004&req=4
Re-discovering PDE3 inhibitors - New opportunities for a long neglected target | Lund University Diabetes CentreRe-discovering PDE3 inhibitors - New opportunities for a long neglected target | Lund University Diabetes Centre
The PDE3 enzymes or low Kin cGMP-inhibited phosphodiesterases have long been established as important mediators of cellular physiology, and synthetic PDE3 inhibitors have been critical to the delineation of the enzymes roles. Yet despite decades of progress on the biology of these enzymes, the medicinal chemistry landscape relating to PDE3 inhibitors has remained essentially unchanged since the mid 1990s. Up until then the field was at the cutting edge of drug design; without the tools of molecular and structural biology, molecules of high potency were being achieved using logical pharmacophore models and lead modification. Yet virtually all the impetus went out of this area on the back of failures at the clinic and PDE3 as a therapeutic target largely fell out of favour. A decade later and with the new technologies of structural and molecular biology breathing new life into PDE3 research in general, PDE3 inhibitors are sought for target validation in an array of therapeutic applications. ...
https://www.ludc.lu.se/eva-degerman-pi/publication/c9617d4a-51d8-4376-a9d4-34b35370c703
olprinone | Semantic Scholarolprinone | Semantic Scholar
We investigated the inotropic effect of SCH00013 (4, 5-dihydro-6-[1-[2-hydroxy-2-(4-cyanophenyl)ethyl]-1,2,5, 6-tetrahydropyrido… Expand ...
https://www.semanticscholar.org/topic/olprinone/555663
Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic...Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic...
TY - JOUR. T1 - Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic leukemia. AU - Zhang, Lingzhi. AU - Murray, Fiona. AU - Zahno, Anja. AU - Kanter, Joan R.. AU - Chou, Daisy. AU - Suda, Ryan. AU - Fenlon, Michael. AU - Rassenti, Laura. AU - Cottam, Howard. AU - Kipps, Thomas J.. AU - Insel, Paul A.. PY - 2008/12/9. Y1 - 2008/12/9. N2 - Cyclic nucleotide phosphodiesterase (PDE) isoforms can influence disease pathogenesis and be novel therapeutic targets. Because lower cAMP levels may contribute to the decreased apoptosis that occurs in chronic lymphocytic leukemia (CLL), we assessed the expression levels of PDE isoforms in peripheral blood mononuclear cells (PBMC) of healthy adults and patients with CLL. We found a unique PDE mRNA signature in CLL: higher levels than in normal PBMC of PDE7B (increased approximate to 23-fold) and lower levels of PDE3B, 4D, 5A, and 9A mRNA (each decreased approximate to 30-fold). Increased ...
https://abdn.pure.elsevier.com/en/publications/cyclic-nucleotide-phosphodiesterase-profiling-reveals-increased-e
Phosphodiesterase III Inhibition Increases cAMP levels and augments the infarct size limiting effect of a dpp-4 inhibitor in...Phosphodiesterase III Inhibition Increases cAMP levels and augments the infarct size limiting effect of a dpp-4 inhibitor in...
TY - JOUR. T1 - Phosphodiesterase III Inhibition Increases cAMP levels and augments the infarct size limiting effect of a dpp-4 inhibitor in mice with type-2 diabetes mellitus. AU - Birnbaum, Yochai. AU - Castillo, Alexander C.. AU - Qian, Jinqiao. AU - Ling, Shukuan. AU - Ye, Hongmei. AU - Perez-Polo, Jose R.. AU - Bajaj, Mandeep. AU - Ye, Yumei. PY - 2012/12/1. Y1 - 2012/12/1. N2 - Purpose We assessed whether phosphodiesterase-III inhibition with cilostazol (Cil) augments the infarct size (IS)-limiting effects of MK0626 (MK), a dipeptidyl-peptidase-4 (DPP4) inhibitor, by increasing intracellular cAMP in mice with type-2 diabetes. Methods Db/Db mice received 3-day MK (0, 1, 2 or 3 mg/kg/d) with or without Cil (15 mg/kg/d) by oral gavage and were subjected to 30 min coronary artery occlusion and 24 h reperfusion. Results Cil and MK at 2 and 3 mg/kg/d significantly reduced IS. Cil and MK had additive effects at all three MK doses. IS was the smallest in the MK-3+Cil. MK in a dose dependent manner ...
https://researchexperts.utmb.edu/en/publications/phosphodiesterase-iii-inhibition-increases-camp-levels-and-augmen
cGMP-inhibited phosphodiesterases (PDE3 gene family) | Biochemical Society TransactionscGMP-inhibited phosphodiesterases (PDE3 gene family) | Biochemical Society Transactions
Thank you for your interest in spreading the word about Biochemical Society Transactions.. NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.. ...
http://www.biochemsoctrans.org/content/24/4/1010
Items where Department is Biomedical & Life Sciences and Year is 2014 - Lancaster EPrintsItems where Department is Biomedical & Life Sciences and Year is 2014 - Lancaster EPrints
MacPherson, Tara and Armstrong, Jane and Criddle, David and Wright, Karen (2014) Physiological intestinal oxygen modulates the Caco-2 cell model and increases sensitivity to the phytocannabinoid cannabidiol. In Vitro Cellular and Developmental Biology - Animal, 50 (5). pp. 417-426. ISSN 1071-2690 Maki, Takakuni and Okamoto, Yoko and Carare, Roxana O. and Hase, Yoshiki and Hattori, Yorito and Hawkes, Cheryl A. and Saito, Satoshi and Yamamoto, Yumi and Terasaki, Yasukazu and Ishibashi-Ueda, Hatsue and Taguchi, Akihiko and Takahashi, Ryosuke and Miyakawa, Taihei and Kalaria, Raj N. and Lo, Eng H. and Arai, Ken and Ihara, Masafumi (2014) Phosphodiesterase III inhibitor promotes drainage of cerebrovascular β-amyloid. Annals of Clinical and Translational Neurology, 1 (8). pp. 519-533. ISSN 2328-9503 Mann, Elizabeth R. and Bernardo, David and Ng, Siew C. and Rigby, Rachael J. and Al-hassi, Hafid O. and Landy, Jon and Peake, Simon T. C. and Spranger, Henning and English, Nicholas R. and Thomas, Linda ...
https://eprints.lancs.ac.uk/view/divisions/ham=5Fbmls/2014.html
116355-08-9,Olprinone,Olprinone intermediates,Imidazo[1,2-a]Pyridin - Nanjing King-Pharm Co., Ltd.116355-08-9,Olprinone,Olprinone intermediates,Imidazo[1,2-a]Pyridin - Nanjing King-Pharm Co., Ltd.
Nanjing King-Pharm Co., Ltd. Supply 1-(Imidazo[1,2-a]Pyridin-6-yl)Propan-2-One,CAS No: 116355-08-9,Olprinone,Olprinone intermediates,Imidazo[1,2-a]Pyridin。
http://king-pharm.com/info.asp?casno=116355-08-9&1-%20
Elizabeth A. Bowles , NC DOCKS (North Carolina Digital Online Collection of Knowledge and Scholarship)
Background Within erythrocytes (RBCs), cAMP levels are regulated by phosphodiesterases (PDEs). Increases in cAMP and ATP release associated with activation of ß-adrenergic receptors (ßARs) and prostacyclin receptors (IPRs) are regulated by PDEs 2, 4 ...
https://libres.uncg.edu/ir/clist.aspx?id=13172
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http://www.abcam.cn/recombinant-mouse-pde5a-protein-ab80330.html
2020 Cyclic Nucleotide Phosphodiesterases (GRS) Seminar GRC2020 Cyclic Nucleotide Phosphodiesterases (GRS) Seminar GRC
The 2020 Gordon Research Seminar on Cyclic Nucleotide Phosphodiesterases (GRS) will be held in Les Diablerets, Switzerland. Apply today to reserve your spot.
https://www.grc.org/cyclic-nucleotide-phosphodiesterases-grs-conference/2020/
JoVE Search Results: Cyclic Nucleotide Phosphodiesterases%2C Type 5
Adenosine, Magnesium, Kinase, Protein Kinase, Mitosis, Memory, Learning, Mice, Brain, Hippocampus, Bone, Bone Marrow, Cell, and Cell Cycle
http://labindex.jove.com/group/Cyclic-Nucleotide-Phosphodiesterases%2C-Type-5
West anthony r cyclic nucleotide phosphodiesterases in the central nervous system from biology to dru - найти leaguechampions.ruWest anthony r cyclic nucleotide phosphodiesterases in the central nervous system from biology to dru - найти leaguechampions.ru
Emphasizes the integration of major areas of drug discovery and their importance in candidate evaluation It is believed that selecting the «right» drug candidate for development is the key to success. In the last decade, pharmaceutical R&D departments have integrated pharmacokinetics and drug metabolism, pharmaceutics, and toxicology into early drug discovery to improve the assessment of potential drug compounds. Now, Evaluation of Drug Candidates for Preclinical Development provides a complete view and understanding of why absorption-distribution-metabolism-excretion-toxicology (ADMET) plays a pivotal role in drug discovery and development. Encompassing the three major interrelated areas in which optimization and evaluation of drug developability is most critical-pharmacokinetics and drug metabolism, pharmaceutics, and safety assessment-this unique resource encourages integrated thinking in drug discovery. The contributors to this volume: Cover drug transporters, cytochrome P-450 and ...
http://leaguechampions.ru/west-anthony-r-cyclic-nucleotide-phosphodiesterases-in-the-central-nervous-system-from-biology-to-drug-discovery/
Hormones, male infertility, spermatogenesis.
The PDE7B gene encodes 35-cyclic nucleotide phosphodiesterase (PDE) and a known target in cognitive impairments. Therefore, it is of interest to design and development of potential inhibitors with PDE7B with improved binding features. We document that the amino acid residues such as H186, K190, and G113 of PDE7B protein showed crucial interactions with aspirin for further consideration in this context.
http://www.bioinformation.net/016/97320630016183.htm
Non-adrenergic Vasoactives · Part One
Key non-adrenergic cardiovascular drugs include vasopressin (and its analogues, teripressin and ornipressin), phosphodiesterase III inhibitors such as milrinone, and calcium sensitisers such as levosimendan.. ...
http://www.partone.lifeinthefastlane.com/non-adrenergic_drugs.html
JCI - WelcomeJCI - Welcome
Since cAMP blocks meiotic maturation of mammalian and amphibian oocytes in vitro and cyclic nucleotide phosphodiesterase 3A (PDE3A) is primarily responsible for oocyte cAMP hydrolysis, we generated PDE3A-deficient mice by homologous recombination. The Pde3a-/- females were viable and ovulated a normal number of oocytes but were completely infertile, because ovulated oocytes were arrested at the germinal vesicle stage and, therefore, could not be fertilized. Pde3a-/- oocytes lacked cAMP-specific PDE activity, contained increased cAMP levels, and failed to undergo spontaneous maturation in vitro (up to 48 hours). Meiotic maturation in Pde3a-/- oocytes was restored by inhibiting protein kinase A (PKA) with adenosine-3′,5′-cyclic monophosphorothioate, Rp-isomer (Rp-cAMPS) or by injection of protein kinase inhibitor peptide (PKI) or mRNA coding for phosphatase CDC25, which confirms that increased cAMP-PKA signaling is responsible for the meiotic blockade. Pde3a-/- oocytes that underwent germinal ...
https://www.jci.org/tags/37?content=articles&page=5
Stimulation of mitochondrial biogenesis through induction of cGMP promotes recovery of mitochondrial and renal function...
Mitochondrial damage and dysfunction are major pathophysiological mechanisms underlying acute kidney injury (AKI). Following various forms of AKI, mitochondrial biogenesis, the de novo generation of new, functional mitochondria, is suppressed. Pharmacological stimulation of PPARγ-coactivator-1α (PGC-1α), the master regulator of mitochondrial biogenesis, promotes recovery of mitochondrial and renal function after AKI. The primary goals of this project were the evaluation of renal cGMP as a modulator of mitochondrial biogenesis in AKI, and the assessment of phosphodiesterase (PDE) inhibitors and guanylyl cyclase (GC) activators as novel agents to induce mitochondrial biogenesis and promote renal recovery. cGMP has been demonstrated to stimulate mitochondrial biogenesis and function. Both cGMP generation through guanylyl cyclase and degradation through PDEs are highly regulated processes. Compounds that regulate cGMP levels, including the PDE3 inhibitors cilostamide and trequinsin, and the PDE5 ...
http://digital.library.musc.edu/cdm/singleitem/collection/mtd/id/906/rec/5
Stimulation of mitochondrial biogenesis through induction of cGMP promotes recovery of mitochondrial and renal function...
Mitochondrial damage and dysfunction are major pathophysiological mechanisms underlying acute kidney injury (AKI). Following various forms of AKI, mitochondrial biogenesis, the de novo generation of new, functional mitochondria, is suppressed. Pharmacological stimulation of PPARγ-coactivator-1α (PGC-1α), the master regulator of mitochondrial biogenesis, promotes recovery of mitochondrial and renal function after AKI. The primary goals of this project were the evaluation of renal cGMP as a modulator of mitochondrial biogenesis in AKI, and the assessment of phosphodiesterase (PDE) inhibitors and guanylyl cyclase (GC) activators as novel agents to induce mitochondrial biogenesis and promote renal recovery. cGMP has been demonstrated to stimulate mitochondrial biogenesis and function. Both cGMP generation through guanylyl cyclase and degradation through PDEs are highly regulated processes. Compounds that regulate cGMP levels, including the PDE3 inhibitors cilostamide and trequinsin, and the PDE5 ...
http://digital.library.musc.edu/cdm/singleitem/collection/mtd/id/906/rec/7
Genetically Encoded Biosensors Reveal PKA Hyperphosphorylation on the Myofilaments in Rabbit Heart FailureNovelty and...Genetically Encoded Biosensors Reveal PKA Hyperphosphorylation on the Myofilaments in Rabbit Heart FailureNovelty and...
A tonic PKA activity is maintained by adenylyl cyclase-dependent cAMP production and PDE-dependent cAMP hydrolysis.19,26 Our results show that PDE4 is the major enzyme that controls local PKA activity along the sarcolemma, whereas PDE3 mediates primarily cAMP hydrolysis on the myofilaments (Figure 5). In agreement, both PDE4D and PDE4B display overlap with the membrane marker caveolin-3 (Online Figure II), consistent with a recent report showing that both enzymes have a binding motif to caveolin-3;27 loss of caveolin-3 may lead to loss of PDE4 activity at the sarcolemma. In contrast, PDE3 displays a colocalization with myofibrils (Online Figure II), supporting its primary role in controlling local cAMP and PKA activity there (Figure 5). Meanwhile, we observe a high tonic PKA activity on the myofilaments, which is consistent with a relatively high PKA phosphorylation of myosin-binding protein C and TnI in healthy cardiac tissues.28. Although the PKA activity is usually depressed in the late stage ...
http://circres.ahajournals.org/content/119/8/931
Emerging therapies for severe asthma | BMC Medicine | Full TextEmerging therapies for severe asthma | BMC Medicine | Full Text
A number of novel drugs under development may prove to have a role in the management of asthma. Phosphodiesterase (PDE)4 inhibitors have immunomodulatory effects over a number of inflammatory cells potentially relevant to the treatment of severe asthma [56]. High doses of phosphodiesterase (PDE)4 inhibitors may be necessary to treat severe asthma, and gastro-intestinal side effects may limit their use [56-58], although inhaled PDE4 inhibitors may improve their therapeutic index [59, 60]. Inhibition of protein kinases such as p38 mitogen-activated protein kinase (MAPK) and other tyrosine kinases involved in cellular signalling of pro-inflammatory cytokines may have a role in the treatment of severe asthma [61-63]. For example, a phase 3 study evaluating a tyrosine kinase inhibitor of the c-KIT receptor masitinib commenced recently.. Several drugs licensed for treating other conditions may also have a role in the management of asthma. In a randomized controlled trial of 58 patients with severe ...
https://0-bmcmedicine-biomedcentral-com.brum.beds.ac.uk/articles/10.1186/1741-7015-9-102
JCI - Deletion of phosphodiesterase 4D in mice shortens α2-adrenoceptor-mediated anesthesia, a behavioral correlate of emesisJCI - Deletion of phosphodiesterase 4D in mice shortens α2-adrenoceptor-mediated anesthesia, a behavioral correlate of emesis
The administration of many PDE4 inhibitors has been associated with the side effect of nausea and vomiting. These debilitating adverse events are a significant issue in the therapeutic use of PDE4 inhibitors. Consequently the improvement of the therapeutic window of new generations of PDE4 inhibitors has been a major challenge. It has been previously suggested that the activity on the HARBS of PDE4 correlates with the side effects of emesis and that, hence, PDE4 inhibitors exhibiting a reduced activity on this conformer should have attenuated side effects (13, 15, 31). However, it has now been clarified that the HARBS coincides with the holoenzyme responsible for PDE4 catalysis (11, 12).. An alternative approach to improving the therapeutic index of new generations of PDE4 inhibitors would be to design PDE4 subtype-selective inhibitors, if it could be shown that nausea and vomiting are dependent on a specific PDE4 subtype. The recent demonstration that the emetic potential of PDE4 inhibitors can ...
https://www.jci.org/articles/view/15506
Alteration of vascular reactivity in heart failure: role of phosphodiesterases 3 and 4. | Sigma-AldrichAlteration of vascular reactivity in heart failure: role of phosphodiesterases 3 and 4. | Sigma-Aldrich
Sigma-Aldrich offers abstracts and full-text articles by [F Hubert, M Belacel-Ouari, B Manoury, K Zhai, V Domergue-Dupont, P Mateo, F Joubert, R Fischmeister, V Leblais].
http://www.sigmaaldrich.com/catalog/papers/25048877
Download Cyclic Nucleotide Phosphodiesterases In The Central Nervous System: From Biology To Drug Discovery 2014Download Cyclic Nucleotide Phosphodiesterases In The Central Nervous System: From Biology To Drug Discovery 2014
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Impact of Cilostazol on Restenosis After Percutaneous Coronary Balloon Angioplasty | CirculationImpact of Cilostazol on Restenosis After Percutaneous Coronary Balloon Angioplasty | Circulation
One of the mechanisms by which cilostazol reduces restenosis after PTCA is thought to be inhibition of neointimal proliferation, considered a major mechanism of restenosis after PTCA caused by SMC migration, proliferation, and matrix synthesis.3 4 22 SMC migration and proliferation are induced by growth factors released from activated platelets. As an antiplatelet medication, cilostazol controls the induction by platelet-derived growth factors.12 13 23 More importantly, cilostazol is thought to directly inhibit SMC growth. In vitro studies involving rat aortic smooth muscle cell cultures have shown that increasing the concentration of cilostazol resulted in an increase of intracellular cAMP and a decrease of 3H-thymidine uptake,23 suggesting that phosphodiesterase III inhibitors inhibit SMC growth by affecting its deoxyribonucleic acid, thereby controlling its cell proliferation.24 This direct inhibition of SMC proliferation is considered to be the main contributor to the significant reduction ...
http://circ.ahajournals.org/content/100/1/21
Publications : CRDSI
In mammals, adenosine 3, 5-cyclic monophosphate (cAMP) is known to play highly important roles in sperm motility and acrosomal exocytosis. It is known to act through protein phosphorylation via PRKA and through the activation of guanine nucleotide exchange factors like EPAC. Sperm intracellular cAMP levels depend on the activity of adenylyl cyclases, mostly SACY, though transmembrane-containing adenylyl cyclases are also present, and on the activity of cyclic nucleotide phosphodiesterases (PDE) whose role is to degrade cAMP into 5-AMP. The PDE superfamily is subdivided into 11 families (PDE1 to 11), which act on either cAMP or cGMP, or on both cAMP and cGMP although with different enzymatic properties. PDE10, which is more effective on cAMP than cGMP, has been known for almost 15 years and is mostly studied in the brain where it is associated with neurological disorders. Although a high level of PDE10A gene expression is observed in the testis, information on the identity of the isoforms or ...
https://www.crdsi.ulaval.ca/la-recherche/publications/afficher_publication/details/identification-and-localization-of-the-cyclic-nucleotide-phosphodiesterase-10a-in-bovine-testis-and/
Reciprocal regulation of calcium dependent and calcium independent cyclic AMP hydrolysis by protein phosphorylationReciprocal regulation of calcium dependent and calcium independent cyclic AMP hydrolysis by protein phosphorylation
The hydrolysis of cyclic nucleotide second messengers takes place through multiple cyclic nucleotide phosphodiesterases (PDEs). The significance of this diversification is not fully understood. Here we report the differential regulation of low K(m) Ca2+-activated (PDE1C) and Ca2+-independent, rolipr …
https://pubmed.ncbi.nlm.nih.gov/12065651/?dopt=Abstract
Moracin M | Phosphodiesterase (PDE) Inhibitor | MedChemExpressMoracin M | Phosphodiesterase (PDE) Inhibitor | MedChemExpress
Moracin M, a phenolic component in the skin of Morus alba L., is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity. - Mechanism of Action & Protocol.
https://www.medchemexpress.com/moracin-m.html
Effects of Roflumilast on Insulin and Blood Sugar Levels in Prediabetic Overweight and Obese Individuals - Tabular View -...Effects of Roflumilast on Insulin and Blood Sugar Levels in Prediabetic Overweight and Obese Individuals - Tabular View -...
Resveratrol, a polyphenol most notably found in red wine has anti-aging properties in mice fed a high-fat diet; resveratrol protects against obesity and type 2 diabetes. Several clinical trials have been conducted to study the metabolic effects of resveratrol. Although these trials have used different subject groups (e.g. obese healthy, type 2 diabetics or older adults with glucose intolerance), they suggest that resveratrol may improve insulin sensitivity. However, the therapeutic potential of resveratrol is diminished by the fact that it has a very promiscuous target profile. In order to translate resveratrol biology into clinical application, it is helpful to identify the cellular target(s) of resveratrol that mediate the desired effects and to develop therapies specific for that target(s). Recently, we discovered that the metabolic effects of resveratrol appear to result from competitive inhibition of cAMP-degrading phosphodiesterases (PDEs), which increases cAMP levels. The cAMP-dependent ...
https://clinicaltrials.gov/ct2/show/record/NCT01862029?term=Prediabetes&lup_s=07%2F14%2F2013&lup_d=14&show_rss=Y&sel_rss=mod14
HD Biosciences Co., Ltd.
cAMP PDEs are emerging as a promising class of drug targets in asthma and cardiovascular disease therapeutic areas. HDB has established the cell-based screening assay for cAMP phosphodiesterase (PDE) inhibitors in HDB based on the Codex ACTOne™ technology. The specificity of the assay has been verified by known PDE inhibitors. Only PDE4 and pan-PDE inhibitors showed positive signals in the cell line that was optimized ...
http://www.hdbiosciences.com/EngOtherEnzyme.htm
Specific CD3{varepsilon} Epsilon Association of a Phosphodiesterase 4B by Miren L. Baroja, Lenora B. Cieslinski et al.Specific CD3{varepsilon} Epsilon Association of a Phosphodiesterase 4B by Miren L. Baroja, Lenora B. Cieslinski et al.
cAMP-specific phosphodiesterases (PDE) comprise an extensive family of enzymes that control intracellular levels of cAMP and thus regulate T cell responses. It is not known how the function of these enzymes is altered by TCR engagement. We have examined this issue by studying one of the PDE isozymes (PDE4B). PDE4B RNA and protein were detected in resting PBLs, and the levels of PDE4B protein increased with cell cycling. In peripheral blood T cells, two previously reported PDE4B isoforms could be detected: one was 75-80 kDa (PDE4B1) and the other was 65-67 kDa (PDE4B2). These two isoforms differed in their N-terminal sequence, with the presence of four potential myristylation sites in the PDE4B2 that are absent in PDE4B1. Consequently, only PDE4B2 was found in association with the CD3{varepsilon} chain of the TCR. In addition, although both isoforms were phosphorylated in tyrosines in pervanadate-stimulated T cells, only the TCR-associated PDE4B2 was tyrosine-phosphorylated following CD3 ligation. The
https://ir.lib.uwo.ca/immunologypub/50/
CAMP - The School of Biomedical Sciences Wiki
Cyclic AMP (cAMP) or cyclic adenosine monophosphate acts as a secondary messenger and is used in cell signalling. The concentration of cAMP in cytosol can be increased via an extracellular signal. It can be deactivated by phosphodiesterase (PDE) into AMP. In most animal cells, cAMP can activate protein kinase A (PKA) by binding to its regulatory subunits which activates and release its active catalytic subunits. These active catalytic subunits can then go on to phosphorylate other proteins, creating a signalling cascade[1]. In unstimulated cells, levels of cAMP are kept low by phosphodiesterases in order to keep the bound inactive[2]. ATP is converted to cAMP by adenylyl cyclase, cAMP is then used in a range of signalling pathways. ...
https://teaching.ncl.ac.uk/bms/wiki/index.php?title=CAMP&oldid=15500
Pde10 inhibitors and compositions containing them and methods
EXAMPLE 66. ANALYSIS of CONNECTIONS. PDE 10 biochemical analysis. Fosfodiesterazu (PDE) analysis was performed using recombinant human PDE 1A3, 2A3, 3 catalytic phase, 4 catalytic site, 5 catalytic site, 7A, 8A, 9A2, 10A1 11A1 and the enzymes expressed in a baculovirus system using Sf9 cells. PDE activity was measured using a modification of the two-stage method of Thompson and Appleman, described above, which is adapted to format 96-well plates. The effect of PDE inhibitors was determined by study of a fixed amount of enzyme in the presence of concentrations of the test compounds and concentrations of the substrate is smaller than Kmso that Ki was equal to IC50. The final volume for analysis was 110 μl with buffer (10 mm MgCl2; 40 mm Tris·HCl; pH 7,4). The reaction was started with the enzyme and withstood C (3H)-�stratum and substance for 20 minutes at 30°C. The reaction was stopped by denaturation of the enzyme (heating the reaction mixture at 70°C for 2 minutes). Then the reaction ...
http://russianpatents.com/patent/254/2545456.html
Mardepodect (PF-2545920) | ≥99%(HPLC) | Selleck | PDE inhibitor ...Mardepodect (PF-2545920) | ≥99%(HPLC) | Selleck | PDE inhibitor ...
PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM. Find all the information about PF-2545920 for cell signaling research.
https://www.selleckchem.com/products/pf-2545920.html
OriGene - PDE8B (NM 001029854) cDNA CloneOriGene - PDE8B (NM 001029854) cDNA Clone
PDE8B - PDE8B (untagged)-Human phosphodiesterase 8B (PDE8B), transcript variant 2 available for purchase from OriGene - Your Gene Company.
http://www.origene.com/cdna/trueclone/accession/NM_001029854/SC302441.aspx
PDE4B - WikipediaPDE4B - Wikipedia
cAMP-specific 3,5-cyclic phosphodiesterase 4B is an enzyme that in humans is encoded by the PDE4B gene. This gene is a member of the type IV, cyclic AMP (cAMP)-specific, cyclic nucleotide phosphodiesterase (PDE) family. Cyclic nucleotides are important second messengers that regulate and mediate a number of cellular responses to extracellular signals, such as hormones, light, and neurotransmitters. The cyclic nucleotide phosphodiesterases (PDEs) regulate the cellular concentrations of cyclic nucleotides and thereby play a role in signal transduction. This gene encodes a protein that specifically hydrolyzes cAMP. Alternate transcriptional splice variants, encoding different isoforms, have been characterized. Altered activity of this protein has been associated with schizophrenia and bipolar disorder. PDE4B is believed to be the PDE4 subtype involved in the antipsychotic effects of PDE4 inhibitors such as rolipram. PDE4B is involved in dopamine-associated and stress-related behaviours. It has ...
https://en.wikipedia.org/wiki/PDE4B
Identification of human PDE7B, a cAMP-specific phosphodiesteraseIdentification of human PDE7B, a cAMP-specific phosphodiesterase
We isolated a human cAMP-specific phosphodiesterase (PDE7B) cDNA from human caudate nucleus. The human PDE7B was composed of 450 amino acid residues with a molecular mass of 51,835 Da. The deduced amino acid sequence of human PDE7B was 64.1% identical to that of human PDE7A (67.1% identity in the ca …
https://pubmed.ncbi.nlm.nih.gov/10814504/?dopt=Abstract
Chen Yan, Ph.D. - University of Rochester Medical CenterChen Yan, Ph.D. - University of Rochester Medical Center
General Research Interests: Regulation and function of cyclic nucleotide phosphodiesterases in the cardiovascular system. Second messenger cyclic nucleotides (cAMP and cGMP) regulate many signaling pathways in the cardiovascular system. For example, the vascular tone, smooth muscle cell growth, and cardiac muscle contractility are all regulated by cyclic nucleotide signaling. We are interested in phosphodiesterases (PDEs), the enzymes that break down cyclic nucleotides and thus control the amplitude, duration, and compartmentalization of cyclic nucleotide signaling in the cell. It has become increasingly clear that cyclic nucleotide degradation by PDEs is not a constitutive function of the cell, but rather a highly regulated one controlled by different mechanisms in different physiological and pathological circumstances. PDE regulation and function is further complicated by the fact that there are more than 50 individual PDEs belonging to 11 different PDE families, yet our understanding of the ...
https://www.urmc.rochester.edu/people/23115996-chen-yan/researchers
Chen Yan, Ph.D. - University of Rochester Medical CenterChen Yan, Ph.D. - University of Rochester Medical Center
General Research Interests: Regulation and function of cyclic nucleotide phosphodiesterases in the cardiovascular system. Second messenger cyclic nucleotides (cAMP and cGMP) regulate many signaling pathways in the cardiovascular system. For example, the vascular tone, smooth muscle cell growth, and cardiac muscle contractility are all regulated by cyclic nucleotide signaling. We are interested in phosphodiesterases (PDEs), the enzymes that break down cyclic nucleotides and thus control the amplitude, duration, and compartmentalization of cyclic nucleotide signaling in the cell. It has become increasingly clear that cyclic nucleotide degradation by PDEs is not a constitutive function of the cell, but rather a highly regulated one controlled by different mechanisms in different physiological and pathological circumstances. PDE regulation and function is further complicated by the fact that there are more than 50 individual PDEs belonging to 11 different PDE families, yet our understanding of the ...
https://www.urmc.rochester.edu/people/23115996-chen-yan/articles
What does 2,3-cyclic-nucleotide phosphodiesterases mean?What does 2,3-cyclic-nucleotide phosphodiesterases mean?
Definition of 2,3-cyclic-nucleotide phosphodiesterases in the Definitions.net dictionary. Meaning of 2,3-cyclic-nucleotide phosphodiesterases. What does 2,3-cyclic-nucleotide phosphodiesterases mean? Information and translations of 2,3-cyclic-nucleotide phosphodiesterases in the most comprehensive dictionary definitions resource on the web.
http://www.definitions.net/definition/2
Cellular distribution of phosphodiesterase isoforms in rat cardiac tissue. | Circulation ResearchCellular distribution of phosphodiesterase isoforms in rat cardiac tissue. | Circulation Research
We have resolved multiple forms of cyclic nucleotide phosphodiesterase (PDE) in whole rat ventricle and in isolated rat ventricular myocytes by use of anion-exchange high-performance liquid chromatography. One major form, the soluble calmodulin-stimulated PDE, is apparently absent from isolated myocytes. We discern four peaks of PDE activity (designated A-D in the order of their elution) in a soluble fraction obtained from whole rat ventricle. Peak A is stimulated twofold to threefold by the addition of calcium and calmodulin (Ca2+/CalM) and preferentially hydrolyzes cGMP over cAMP (in the presence of Ca2+/CalM, KmcGMP = 1.5 microM, KmcAMP = 17 microM). Peak B has similar affinities for both cAMP and cGMP (half-maximum velocities achieved at 30 microM substrate) and demonstrates positive cooperativity with cAMP but not with cGMP. The hydrolysis of cAMP by peak B is stimulated by cGMP at substrate concentrations up to 20 microM; the maximum effect is seen at 1 microM cAMP (25-fold stimulation by ...
http://circres.ahajournals.org/content/68/4/1070
Cyclic Nucleotide Phosphodiesterase from Spinacea oleracea L.: Subcellular Distribution and Properties | Biochemical Society...Cyclic Nucleotide Phosphodiesterase from Spinacea oleracea L.: Subcellular Distribution and Properties | Biochemical Society...
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http://www.biochemsoctrans.org/content/5/4/975
OriGene - Pde4d (NM 011056) Human ORF cDNA CloneOriGene - Pde4d (NM 011056) Human ORF cDNA Clone
Pde4d - Pde4d (GFP-tagged) - Mouse phosphodiesterase 4D cAMP specific (Pde4d), (10ug) available for purchase from OriGene - Your Gene Company.
http://www.origene.com/Mouse_ORF/MG225474.aspx
Pugnacious P: Paytons battle with PDE…diagnosisPugnacious P: Paytons battle with PDE…diagnosis
After reviewing the MRI and spinal tap from U of I, he confirmed the diagnosis of PDE (that the right side of the brain and its lining was inflamed and being attacked by her own immune system), but quickly snapped us out of our funk. He didnt down play the seriousness of the situation, but said that he had successfully treated PDE before and he has no reason to think it couldnt happen again. He warned us that we would likely have to test different combinations and dosages and there were no guarantees that the drug regimen would work for Payton. However, there was no reason to give up just yet; we should still have some hope. We stayed in Chicago the rest of the week while Dr. Podell developed the treatment, and each day we saw our little girl come back a little at a time. By the end of the week, he was confident she was stable enough to go home ...
http://pugnaciousp.blogspot.com/2011/05/paytons-battle-with-pdediagnosis.html?showComment=1304694689499
Pugnacious P: Paytons battle with PDE…diagnosisPugnacious P: Paytons battle with PDE…diagnosis
After reviewing the MRI and spinal tap from U of I, he confirmed the diagnosis of PDE (that the right side of the brain and its lining was inflamed and being attacked by her own immune system), but quickly snapped us out of our funk. He didnt down play the seriousness of the situation, but said that he had successfully treated PDE before and he has no reason to think it couldnt happen again. He warned us that we would likely have to test different combinations and dosages and there were no guarantees that the drug regimen would work for Payton. However, there was no reason to give up just yet; we should still have some hope. We stayed in Chicago the rest of the week while Dr. Podell developed the treatment, and each day we saw our little girl come back a little at a time. By the end of the week, he was confident she was stable enough to go home ...
http://pugnaciousp.blogspot.com/2011/05/paytons-battle-with-pdediagnosis.html?showComment=1304701960151
Gardiner Pde, Glen Iris (VIC) - Explore Local Property MarketGardiner Pde, Glen Iris (VIC) - Explore Local Property Market
Explore Gardiner Pde, Glen Iris (VIC). Learn about Gardiner Pde, Glen Iris and find out whats happening in the local property market.
https://www.realestate.com.au/vic/glen-iris-3146/gardiner-pde/
1-methyl-3-octylimidazolium chloride | Semantic Scholar1-methyl-3-octylimidazolium chloride | Semantic Scholar
Herein, the binding of 1-methyl-3-octylimidazolium chloride [OMIM][Cl] ionic liquid with hen egg white lysozyme (HEWL) has been… Expand ...
https://www.semanticscholar.org/topic/1-methyl-3-octylimidazolium-chloride/1356326
OligodendrocyteOligodendrocyte
... 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 central nervous system (CNS). Oligodendrocytes were discovered by Pío del ... Oligodendrocytes (from Greek 'cells with a few branches'), or oligodendroglia, are a type of neuroglia whose main functions are ...
https://en.wikipedia.org/wiki/Oligodendrocyte
Neuronal calcium sensor-1Neuronal 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 ...
https://en.wikipedia.org/wiki/Neuronal_calcium_sensor-1
EHNAEHNA
"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) ...
https://en.wikipedia.org/wiki/EHNA
PDE1CPDE1C
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: ...
https://en.wikipedia.org/wiki/PDE1C
P19 cellP19 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; ...
https://en.wikipedia.org/wiki/P19_cell
CNPCNP
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 ...
https://en.wikipedia.org/wiki/CNP
Phosphodiesterase 3Phosphodiesterase 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 ...
https://en.wikipedia.org/wiki/Phosphodiesterase_3
Cyclic nucleotideCyclic 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 ...
https://en.wikipedia.org/wiki/Cyclic_nucleotide
EmoxypineEmoxypine
Modulates the activity of membrane-bound enzymes: phosphodiesterase, cyclic nucleotides, adenylate cyclase, aldoreductase, ... Its chemical structure resembles that of pyridoxine (a type of vitamin B6). Emoxypine was first synthesized by L.D. Smirnov and ... Emoxypine (2-ethyl-6-methyl-3-hydroxypyridine), also known as Mexidol or Mexifin when used as the succinate salt, is an ... doi:10.1007/s11055-012-9646-3. S2CID 39971165. Dumayev KM, Voronina TA, Smirnov LD (1995). Antioxidants in the prophylaxis and ...
https://en.wikipedia.org/wiki/Emoxypine
Benjamin Weiss (scientist)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 ... Cyclic Nucleotide Phosphodiesterases: Weiss and co-workers developed rapid phosphodiesterease assays [3, 4], separated ... Weiss, B. and Winchurch, R.A.: Analyses of cyclic nucleotide phosphodiesterases in lymphocytes from normal and aged leukemic ...
https://en.wikipedia.org/wiki/Benjamin_Weiss_(scientist)
PDE4BPDE4B
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. ( ...
https://en.wikipedia.org/wiki/PDE4B
ABCC5ABCC5
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 ...
https://en.wikipedia.org/wiki/ABCC5
CGMP-specific phosphodiesterase type 5CGMP-specific phosphodiesterase type 5
"Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Advances in Cyclic ... Cyclic guanosine monophosphate-specific phosphodiesterase type 5 is an enzyme (EC 3.1.4.17) from the phosphodiesterase class. ... Fertel R, Weiss B (July 1976). "Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung" ( ... Weiss B, Hait WN (1977). "Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annual ...
https://en.wikipedia.org/wiki/CGMP-specific_phosphodiesterase_type_5
PDE9APDE9A
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- ...
https://en.wikipedia.org/wiki/PDE9A
Cyclic adenosine monophosphateCyclic adenosine monophosphate
... cAMP binds to and regulates the function of ion channels such as the HCN channels and a few other cyclic nucleotide-binding ... cyclic monophosphate (8-Br-cAMP) Acrasin specific to chemotactic use in Dictyostelium discoideum. phosphodiesterase 4 (PDE 4) ... If a cell lacks GM1 the toxin most likely binds to other types of glycans, such as Lewis Y and Lewis X, attached to proteins ... such as cyclic adenosine monophosphate, cyclic AMP). Cyclic AMP is synthesized from ATP by adenylate cyclase located on the ...
https://en.wikipedia.org/wiki/Cyclic_adenosine_monophosphate
BucladesineBucladesine
... 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 ... Nucleotides, Carboxamides, PDE3 inhibitors, All stub articles, Cardiovascular system drug stubs). ...
https://en.wikipedia.org/wiki/Bucladesine
List of EC numbers (EC 3)List of EC numbers (EC 3)
... cyclic-nucleotide phosphodiesterase EC 3.1.4.18: Now EC 3.1.16.1, spleen exonuclease EC 3.1.4.19: Now EC 3.1.13.3, ... type I site-specific deoxyribonuclease EC 3.1.21.4: type II site-specific deoxyribonuclease EC 3.1.21.5: type III site-specific ... phosphodiesterase * EC 3.1.4.59: cyclic-di-AMP phosphodiesterase * EC 3.1.4.60: pApA phosphodiesterase * EC 3.1.4.61: cyclic 2, ... CMP-N-acylneuraminate phosphodiesterase EC 3.1.4.41: sphingomyelin phosphodiesterase D EC 3.1.4.42: glycerol-1,2-cyclic- ...
https://en.wikipedia.org/wiki/List_of_EC_numbers_(EC_3)
Caffeine-induced anxiety disorderCaffeine-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 ...
https://en.wikipedia.org/wiki/Caffeine-induced_anxiety_disorder
CGAS-STING cytosolic DNA sensing pathwayCGAS-STING cytosolic DNA sensing pathway
cGAMP was found to be much more potent than other cyclic di-nucleotides (c-di-GMP and c-di-AMP). cGAMP was shown to ... STING's general role as an adapter molecule in the cytosolic DNA-type 1 IFN response across cell types has been suggested 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 ...
https://en.wikipedia.org/wiki/CGAS–STING_cytosolic_DNA_sensing_pathway
PDE6BPDE6B
"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 ...
https://en.wikipedia.org/wiki/PDE6B
PDE4APDE4A
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 ...
https://en.wikipedia.org/wiki/PDE4A
Phosphodiesterase-4 inhibitorPhosphodiesterase-4 inhibitor
"Functional and biochemical evidence for diazepam as a cyclic nucleotide phosphodiesterase type 4 inhibitor". British Journal of ... 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. ... Moustafa, F; Feldman, SR (16 May 2014). "A Review of Phosphodiesterase-Inhibition and the Potential Role for Phosphodiesterase ...
https://en.wikipedia.org/wiki/Phosphodiesterase-4_inhibitor
PentoxifyllinePentoxifylline
Essayan DM (November 2001). "Cyclic nucleotide phosphodiesterases". The Journal of Allergy and Clinical Immunology. 108 (5): ... "Effect of pentoxifylline on diabetic distal polyneuropathy in type 2 diabetic patients: A randomized trial". Journal of ... Like other methylated xanthine derivatives, pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which ... the effects of non-specific phosphodiesterase inhibition". Clinics. 63 (3): 321-328. doi:10.1590/S1807-59322008000300006. PMC ...
https://en.wikipedia.org/wiki/Pentoxifylline
Cyclic nucleotide phosphodiesteraseCyclic nucleotide phosphodiesterase
"Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... cyclic-nucleotide phosphodiesterases (EC 3.1.4.17) are a family of phosphodiesterases. Generally, these enzymes hydrolyze a ... cyclic-nucleotide phosphodiesterases in rod cells are oligomeric, made up of two heavy catalytic subunits, α (90 kDa) and β (85 ... "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacological Reviews. 58 (3): 488-520. doi: ...
https://en.wikipedia.org/wiki/Cyclic_nucleotide_phosphodiesterase
PhosphodiesterasePhosphodiesterase
"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 ...
https://en.wikipedia.org/wiki/Phosphodiesterase
Pharmacology of antidepressantsPharmacology 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 ...
https://en.wikipedia.org/wiki/Pharmacology_of_antidepressants
ParaxanthineParaxanthine
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 ...
https://en.wikipedia.org/wiki/Paraxanthine
Phosphodiesterase inhibitorPhosphodiesterase 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. ...
https://en.wikipedia.org/wiki/Phosphodiesterase_inhibitor
Phosphodiesterase 2Phosphodiesterase 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. ...
https://en.wikipedia.org/wiki/Phosphodiesterase_2
PDE1PDE1
Lugnier C (March 2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific ... The catalytic domains of phosphodiesterase 1 (and other types of phosphodiesterases) have three helical subdomains: an N- ... 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. ...
https://en.wikipedia.org/wiki/PDE1
Enzyme inhibitorEnzyme 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 selectively toxic to rapidly growing cells, therefore methotrexate is often used in ... cyclic guanosine monophosphate. This signalling molecule triggers smooth muscle relaxation and allows blood flow into the ... 381-382 Although it is possible for mixed-type inhibitors to bind in the active site, this type of inhibition generally results ...
https://en.wikipedia.org/wiki/Enzyme_inhibitor
Sperm chemotaxisSperm chemotaxis
Cyclic GMP possibly opens cyclic nucleotide-gated (CNG) K+-selective channels, thereby causing hyperpolarization of the ... Kong, N., Xu, X., Zhang, Y., Wang, Y., Hao, X., Zhao, Y., Qiao, J., Xia, G. and Zhang, M. (2017) Natriuretic peptide type C ... The cGMP signal is terminated by the hydrolysis of cGMP through phosphodiesterase (PDE) activity and inactivation of GC. On ... The consequential hyperpolarization activates hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels. The ...
https://en.wikipedia.org/wiki/Sperm_chemotaxis
PDE4DPDE4D
"Myomegalin is a novel protein of the golgi/centrosome that interacts with a cyclic nucleotide phosphodiesterase". The Journal ... These proteins degrade the second messenger cAMP, which is a key signal transduction molecule in multiple cell types, including ... "Myomegalin is a novel protein of the golgi/centrosome that interacts with a cyclic nucleotide phosphodiesterase". The Journal ... Zhang HT (2009). "Cyclic AMP-specific phosphodiesterase-4 as a target for the development of antidepressant drugs". Current ...
https://en.wikipedia.org/wiki/PDE4D
Κ-opioid receptorΚ-opioid receptor
Phosphodiesterases break down cAMP, producing an inhibitory effect in neurons. KORs also couple to inward-rectifier potassium ... Tallent M, Dichter MA, Bell GI, Reisine T (December 1994). "The cloned kappa opioid receptor couples to an N-type calcium ... an in vivo fast-cyclic voltammetry study". The Journal of Pharmacology and Experimental Therapeutics. 284 (1): 151-61. PMID ... on the mouse R1.1 thymoma cell line is coupled to adenylyl cyclase through a pertussis toxin-sensitive guanine nucleotide- ...
https://en.wikipedia.org/wiki/Κ-opioid_receptor
RetinaRetina
... resulting in the closing of Na+ cyclic nucleotide-gated ion channels (CNGs). Thus the cell is hyperpolarised. The amount of ... There are two types of centre-surround structures in the retina - on-centres and off-centres. On-centres have a positively ... This in turn causes the Ga-subunit of the protein to activate a phosphodiesterase (PDE6), which degrades cGMP, ... Although each cell type differentiates from the RPCs in a sequential order, there is considerable overlap in the timing of when ...
https://en.wikipedia.org/wiki/Retina
Cyclic di-AMPCyclic di-AMP
It is one of many ubiquitous nucleotide second messengers including cyclic adenosine monophosphate (cAMP), cyclic guanosine ... "The helicase DDX41 recognizes the bacterial secondary messengers cyclic di-GMP and cyclic di-AMP to activate a type I ... Phosphodiesterase (PDE) enzymes degrade cyclic di-AMP to the linear molecule 5'-pApA (phosphadenylyl adenosine). 5'-pApA is ... "Cyclic nucleotides in archaea: Cyclic di-AMP in the archaeon Haloferax volcanii and its putative role". MicrobiologyOpen. 8 (9 ...
https://en.wikipedia.org/wiki/Cyclic_di-AMP
PDE3 inhibitorPDE3 inhibitor
... s are a type of phosphodiesterase inhibitors. Inhibition of the PDE isoenzyme 3 leads to an increase of ... Most studies used analogues of the nucleotide substrates or derivatives of natural product inhibitors such as xanthine (e.g. ... intracellular concentrations of the second messenger cyclic adenosine monophosphate (cAMP). cAMP mediates the phosphorylation ... A PDE3 inhibitor is a drug which inhibits the action of the phosphodiesterase enzyme PDE3. They are used for the therapy of ...
https://en.wikipedia.org/wiki/PDE3_inhibitor
Biochemical cascadeBiochemical cascade
"Cyclic GMP from the surrounding somatic cells regulates cyclic AMP and meiosis in the mouse oocyte". Development. 136 (11): ... The pathway is further refined to include context-specific annotations such as species, cell/tissue type, or disease type. The ... A new mode of data visualization including time-course, single nucleotide polymorphism (SNP), and splicing, has been ... and are regulated by the phosphodiesterase (PDE). This pathway can be triggered via two mechanisms: physiological stimulus ( ...
https://en.wikipedia.org/wiki/Biochemical_cascade
GAF domainGAF domain
In mammals, GAF domains are found in five members of the cyclic nucleotide phosphodiesterase superfamily: PDE2, PDE5, and PDE6 ... The GAF domain is a type of protein domain that is found in a wide range of proteins from all species. The GAF domain is named ... a ubiquitous signaling motif and a new class of cyclic GMP receptor". The EMBO Journal. 19 (20): 5288-99. doi:10.1093/emboj/ ... "The two GAF domains in phosphodiesterase 2A have distinct roles in dimerization and in cGMP binding". Proceedings of the ...
https://en.wikipedia.org/wiki/GAF_domain
CaffeineCaffeine
Essayan DM (November 2001). "Cyclic nucleotide phosphodiesterases" (PDF). The Journal of Allergy and Clinical Immunology. 108 ( ... Caffeine content in coffee varies widely depending on the type of coffee bean and the method of preparation used; even beans ... Caffeine also increases cyclic AMP levels through nonselective inhibition of phosphodiesterase. Caffeine is a bitter, white ... As a competitive nonselective phosphodiesterase inhibitor, caffeine raises intracellular cyclic AMP, activates protein kinase A ...
https://en.wikipedia.org/wiki/Caffeine
MutationMutation
The number is the position of the nucleotide from the 5' end; the first letter represents the wild-type nucleotide, and the ... Whole genome sequencing results revealed that when Cyclic-di-AMP phosphodiesterase (GdpP) was disrupted in this bacterium, it ... The nomenclature specifies the type of mutation and base or amino acid changes. Nucleotide substitution (e.g., 76A>T) - ... These type of mutation have led to new types of fruits, such as the "Delicious" apple and the "Washington" navel orange. Human ...
https://en.wikipedia.org/wiki/Mutation
Photoreceptor cellPhotoreceptor cell
Unstimulated (in the dark), cyclic-nucleotide gated channels in the outer segment are open because cyclic GMP (cGMP) is bound ... Rather, it is the ratios of responses of the three types of cone cells that can estimate wavelength, and therefore enable color ... Each transducin then activates the enzyme cGMP-specific phosphodiesterase (PDE). PDE then catalyzes the hydrolysis of cGMP to 5 ... resulting in the closure of cyclic nucleotide-gated Na+ ion channels located in the photoreceptor outer segment membrane. As a ...
https://en.wikipedia.org/wiki/Photoreceptor_cell
Retinitis pigmentosa GTPase regulatorRetinitis pigmentosa GTPase regulator
... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... April 2007). "A novel gene for Usher syndrome type 2: mutations in the long isoform of whirlin are associated with retinitis ... characteristic of the highly conserved guanine nucleotide exchange factors. Mutations in this gene have been associated with X- ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ...
https://en.wikipedia.org/wiki/Retinitis_pigmentosa_GTPase_regulator
PDE8BPDE8B
2003). "Comparison of enzymatic characterization and gene organization of cyclic nucleotide phosphodiesterase 8 family in ... 2003). "Alterations on phosphodiesterase type 7 and 8 isozyme mRNA expression in Alzheimer's disease brains examined by in situ ... cyclic nucleotide phosphodiesterase". Biochem Biophys Res Commun. 250 (3): 751-6. doi:10.1006/bbrc.1998.9379. PMID 9784418. " ... cyclic phosphodiesterase 8B is an enzyme that in humans is encoded by the PDE8B gene. GRCm38: Ensembl release 89: ...
https://en.wikipedia.org/wiki/PDE8B
TransducinTransducin
Kroll, S.; Phillips, W. J.; Cerione, R. A. (1989). "The regulation of the cyclic GMP phosphodiesterase by the GDP-bound form of ... Fung, BKK; Hurley, JB; Stryer, L (1981). "Flow of information in the light-triggered cyclic nucleotide cascade of vision". ... It is a type of heterotrimeric G-protein with different α subunits in rod and cone photoreceptors. Light leads to ... Transducin activates phosphodiesterase, which results in the breakdown of cyclic guanosine monophosphate (cGMP). The intensity ...
https://en.wikipedia.org/wiki/Transducin
Tubulin alpha-1A chainTubulin alpha-1A chain
Cyclic nucleotide 3'-phosphodiesterase: a membrane-bound, microtubule-associated protein and membrane anchor for tubulin". ... Mutations to the TUBA1A gene manifest clinically as Type 3 Lissencephaly. In general, lissencephaly is characterized by agyria ... with respect to wild-type counterparts), showing that the S140G mutation has value as a model for detailing disease associated ... while attribution to a specific type is obtained by microarray. Treatment is symptomatic; anti-convulsive drugs for seizure ...
https://en.wikipedia.org/wiki/Tubulin_alpha-1A_chain
Guanylate cyclaseGuanylate cyclase
Because RETGC-1 produces cGMP, which keeps cyclic nucleotide-gated channels open allowing the influx of calcium, this mutation ... There are membrane-bound (type 1, guanylate cyclase-coupled receptor) and soluble (type 2, soluble guanylate cyclase) forms of ... Once formed, cGMP can be degraded by phosphodiesterases, which themselves are under different forms of regulation, depending on ... cyclic-GMP-forming)) is a lyase enzyme that converts guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP) and ...
https://en.wikipedia.org/wiki/Guanylate_cyclase
IL-3 and IL-4 activate cyclic nucleotide phosphodiesterases 3 (PDE3) and 4 (PDE4) by different mechanisms in FDCP2 myeloid...IL-3 and IL-4 activate cyclic nucleotide phosphodiesterases 3 (PDE3) and 4 (PDE4) by different mechanisms in FDCP2 myeloid...
type. Contribution to journal publication status. published. subject. *Immunology in the medical area ... In FDCP2 myeloid cells, IL-4 activated cyclic nucleotide phosphodiesterases PDE3 and PDE4, whereas IL-3, granulocyte-macrophage ... In FDCP2 myeloid cells, IL-4 activated cyclic nucleotide phosphodiesterases PDE3 and PDE4, whereas IL-3, granulocyte-macrophage ... IL-4 activated cyclic nucleotide phosphodiesterases PDE3 and PDE4, whereas IL-3, granulocyte-macrophage CSF (GM-CSF), and ...
https://lup.lub.lu.se/search/publication/4dc2bc02-b208-43f3-96fc-9ae11a14ae3c
WO2004108726A1 - 2-SUBSTITUTED PHENYL-5,7-DIALKYL-3,7-DIHYDROPYRROLE [2,3-d] PYRIMIDINE-4-ONE DERIVATIVES, THE PREPARATION AND...
Type 5 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 description 2 * 108010037581 Type 5 Cyclic Nucleotide ... ZOOGRGPOEVQQDX-UUOKFMHZSA-N Cyclic guanosine monophosphate Chemical compound data:image/svg+xml;base64, ... 150000007530 organic bases Chemical class 0.000 claims description 3 * 125000002971 oxazolyl group Chemical group 0.000 claims ... 239000002202 Polyethylene glycol Substances 0.000 claims description 3 * 150000001412 amines Chemical class 0.000 claims ...
https://patents.google.com/patent/WO2004108726A1/en
Galectin-3 in heart failure with preservedejection fraction. A RELAX trial substudy (phosphodiesterase-5 inhibition to improve...
Type 5 Cyclic Nucleotide Phosphodiesterases Medicine & Life Sciences 100% * Galectin 3 Medicine & Life Sciences 90% ... Methods: Two hundred eight patients from the RELAX (Phosphodiesterase-5 Inhibition to Improve Clinical Status and Exercise ... Methods: Two hundred eight patients from the RELAX (Phosphodiesterase-5 Inhibition to Improve Clinical Status and Exercise ... Methods: Two hundred eight patients from the RELAX (Phosphodiesterase-5 Inhibition to Improve Clinical Status and Exercise ...
https://mayoclinic.pure.elsevier.com/en/publications/galectin-3-in-heart-failure-with-preservedejection-fraction-a-rel
PDE - Other - Transporters - Proteins - ProductsPDE - Other - Transporters - Proteins - Products
Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. B. ... are essential regulators of cyclic nucleotide signaling with diverse physiological functions. Roughly, the sub-types can be ... Phosphodiesterases listed: PDE, PLC, PLD. [1] A. Chandra et al. TheGDI-like solubilizing factor PDEδ sustains the spatial ... Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. ...
https://www.axonmedchem.com/products/proteins/transporters/other/pde
Intraspinal Transplantation of Autologous Neurogenically-Induced Bone Marrow-Derived Mesenchymal Stem Cells in the Treatment of...Intraspinal Transplantation of Autologous Neurogenically-Induced Bone Marrow-Derived Mesenchymal Stem Cells in the Treatment of...
Cyclic-Nucleotide Phosphodiesterases / analysis * 2,3-Cyclic-Nucleotide Phosphodiesterases / metabolism ... Publication types * Research Support, Non-U.S. Govt MeSH terms * 2,3- ... In eight months-followed up 4 cases were evaluated by the same parameter; gait score had improved in 3 cases, and propriception ... improved in 2 cases, and nociception improved in 3 cases. Conclusion: Our findings suggest that utility of autologous NIBM-MSCs ...
https://pubmed.ncbi.nlm.nih.gov/26242341/
Persistent Pulmonary Hypertension of the Newborn (PPHN): Practice Essentials, Overview, EtiologyPersistent Pulmonary Hypertension of the Newborn (PPHN): Practice Essentials, Overview, Etiology
Among the 11 isoforms of phosphodiesterases (PDEs), the most important are the PDE3 and PDE5 isoforms, which degrade cyclic ... leading to the conversion of guanosine triphosphate nucleotide into cyclic guanosine monophosphate (cGMP). The increase in ... or nitric oxide synthase type 3) is the most extensively studied enzyme in persistent pulmonary hypertension of the newborn ( ... 9, 10] cGMP is down-regulated by phosphodiesterase 5 activity. Phosphodiesterase 5, which is abundantly expressed in lung ...
https://www.medscape.com/answers/898437-71012/what-are-the-most-common-causes-of-persistent-pulmonary-hypertension-of-the-newborn-pphn
DeCSDeCS
Cyclic Nucleotide Phosphodiesterase PDE3 Family. Cyclic Nucleotide Phosphodiesterases, Type 3A. Cyclic Nucleotide ... cGMP-Inhibited Cyclic Nucleotide Phosphodiesterase cGMP-Inhibited Phosphodiesterase Cyclic Nucleotide Phosphodiesterases, Type ... Cyclic Nucleotide Phosphodiesterases, Type 3A - Narrower Concept UI. M0367999. Preferred term. Cyclic Nucleotide ... Cyclic Nucleotide Phosphodiesterase PDE3 Family Phosphodiesterase III Phosphodiesterase, cGMP-Inhibited cGMP Inhibited Cyclic ...
https://decs.bvsalud.org/en/ths/resource/?id=52678
Carlos Molina - Research output - Montclair State University
Nuclear response to cyclic AMP: Central role of transcription factor CREM (cyclic-AMP-responsive-element modulator). Lalli, E. ... Functional role of phosphodiesterase 3 in cardiomyocyte apoptosis: Implication in heart failure. Ding, B., Abe, J. I., Wei, H. ... up-regulation of the cyclin D2 gene and acquisition of new cyclin-dependent kinase partners in human T-cell leukemia virus type ... Inducible cyclic AMP early repressor protein in rat pinealocytes: A highly sensitive natural reporter for regulated gene ...
https://researchwith.montclair.edu/en/persons/carlos-molina/publications/
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs.bvs.br/I/dcsnew2008.txt
Trans-regulation of oligodendrocyte myelination by neurons through small GTPase Arf6-regulated secretion of fibroblast growth...Trans-regulation of oligodendrocyte myelination by neurons through small GTPase Arf6-regulated secretion of fibroblast growth...
... cyclic nucleotide 3′-phosphodiesterase (CNP)-Cre mice9,10, respectively. Unexpectedly, N-Arf6-CKO mice but not O-Arf6-CKO mice ... To clarify in which cell type Arf6 expression is required for myelination, we generated neuron- and oligodendrocyte-specific ... These processes of guanine nucleotide exchange and GTP hydrolysis are regulated and accelerated by guanine nucleotide exchange ... Another possibility is that the CNP-Cre promoter generates Cre activity in cell types other than oligodendrocytes at low ...
https://www.nature.com/articles/ncomms5744?error=cookies_not_supported&code=eb053ac1-2b23-4e94-b201-4cd1407f04fd
Pesquisa | Portal Regional da BVSPesquisa | Portal Regional da BVS
... cyclic nucleotide 3-phosphodiesterase) showed no significant changes. Total Akt levels were unchanged, while an increased ... Cell type specific enzymatic markers (glutamine synthase, choline acetyltransferase and 2,3- ... Three novel cyclic hexapeptides, sclerotides C-E (1-3), and a new lipodepsipeptide, scopularide I (4), together with a known ... Cyclic Peptides from the Soft Coral-Derived Fungus Aspergillus sclerotiorum SCSIO 41031. ...
https://pesquisa.bvsalud.org/portal/?lang=pt&q=mh:Acetilcolinesterase/efeitos+dos+f%C3%A1rmacos
100-61-8 | MFCD00008283 | N-Methylaniline
Title: Cyclic nucleotide phosphodiesterase type 4 inhibitors: evaluation of pyrazolo[1,5-a]-1,3,5-triazine ring system as an ... bisphosphate C-nucleotide analogues as the first reported in vivo stable P2Y(1)-receptor antagonists.. Journal: The Journal of ... Title: Air-stable Pd(R-allyl)LCl (L= Q-Phos, P(t-Bu)3, etc.) systems for C-C/N couplings: insight into the structure-activity ... Title: 3-substitued indoles: one-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities.. Journal: ...
https://www.aablocks.com/prod/100-61-8
Cardiovascular DiseaseCardiovascular Disease
Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 M and inhibitor of ... Product Types. PROTACs. Natural Products. LNPs for Drug Delivery. All Targets. Screening Libraries Bioactive Compound Library. ... Ambrisentan is an oral, once-daily endothelin receptor antagonist that is selective for the endothelin type A receptor (IC50s ... GSK-3. Hedgehog. JAK. MST. Notch. PKA. PORCN. ROCK. Secretase. sFRP-1. Smo. STAT. Wnt. YAP. β-catenin. BMI-1. TGF-beta Receptor ...
https://www.csnpharm.com/cardiovascular-disease.html
PDE3A mutations cause autosomal dominant hypertension with brachydactyly - MDC RepositoryPDE3A mutations cause autosomal dominant hypertension with brachydactyly - MDC Repository
... in six unrelated families with mendelian hypertension and brachydactyly type E (HTNB). The syndrome features brachydactyly type ... Here we report six missense mutations in PDE3A (encoding phosphodiesterase 3A) ... MDC Repository is powered by EPrints 3 which is developed by the School of Electronics and Computer Science at the University ...
http://edoc.mdc-berlin.de/14795/
June | 2018 | Hif signaling
None of the patients with low VWF:RCo, decreased VWF:RCo/VWF:Ag ratio and p.D1472H had VWD type 2M mutations identified. This ... Of these 23 patients, 6 with borderline low VWF:RCo were given provisional diagnosis of VWD type 1 by treating physicians, ... Results: Among 55 cirrhotic drivers with MHE [males, median age 53 years (range 30-60)], 7 (12.7%) reported any type of ... 2 type 2 diabetes,3 Dimethyl sulfoxide hypertension,4 and certain cancers.5 Although many related genes and signaling pathways ...
https://hif-signaling.com/index.php/2018/06/
TCR- and CD28-mediated recruitment of phosphodiesterase 4 to lipid rafts potentiates TCR signaling. - Oxford Neuroscience
... beta-arrestin in complex with cAMP-specific phosphodiesterase 4 (PDE4) was recruited to lipid rafts which down-regulated cAMP ... Cyclic AMP, Cyclic AMP-Dependent Protein Kinases, Cyclic Nucleotide Phosphodiesterases, Type 4, Humans, Lymphocyte Activation, ... TCR- and CD28-mediated recruitment of phosphodiesterase 4 to lipid rafts potentiates TCR signaling. ... TCR- and CD28-mediated recruitment of phosphodiesterase 4 to lipid rafts potentiates TCR signaling. ...
https://www.neuroscience.ox.ac.uk/publications/55997?e6df861c-9f08-11ed-a592-061ab7f93640
Persistent Pulmonary Hypertension of the Newborn (PPHN): Practice Essentials, Overview, Etiology
Among the 11 isoforms of phosphodiesterases (PDEs), the most important are the PDE3 and PDE5 isoforms, which degrade cyclic ... leading to the conversion of guanosine triphosphate nucleotide into cyclic guanosine monophosphate (cGMP). The increase in ... or nitric oxide synthase type 3) is the most extensively studied enzyme in persistent pulmonary hypertension of the newborn ( ... 9, 10] cGMP is down-regulated by phosphodiesterase 5 activity. Phosphodiesterase 5, which is abundantly expressed in lung ...
https://www.staging.medscape.com/answers/898437-71005/what-is-fetal-pulmonary-hypertension
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2014.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2013.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2018.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2012.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2008.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2010.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2020.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2015.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2017.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2011.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2009.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2016.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE 1984-2007 BX - Cyclic Nucleotide Phosphodiesterases, Type I MH - Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ... class have additional specificity for CYCLIC-GMP. HN - 2008(2000) MH - Cyclic Nucleotide Phosphodiesterases, Type 3 UI - ... HN - 2008 MH - Cyclic Nucleotide Phosphodiesterases, Type 1 UI - D054677 MN - D08.811.277.352.640.150.100 MN - D08.811.277.352. ...
https://decs2019.bvsalud.org/I/dcsnew2008.txt
Guanosine monophosphatePDE4PDE3Calmodulin-dependentCAMP and cGMPPDE5Protein KinasesInhibitorsCNPaseGuanineBiochemicalRv0805PhysiologicalPeptideEnzymesAllostericEncodesProteinsPharmacologicalGuanylyl cyclaseRegulatoryActivationInhibitorHumansSynthaseCatalytic ActivityTargetsInhibitionRegulationSuperfamilyConcentrationsSignalingInhibitMutation19952022FamilyPrimarilyHumanExonucleasesCalciumStimulation
Guanosine monophosphate2
  • Both inhibitors augment cyclic guanosine monophosphate (cGMP) to activate protein kinase G, with PDE5-I regulating nitric oxide (NO) and PDE9-I natriuretic peptide-dependent signaling. (omicsdi.org)
  • PDEs are a diverse family of enzymes that have different tissue distributions and functions but that all exert their effect by lowering intracellular levels of cyclic nucleotides, such as cyclic guanosine monophosphate (cGMP). (medscape.com)
PDE46
  • 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. (lu.se)
  • 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. (lu.se)
  • AG-490 and wortmannin, not TNF-alpha, inhibited activation of PDE4 by IL-3. (lu.se)
  • 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. (lu.se)
  • 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). (lu.se)
  • Upon T cell activation of human peripheral blood T cells, we found that the majority of cAMP was generated in T cell lipid rafts followed by activation of protein kinase A. However, upon TCR and CD28 coligation, beta-arrestin in complex with cAMP-specific phosphodiesterase 4 (PDE4) was recruited to lipid rafts which down-regulated cAMP levels. (ox.ac.uk)
PDE31
  • Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 M and inhibitor of adenosine uptake. (csnpharm.com)
Calmodulin-dependent2
  • In addition to binding to L-type calcium channels, felodipine binds to a number of calcium-binding proteins, exhibits competitive antagonism of the mineralcorticoid receptor, inhibits the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase, and blocks calcium influx through voltage-gated T-type calcium channels. (drugbank.com)
  • Another study demonstrated that felodipine attenuates the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase (CaMPDE) by binding to the PDE-1B1 and PDE-1A2 enzyme subunits. (drugbank.com)
CAMP and cGMP2
  • We investigated whether elevation of intracellular cyclic nucleotides (cAMP and cGMP) inhibit cell proliferation and migration of cultured embryonic rat aortic vascular smooth muscle (VSM) cells (A7r5). (nii.ac.jp)
  • The affinities of cAMP and cGMP for wild-type GAF-B alone were ∼4-fold greater than for the holoenzyme, suggesting that the presence of neighboring domains alters the conformation of GAF-B. More importantly, the PDE2A GAF-B, GAF-A/B, GAF-A/B+C domains, and holoenzyme all bind cGMP with much higher affinity than has previously been reported. (mssm.edu)
PDE56
  • Here we contrast 2 closely related therapies, inhibitors of phosphodiesterase type 5 or type 9 (PDE5-I, PDE9-I), given to mice subjected to sustained cardiac pressure overload (PO). (omicsdi.org)
  • Recently, we showed that within the NO-induced cGMP response in human platelets, activation and phosphorylation of phosphodiesterase type 5 (PDE5) occurred. (omicsdi.org)
  • Here, we identify cyclic GMP-dependent protein kinase I as the kinase responsible for the NO-induced PDE5 phosphorylation. (omicsdi.org)
  • cGMP-specific, cGMP-binding phosphodiesterase (PDE5) regulates such physiological processes as smooth muscle relaxation and neuronal survival. (omicsdi.org)
  • In vitro anticoagulants have shown that the penis of tadalafil is more likely on PDE5 than on other phosphodiesterases. (betterdad.com)
  • Phosphodiesterase type 5 (PDE5) inhibitors are the principal oral agents used in ED. (medscape.com)
Protein Kinases1
  • Activator of cGMP-dependent protein kinases I α, I β & type II and cGMP-gated ion channels (cyclic GMP agonist). (biolog.de)
Inhibitors3
  • Gal-3 did not identify patients who responded to phosphodiesterase type 5 (PDE-5) inhibitors (interaction p= 0.53). (elsevier.com)
  • The effect of the phosphodiesterase (PDE) isozyme selective inhibitors siguazodan (PDE III-selective), rolipram (PDE IV-selective), denbufylline (PDE IV-selective) and zaprinast (PDE V-selective) was examined on the relaxant responses to field stimulation and on relaxations elicited by the nitric oxide donor 3-morpholinosydnonimine-N-ethylcarbamide (SIN-1). (unboundmedicine.com)
  • The response to field stimulation in the presence of alpha-chymotrypsin (the putative nitric oxide component), at all the frequencies tested, was potentiated significantly by the PDE IV inhibitors rolipram (1 and 10 microM) and denbufylline (3 and 10 microM) as were responses to SIN-1. (unboundmedicine.com)
CNPase1
  • CNPase (2',3'-Cyclic-nucleotide 3'-phosphodiesterase) is showing promising potential in being a protein biomarker for the mental illness schizophrenia, due to a modified expression pattern in schizophrenia patients. (fapesp.br)
Guanine2
  • These processes of guanine nucleotide exchange and GTP hydrolysis are regulated and accelerated by guanine nucleotide exchange factors and GTPase-activating proteins, respectively. (nature.com)
  • element that accounts for guanine nucleotide specificity. (cornell.edu)
Biochemical3
  • A close ortholog of 239FB is found in adult tissues, and biochemical characterization of the 239AB protein demonstrated significant hydrolytic activity against 2',3'-cAMP, thus representing the first evidence for a Class III cyclic nucleotide phosphodiesterase in mammals. (iisc.ac.in)
  • Trl1 enzymes are found in all human fungal pathogens and are promising targets for antifungal drug discovery because their domain compositions and biochemical mechanisms are unique compared to the mammalian RtcB-type tRNA splicing enzyme. (cornell.edu)
  • The Rv0805 gene from Mycobacterium tuberculosis encodes a 3',5'-cyclic nucleotide phosphodiesterase: biochemical and mutational analysis. (rhea-db.org)
Rv08051
  • We have recently identified the first Class III cyclic nucleotide phosphodiesterase, Rv0805, from Mycobacterium tuberculosis, which biochemically and structurally belongs to the superfamily of metallophosphoesterases. (iisc.ac.in)
Physiological2
  • are essential regulators of cyclic nucleotide signaling with diverse physiological functions. (axonmedchem.com)
  • Cyclic GMP can directly stimulate If but it is ∼10-fold less potent than the 'physiological' If-gating nucleotide, cAMP. (ox.ac.uk)
Peptide1
  • In contrast, recent studies have shown that C-type Natriuretic Peptide (CNP) is an important anabolic regulator of cartilage growth, and loss-of-function mutations in the human CNP receptor gene cause dwarfism. (biomedcentral.com)
Enzymes3
  • Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. (axonmedchem.com)
  • Cyclic nucleotides are hydrolyzed and compartmentalized by a family of enzymes called phosphodieterases. (novusbio.com)
  • CaMPDE is one of the key enzymes involved in cyclic nucleotides and calcium second messenger systems. (drugbank.com)
Allosteric1
  • 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. (bvsalud.org)
Encodes1
  • Mroczek S, Krwawicz J, Kutner J, Lazniewski M, Kucinski I, Ginalski K, Dziembowski A. C16orf57, a gene mutated in poikiloderma with neutropenia, encodes a putative phosphodiesterase responsible for the U6 snRNA 3' end modification. (medlineplus.gov)
Proteins1
  • The differentiation of mesenchymal cells into chondroblasts is regulated by the activity of the Sox9 transcription factor, which controls the expression of principal genes encoding the extracellular matrix proteins of cartilage, such as collagen type II and aggrecan [ 4 ]. (biomedcentral.com)
Pharmacological1
  • Tissue and substrate specificity of inhibition by alkoxy-aryl-lactams of platelet and arterial smooth muscle cyclic nucleotide phosphodiesterases relationship to pharmacological activity. (archives-ouvertes.fr)
Guanylyl cyclase1
  • Adenylyl cyclase class-3/4/guanylyl cyclase [Interproscan]. (ntu.edu.sg)
Regulatory1
  • P. Banky, L. Huang, and S. S. Taylor , Dimerization/docking domain of the type Ia regulatory subunit of cAMP-dependent protein kinase. (inserm.fr)
Activation2
  • Adjusting for age, sex, and/or cystatin-C, Gal-3 was not associated with biomarkers of neurohumoral activation, fibrosis, inflammation or myocardial necrosis, congestion or quality-of-life impairment, cardiac remodeling or dysfunction, or exercise intolerance. (elsevier.com)
  • Modifications in second messenger levels, protein levels, immune cells, cytoskeleton or activation of different cellular death types have been published as consequence of YTX exposure. (mdpi.com)
Inhibitor2
  • BIO is an inhibitor of GSK-3 and CDK1cyclinB complex. (csnpharm.com)
  • Olprmone hydrochloride (OPN, 1 mM) , type 3 phosphodiesterase inhibitor, inhibited cell proliferation, and synergistically inhibited in the presence of db-cAMP (0.3 mM). (nii.ac.jp)
Humans1
  • Comparison of enzymatic characterization and gene organization of cyclic nucleotide phosphodiesterase 8 family in humans. (rhea-db.org)
Synthase1
  • Cell type specific enzymatic markers (glutamine synthase, choline acetyltransferase and 2',3'-cyclic nucleotide 3'-phosphodiesterase) showed no significant changes. (bvsalud.org)
Catalytic Activity1
  • Binding of cGMP to the GAF-B domain of phosphodiesterase 2A allosterically activates catalytic activity. (mssm.edu)
Targets1
  • This has involved the study of noradrenergic mechanisms in the actions of antidepressant drugs and of cyclic nucleotide phosphodiesterases as potential targets for novel antidepressant, anxiolytic, and memory-enhancing drugs. (buffalo.edu)
Inhibition4
  • A RELAX trial substudy (phosphodiesterase-5 inhibition to improve clinical status and exercise capacity in diastolic heartfailure). (elsevier.com)
  • Methods: Two hundred eight patients from the RELAX (Phosphodiesterase-5 Inhibition to Improve Clinical Status and Exercise Capacity in Diastolic Heart Failure) trial of sildenafil in HFpEF had Gal-3 measured at enrollment. (elsevier.com)
  • Conclusions: In overt HFpEF, Gal-3 was related to severity of renal dysfunction and accounting for this, was not independently associated with severity of pathophysiological derangements or response PDE-5 inhibition. (elsevier.com)
  • Though felodipine exhibits binding to many endogenous molecules, its vasodilatory effects are still thought to be brought about primarily through inhibition of voltage-gated L-type calcium channels. (drugbank.com)
Regulation2
  • The syndrome features brachydactyly type E (BDE), severe salt-independent but age-dependent hypertension, an increased fibroblast growth rate, neurovascular contact at the rostral-ventrolateral medulla, altered baroreflex blood pressure regulation and death from stroke before age 50 years when untreated. (mdc-berlin.de)
  • Myocardial Phosphodiesterases and Their Role in cGMP Regulation. (omicsdi.org)
Superfamily1
  • Cyclic nucleotide phosphodiesterases comprise an 11-member superfamily yielding near 100 isoform variants that hydrolyze cAMP or cGMP to their respective 5'-monophosphate form. (omicsdi.org)
Concentrations2
  • Apoptotic cell death, as measured using caspase-3 activity was evident only at 100 µM concentrations. (bvsalud.org)
  • This high affinity suggests that cGMP binding to PDE2 GAF-B activates the enzyme rapidly, stoichiometrically, and in an all or none fashion, rather than variably over a large range of cyclic nucleotide concentrations. (mssm.edu)
Signaling1
  • TCR- and CD28-mediated recruitment of phosphodiesterase 4 to lipid rafts potentiates TCR signaling. (ox.ac.uk)
Inhibit1
  • A possible strategy to inhibit undesired PPIs is to design small organic molecules binding in the zone of interactions and the increasing number of such recent success stories prove it [ 3 - 5 ]. (biomedcentral.com)
Mutation1
  • Generation of a rat 239FB protein with a mutation corresponding to a single nucleotide polymorphism seen in human 239FB led to complete inactivation of the protein. (iisc.ac.in)
19951
20221
Family2
  • part of family of 3'-to5' exonucleases. (lbl.gov)
  • XIII" YMR047C 3 13 3 YMR047C "Nuclear pore complex protein that is member of GLFG repeat-containing family of nucleoporins and is,XIII" YMR049C 3 13 4 YMR049C "Ymr049cp,XIII" YMR051C 3 13 5 YMR051C "TyA Gag protein. (davidson.edu)
Primarily2
  • These results suggest that the nitric oxide component of the nonadrenergic, noncholinergic relaxant response is mediated primarily via cyclic AMP whose action is inactivated by a PDE IV isozyme and also by cyclic GMP which is inactivated by a PDE V isozyme. (unboundmedicine.com)
  • It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. (drugbank.com)
Human2
  • Full-length cDNAs of human cyclic nucleotide phosphodiesterase 8B (PDE8B) were isolated. (rhea-db.org)
  • Multilocus sequencing of 3 chromosomal loci ( flaB, rrs , and gyrB ) indicated that the isolates were identical to those of B. turicatae 91E135 (a tick isolate) and BTE5EL (a human isolate). (cdc.gov)
Exonucleases1
  • RNA exonucleases cut off (cleave) building blocks called nucleotides one at a time from molecules of RNA (a chemical cousin of DNA). (medlineplus.gov)
Calcium5
  • There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. (drugbank.com)
  • however, some studies have shown that felodipine also binds to and inhibits T-type calcium channels. (drugbank.com)
  • T-type calcium channels are most commonly found on neurons, cells with pacemaker activity and on osteocytes. (drugbank.com)
  • The pharmacologic significance of T-type calcium channel blockade is unknown. (drugbank.com)
  • Felodipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through voltage-gated L-type calcium channels. (drugbank.com)
Stimulation1
  • Nonadrenergic, noncholinergic relaxations were elicited by field stimulation (1-16 Hz, 1 msec, 8 V for 15 sec) of guinea pig trachea desensitized with capsaicin (3 microM), pretreated with atropine (1 microM), propranolol (1 microM), indomethacin (3 microM) and treated with alpha-chymotrypsin (2 U/ml) and contracted with 3 microM histamine. (unboundmedicine.com)