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.
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.
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.
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.
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.
A class of enzymes that catalyze the hydrolysis of one of the two ester bonds in a phosphodiester compound. EC 3.1.4.
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.-.
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
Enzymes that catalyze the hydrolysis of cyclic GMP to yield guanosine-5'-phosphate.
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.
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)
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.
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.
A phosphodiesterase 4 inhibitor with antidepressant properties.
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
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
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.
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.
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.
The rate dynamics in chemical or physical systems.
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.
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)
Compounds that specifically inhibit PHOSPHODIESTERASE 3.
Compounds that specifically inhibit PHOSPHODIESTERASE 4.
Inhibitor of phosphodiesterases.
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.
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.
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.
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.
Enzymes that catalyze the cleavage of a phosphorus-oxygen bond by means other than hydrolysis or oxidation. EC 4.6.
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.
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)
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)
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.
A group of cyclic GMP-dependent enzymes that catalyze the phosphorylation of SERINE or THREONINE residues of proteins.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
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.
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.
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.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
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.
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.
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.
A single nucleotide variation in a genetic sequence that occurs at appreciable frequency in the population.
Compounds that specifically inhibit PHOSPHODIESTERASE 5.
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.
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.
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.
The process of cleaving a chemical compound by the addition of a molecule of water.
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.
Purine bases found in body tissues and fluids and in some plants.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
The region of an enzyme that interacts with its substrate to cause the enzymatic reaction.
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.
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.
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.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.

Characterization of TbPDE2A, a novel cyclic nucleotide-specific phosphodiesterase from the protozoan parasite Trypanosoma brucei. (1/68)

This study reports the identification and characterization of a cAMP-specific phosphodiesterase from the parasitic hemoflagellate Trypanosoma brucei. TbPDE2A is a class I phosphodiesterase. Its catalytic domain exhibits 30-40% sequence identity with those of all 11 mammalian phosphodiesterase (PDE) families, as well as with PDE2 from Saccharomyces cerevisiae, dunce from Drosophila melanogaster, and regA from Dictyostelium discoideum. The overall structure of TbPDE2A resembles that of human PDE11A in that its N-terminal region contains a single GAF domain. This domain is very similar to those of the mammalian PDE2, -5, -6, -10, and -11, where it constitutes a potential cGMP binding site. TbPDE2A can be expressed in S. cerevisiae, and it complements an S. cerevisiae PDE deletion strain. Recombinant TbPDE2A is specific for cAMP, with a K(m) of approximately 2 micrometer. It is entirely resistant to the nonselective PDE inhibitor 3-isobutyl-1-methylxanthine, but it is sensitive to trequinsin, dipyridamole, sildenafil, and ethaverine with IC(50) values of 5.4, 5.9, 9.4, and 14.2 micrometer, respectively. All four compounds inhibit proliferation of bloodstream form trypanosomes in culture, indicating that TbPDE2A is an essential enzyme.  (+info)

Cyclic GMP regulation of the L-type Ca(2+) channel current in human atrial myocytes. (2/68)

1. The regulation of the L-type Ca(2+) current (I(Ca)) by intracellular cGMP was investigated in human atrial myocytes using the whole-cell patch-clamp technique. 2. Intracellular application of 0.5 microM cGMP produced a strong stimulation of basal I(Ca) (+64 +/- 5 %, n = 60), whereas a 10-fold higher cGMP concentration induced a 2-fold smaller increase (+36 +/- 8 %, n = 35). 3. The biphasic response of I(Ca) to cGMP was not mimicked by the cGMP-dependent protein kinase (PKG) activator 8-bromoguanosine 3',5' cyclic monophosphate (8-bromo-cGMP, 0.5 or 5 microM), and was not affected by the PKG inhibitor KT 5823 (100 nM). 4. In contrast, cGMP stimulation of I(Ca) was abolished by intracellular perfusion with PKI (10 microM), a selective inhibitor of the cAMP-dependent protein kinase (PKA). 5. Selective inhibition of the cGMP-inhibited phosphodiesterase (PDE3) by extracellular cilostamide (100 nM) strongly enhanced basal I(Ca) in control conditions (+78 +/- 13 %, n = 7) but had only a marginal effect in the presence of intracellular cGMP (+22 +/- 7 % in addition to 0.5 microM cGMP, n = 11; +20 +/- 22 % in addition to 5 microM cGMP, n = 7). 6. Application of erythro-9-[2-hydroxy-3-nonyl]adenine (EHNA, 30 microM), a selective inhibitor of the cGMP-stimulated phosphodiesterase (PDE2), fully reversed the secondary inhibitory effect of 5 microM cGMP on I(Ca) (+99 +/- 16 % stimulation, n = 7). 7. Altogether, these data indicate that intracellular cGMP regulates basal I(Ca) in human atrial myocytes in a similar manner to NO donors. The effect of cGMP involves modulation of the cAMP level and PKA activity via opposite actions of the nucleotide on PDE2 and PDE3.  (+info)

Local response of L-type Ca(2+) current to nitric oxide in frog ventricular myocytes. (3/68)

1. The regulation of L-type Ca(2+) current (I(Ca)) by the two nitric oxide (NO) donors sodium nitroprusside (SNP, 1 microM to 1 mM) and (+/-)-S-nitroso-N-acetylpenicillamine (SNAP, 3 or 10 microM) was investigated in frog ventricular myocytes using double voltage clamp and double-barrelled microperfusion techniques. 2. SNP and SNAP depressed the isoprenaline (ISO, 10-100 nM)- or forskolin (FSK, 1 microM)-mediated stimulation of I(Ca) via cGMP activation of the cGMP-stimulated phosphodiesterase (PDE2). Complete inhibition of the ISO (100 nM) response was observed at 1 mM SNP. 3. When SNP was applied locally, i.e. to one-half of the cell, and ISO to the whole cell, the response of I(Ca) to ISO was strongly antagonized in the cell half exposed to SNP (up to 100 % inhibition at 1 mM SNP) but a relatively small depression was observed in the other half of the cell (only 20 % inhibition at 1 mM SNP). 4. The NO scavenger 2-(4-carboxyphenyl)-4,4,5,5-tetramethylimidazoline-1-oxyl 3-oxide (carboxy-PTIO, 1 mM) reversed the local effect of SNAP (3 microM) on FSK-stimulated I(Ca) when applied to the same side as the NO donor, but had no effect when applied to the other side of the cell. 5. A local application of erythro-9-(2-hydroxy-3-nonyl)adenine (EHNA, 30 microM), a selective inhibitor of PDE2, fully reversed the local effect of SNP (100 microM) or SNAP (10 microM) on I(Ca) but had no effect on the distant response. 6. When EHNA was applied on the distant side, with SNP (1 mM) and ISO (100 nM) applied locally, the distant effect of SNP was fully reversed. 7. Our results demonstrate that in frog ventricular myocytes stimulation of guanylyl cyclase by NO leads to a strong local depletion of cAMP near the L-type Ca(2+) channels due to activation of PDE2, but only to a modest reduction of cAMP in the rest of the cell. This may be explained by the existence of a tight microdomain between L-type Ca(2+) channels and PDE2.  (+info)

NO-cGMP pathway increases the hyperpolarisation-activated current, I(f), and heart rate during adrenergic stimulation. (4/68)

OBJECTIVES: The role of the nitric oxide (NO)-cGMP pathway in the autonomic modulation of cardiac pacemaking is controversial and may involve an interplay between the L-type calcium current, I(CaL), and the hyperpolarisation activated current, I(f). We tested the hypothesis that following adrenergic stimulation, the NO-cGMP pathway stimulates phosphodiesterase 2 (PDE2) to reduce cAMP dependent stimulation of I(f) and heart rate (HR). METHODS: In the presence of norepinephrine (NE, 1 microM), the effects of the NO donor sodium nitroprusside (SNP) were evaluated in sinoatrial node (SAN)/atria preparations and isolated SAN cells from adult guinea pigs. RESULTS: Contrary to our hypothesis, SNP (10 and 100 microM, n=5) or the membrane permeable cGMP analogue, 8Br-cGMP (0.5 mM, n=6) transiently increased HR by 5+/-1, 12+/-1 and 12+/-2 beats/min, respectively. The guanylyl cyclase inhibitor 1H-(1,2,4)-oxadiazolo-(4,3-a)-quinoxalin-1-one (ODQ, 10 microM, n=5) abolished the increase in HR to SNP (100 microM) as did the I(f) blockers caesium chloride (2 mM, n=7) and 4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino)-pyrimidinium chloride (ZD7288, 1 microM, n=7). Addition of SNP (10 microM) also transiently increased I(f) in SAN cells (n=5). After inhibition of PDE2 with erythro-9-(2-hydroxy-3-nonyl)-adenine (EHNA, 10 microM, n=5), the increase in HR to SNP in the presence of NE was significantly augmented and maintained. RT-PCR analysis confirmed the presence of PDE2 in addition to cGMP inhibited PDE3 mRNA in central SAN tissue. CONCLUSIONS: These results suggest that during adrenergic stimulation, activation of the NO-cGMP pathway does not decrease HR, but has a transient stimulatory effect that is I(f) dependent, and is limited in magnitude and duration by stimulation of PDE2.  (+info)

The cAMP-specific phosphodiesterase TbPDE2C is an essential enzyme in bloodstream form Trypanosoma brucei. (5/68)

Chemotherapy of human sleeping sickness, a fatal disease caused by the protozoan parasite Trypanosoma brucei, is in a dismal state, and the identification and characterization of new drug targets is an urgent prerequisite for an improvement of the dramatic situation in the field. Over the last several years, inhibitors of cyclic nucleotide-specific phosphodiesterases have proven to be highly successful drug candidates for an assortment of clinical conditions. Their potential as antiparasitic drugs has not been explored so far. This study reports the characterization of a cAMP-specific phosphodiesterase from T. brucei, TbPDE2C. This enzyme is a class I phosphodiesterase, and it is a member of a small enzyme family in T. brucei, TbPDE2. Inhibitors of this enzyme block the proliferation of bloodstream form trypanosomes in culture. RNA interference experiments demonstrated that the TbPDE2 family, and in particular TbPDE2C, are essential for maintaining intracellular cAMP concentrations within a physiological range. Bloodstream form trypanosomes are exquisitely sensitive to elevated concentrations of intracellular cAMP, and a disruption of TbPDE2C function quickly leads to the disruption of nuclear and cellular cell division, and to cell death. TbPDE2C might represent a novel drug target for the development of new and effective trypanocidal drugs.  (+info)

Cloning and characterization of a cAMP-specific phosphodiesterase (TbPDE2B) from Trypanosoma brucei. (6/68)

Here we report the cloning, expression, and characterization of a cAMP-specific phosphodiesterase (PDE) from Trypanosoma brucei (TbPDE2B). Using a bioinformatic approach, two different expressed sequence tag clones were identified and used to isolate the complete sequence of two identical PDE genes arranged in tandem. Each gene consists of 2,793 bases that predict a protein of 930 aa with a molecular mass of 103.2 kDa. Two GAF (for cGMP binding and stimulated PDEs, Anabaena adenylyl cyclases, and Escherichia coli FhlA) domains, similar to those contained in many signaling molecules including mammalian PDE2, PDE5, PDE6, PDE10, and PDE11, were located N-terminal to a consensus PDE catalytic domain. The catalytic domain is homologous to the catalytic domain of all 11 mammalian PDEs, the Dictyostelium discoideum RegA, and a probable PDE from Caenorhabditis elegans. It is most similar to the T. brucei PDE2A (89% identity). TbPDE2B has substrate specificity for cAMP with a K(m) of 2.4 microM. cGMP is not hydrolyzed by TbPDE2B nor does this cyclic nucleotide modulate cAMP PDE activity. The nonselective PDE inhibitors 3-isobutyl-1-methylxanthine, papaverine and pentoxifyline are poor inhibitors of TbPDE2B. Similarly, PDE inhibitors selective for the mammalian PDE families 2, 3, 5, and 6 (erythro-9-[3-(2-hydroxynonyl)]-adenine, enoximone, zaprinast, and sildenafil) were also unable to inhibit this enzyme. However, dipyridamole was a reasonably good inhibitor of this enzyme with an IC50 of 27 microM. cAMP plays key roles in cell growth and differentiation in this parasite, and PDEs are responsible for the hydrolysis of this important second messenger. Therefore, parasite PDEs, including this one, have the potential to be attractive targets for selective drug design.  (+info)

Hydrolysis of N-methyl-D-aspartate receptor-stimulated cAMP and cGMP by PDE4 and PDE2 phosphodiesterases in primary neuronal cultures of rat cerebral cortex and hippocampus. (7/68)

Stimulation of N-methyl-D-aspartate (NMDA) receptors on neurons activates both cAMP and cGMP signaling pathways. Experiments were carried out to determine which phosphodiesterase (PDE) families are involved in the hydrolysis of the cyclic nucleotides formed via this mechanism, using primary neuronal cultures prepared from rat cerebral cortex and hippocampus. The nonselective PDE inhibitor 3-isobutyl-1-methylxanthine (IBMX) potentiated the ability of NMDA to increase cAMP and cGMP. However, among the family-selective inhibitors, only the PDE4 inhibitor rolipram enhanced the ability of NMDA to increase cAMP in the neurons. In contrast, only the PDE2 inhibitor erythro-9-(2-hydroxy-3-nonyl) adenine (EHNA) enhanced the ability of NMDA to increase cGMP. Neither adenosine nor an adenosine deaminase inhibitor mimicked the effect of EHNA; this suggests that EHNA's inhibition of PDE2, not its effects on adenosine metabolism, mediates its effects on NMDA-stimulated cGMP concentrations. The PDE inhibitor-augmented effects of NMDA on cAMP and cGMP formation were antagonized by 5-methyl-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imine maleate (MK-801), verifying NMDA receptor mediation. In contrast, only NMDA-mediated cGMP formation was affected by altering either nitric oxide signaling or guanylyl cyclase; this suggests that NMDA-induced changes in cAMP are not secondary to altered cGMP concentrations. Overall, the present findings indicate that cAMP and cGMP formed in neurons as a result of NMDA receptor stimulation are hydrolyzed by PDE4 and PDE2, respectively. Selective inhibitors of the two PDE families will differentially affect the functional consequences of activation of these two signaling pathways by NMDA receptor stimulation.  (+info)

Attenuation of cAMP accumulation in adult rat cardiac fibroblasts by IL-1beta and NO: role of cGMP-stimulated PDE2. (8/68)

Treatment of cultured adult rat cardiac fibroblasts with interleukin-1beta (IL-1beta) induces the inducible nitric oxide synthase (iNOS) expression, increases nitric oxide (NO) and cGMP production, and attenuates cAMP accumulation in response to isoproterenol by ~50%. Reduced cAMP accumulation is due to NO production: the effect is mimicked by NO donors and prevented by N(G)-monomethyl-L-arginine, an NOS inhibitor. Effects of NO are not restricted to the beta-adrenergic response; the response to forskolin is similarly diminished. NO donors only slightly (12%) decrease forskolin-stimulated adenylyl cyclase (AC) activity in cardiac fibroblast plasma membranes, suggesting that the main effect of NO is not a direct one on AC. An inhibitor of soluble guanylyl cyclase inhibits the effects of IL-1beta and NO donors; inhibition of cGMP-dependent protein kinase is without effect. 3-Isobutyl-1-methylxanthine, a nonspecific phosphodiesterase (PDE) inhibitor, and erythro-9-(2-hydroxy-3-nonyl)adenine, a specific inhibitor of the cGMP-stimulated PDE (PDE2), completely restore cAMP accumulation in sodium nitroprusside-treated fibroblasts and largely reverse the attenuated response in IL-1beta-treated fibroblasts. Although NO reportedly acts by reducing AC activity in some cells, in cardiac fibroblasts NO production decreases cAMP accumulation largely by the cGMP-mediated activation of PDE2.  (+info)

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To date, just one structural class of cyclic nucleotide receptors has been characterized, that comprises the bacterial CAP (McKay and Steitz, 1981), the cyclic nucleotide‐regulated protein kinases PKG and PKA (Weber et al., 1989; Su et al., 1995) and the cyclic nucleotide‐gated ion channels (Altenhofen et al., 1991; Kumar and Weber, 1992). This class has been referred to as the cNMP domain family (Schultz et al., 1998). The GAF domains of the cGMP‐regulated PDEs represented a potentially different class of cyclic nucleotide receptors, since they lacked any sequence homology to the cNMP motif. The structure of the YKG9 protein shows no similarity to the cNMP domain and thus establishes beyond any doubt that there are at least two entirely different structural classes of cyclic nucleotide receptors.. The YKG9 structure provides a three‐dimensional template for modeling other GAF domains, including those of the PDEs. The use of multiple threading alignment based on the solved structure ...
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Cyclic nucleotide phosphodiesterases (PDEs) are the only enzymes that degrade the cyclic nucleotides cAMP and cGMP, and play a key role in modulating the amplitude and duration of the signal delivered by these two key intracellular second messengers. Defects in cyclic nucleotide signalling are known to be involved in several pathologies. As a consequence, PDEs have long been recognized as potential drug targets, and they have been the focus of intense research for the development of therapeutic agents. A number of PDE inhibitors are currently available for the treatment of disease, including obstructive pulmonary disease, erectile dysfunction, and heart failure. However, the performance of these drugs is not always satisfactory, due to a lack of PDE-isoform specificity and their consequent adverse side effects. Recent advances in our understanding of compartmentalised cyclic nucleotide signalling and the role of PDEs in local regulation of cAMP and cGMP signals offers the opportunity for the development
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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 ...
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 ...
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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 …
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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 …
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 ...
At this time it is expected that isooctanol will not be a reproductive toxicant. A one-generation study in rats (Hansen, 1992) was performed with the analog substance 1-dodecanol (CAS RN 112-53-8) using the Combined Repeat Dose and Reproductive/Developmental Toxicity Screening Test protoc ol. Male and female rats were administered 1-dodecanol orally via the feed at doses of 100, 500 and 2000 mg/kg/day for a period of 14 days. No effects were seen on reproductive or developmental parameters up to doses of 2000 mg/kg/day. 1-Dodecanol at the dose administered had no influence on body weight, weight gain, food consumption and reproductive efficiency in the parental generation. Pregnancy rates were not statistically altered and there were no differences in the lengths of the gestation periods. No organ toxicity was observed in the females, and there was no effect on the number of pups per litter, weight, sex ratio, or mortality rate from Days 1 to 5 after birth. Test data that will be collected as ...
EHNA is a selective inhibitor of the cGMP-specific phosphodiesterase (PDE2) (IC₅₀s = 0.8 and 2 μM from human and porcine myocardium, respectively, 3.5 μM in rat hepatocyte, and 5.5 μM in human platelet).
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].
The IUPHAR/BPS Guide to Pharmacology. EHNA ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
MacPherson, M., Broderick, K., Graham, S., Day, J., Houslay, M., Dow, J. and Davies, S. (2004) The dg2 (for) gene confers a renal phenotype in Drosophila by modulation of cGMP-specific phosphodiesterase. Journal of Experimental Biology, 207, pp. 2769-2776. (doi:10.1242/jeb.01086) ...
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NMDA and nitric oxide act through the cGMP signal transduction pathway to repress hypothalamic gonadotropin-releasing hormone gene expression.s profile, publications, research topics, and co-authors
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.
Andrea Carter, Susan Spiller, Eve Isabelle Charbonneau, Paulina Delgado, Stephanie Kwong, Thomas Huser, Nathan Rockwell, and Clark Lagarias. We are currently studying a family of cyanobacteriochromes through the use of a bacterium called Thermosynechococcus elongatus, which is a member of a family of thermophilic bacteria that contain cyanobacteriochromes. Cyanobacteriochromes contain GAF domains related to phytochromes. We are currently working with five genes from the genome of T. elongatus with class II GAF domains. GAF domains are blue/green photoreversible. This means that the organism can absorb green and blue photons, and once it is excited above a certain threshold in either color, it will reverse back to absorbing the opposite color, blue or green respectively. The genes we worked with include tlr0924, tll0569, tll0899, tlr0911, and tlr1999. All of these genes have been successfully truncated to GAF domain only and some have been expressed. I specifically worked with tlr1999 gene. Our ...
Increases of cAMP are controlled by the enzyme adenylate cyclase (sAC). This enzyme produces cAMP molecules from the cellular energy reservoir adenosyne triphosphate (ATP). In order for the enzyme to assume this catalytic function, it itself has to be activated, e.g. by bicarbonate.. • The opposite process, e.g. the reduction of cAMP levels, is initiated by another enzyme. The protein involved here originates from the family of phosphodiesterases (PDE); to be precise, an isoform of PDE2A. This enzyme must also be activated so that it may reduce the amount of cAMP contained in the mitochondria. This process is performed by molecules which aggregate along an area at the end of the protein, the N-terminus of the PDE2A molecules.. In this manner, the messenger cAMP acts as an enzyme controlled switch which strengthens or weakens the energy metabolism. The position of the switch is determined by which of the two enzymes dominates: Adenylate cyclase (sAC) increases the amount of cAMP, ...
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HormoneStimuli for ReleaseMechanism of Synthesis/ReleaseTarget Tissue(s)Effects and MOAFeedback RegulationACTHCorticotrophs (CRH)Exocytosis; increase cAMP, which activates PKAAdrenal GlandStimulates production of glucocor...
Cyclic nucleotide phosphodiesterases (PDEs) are important regulators of signal transduction processes mediated by cAMP and cGMP. One PDE family member, PDE3B, plays an important role in the regulation of a variety of metabolic processes such as lipolysis and insulin secretion. In this study, the cellular localization and the role of PDE3B in the regulation of triglyceride, cholesterol and glucose metabolism in hepatocytes were investigated. PDE3B was identified in caveolae, specific regions in the plasma membrane, and smooth endoplasmic reticulum. In caveolin-1 knock out mice, which lack caveolae, the amount of PDE3B protein and activity were reduced indicating a role of caveolin-1/caveolae in the stabilization of enzyme protein. Hepatocytes from PDE3B knock out mice displayed increased glucose, triglyceride and cholesterol levels, which was associated with increased expression of gluconeogenic and lipogenic genes/enzymes including, phosphoenolpyruvate carboxykinase, peroxisome ...
The IUPHAR/BPS Guide to Pharmacology. phosphodiesterase 4D - Phosphodiesterases, 3,5-cyclic nucleotide (PDEs). Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
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"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 ... EHNA (erythro-9-(2-hydroxy-3-nonyl)adenine) is a potent adenosine deaminase inhibitor, ...
Essayan DM (November 2001). "Cyclic nucleotide phosphodiesterases". J. Allergy Clin. Immunol. 108 (5): 671-80. doi:10.1067/mai. ... Cannabinoid type 2 receptor-dependent and -independent immunomodulatory effects". J. Biol. Chem. 281 (20): 14192-206. doi: ... "Binding and Functional Comparisons of Two Types of Tumor Necrosis Factor Antagonists". Journal of Pharmacology and Experimental ... 180 (2): 688-92. doi:10.4049/jimmunol.180.2.688. PMID 18178805. S2CID 45744340. "A new view of drugs used to treat rheumatoid ...
Cyclic-nucleotide 3'-phosphodiesterase (CNPase) List of human cell types derived from the germ layers Carlson, Neil (2010). ... Oligodendrocytes are a type of glial cell. They arise during development from oligodendrocyte precursor cells (OPCs), which can ... They are the last cell type to be generated in the CNS. Oligodendrocytes were discovered by Pío del Río Hortega. ... Oligodendrocytes (from Greek 'cells with a few branches'), or oligodendroglia, are a type of neuroglia whose main functions are ...
... 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 ... 45 (2): 388-402. doi:10.1007/s12035-012-8250-4. hdl:10261/60667. PMID 22396213. S2CID 12709387. Weiss JL, Hui H, Burgoyne RD ( ...
"Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... cyclic 3',5'-nucleotide phosphodiesterase, cyclic 3',5'-phosphodiesterase, 3',5'-nucleotide phosphodiesterase, 3':5'-cyclic ... monophosphate phosphodiesterase (cyclic CMP), cyclic 3',5-nucleotide monophosphate phosphodiesterase, nucleoside 3',5'-cyclic ... cyclic AMP 3',5'-cyclic dAMP 3',5'-cyclic IMP 3',5'-cyclic GMP 3',5'-cyclic CMP There are 11 distinct phosphodiesterase ...
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. " ... High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B is an enzyme that in humans is encoded by ...
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 ... a proposed class of living organisms smaller than the accepted lower limit size for life 2',3'- ...
"Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Advances in Cyclic ... Fertel R, Weiss B (July 1976). "Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung" ( ... cGMP-specific phosphodiesterase type 5 is an enzyme (EC 3.1.4.17) from the phosphodiesterase class. It is found in various ... Weiss B, Hait WN (1977). "Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annual ...
"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 ...
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). Being a Russian company, they did not seek approval ... Emoxypine (2-ethyl-6-methyl-3-hydroxypyridine), also known as Mexidol or Mexifin when used as the succinate salt, is an ... Gruber W (1953). "Synthesis of 3-Hydroxy-2-alkylpyridines". Canadian Journal of Chemistry. 31 (6): 564-568. doi:10.1139/v53-079 ...
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 ( ... Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C is an enzyme that in humans is encoded by the PDE1C ... Rybalkin SD, Rybalkina I, Beavo JA, Bornfeldt KE (2002). "Cyclic nucleotide phosphodiesterase 1C promotes human arterial smooth ...
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. ...
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 ...
"Positive inotropic effect of the inhibition of cyclic GMP-stimulated 3',5'-cyclic nucleotide phosphodiesterase (PDE2) on guinea ... As different PDE types may affect different cAMP pools, the different PDEs may regulate different processes in the cell. PDE2 ... "Biologic regulation through opposing influences of cyclic GMP and cyclic AMP: the Yin Yang hypothesis". Adv Cyclic Nucleotide ... June 1997). "cGMP-stimulated cyclic nucleotide phosphodiesterase regulates the basal calcium current in human atrial myocytes ...
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). pApA is also ... "Cyclic nucleotides in archaea: Cyclic di-AMP in the archaeon Haloferax volcanii and its putative role". MicrobiologyOpen. 8 (9 ...
Cyclic-nucleotide 3'-phosphodiesterase and multiple molecules of the Immune system. GRCh38: Ensembl release 89: ENSG00000197971 ... In general, the major form of MBP is a protein of about 18.5 Kd (170 residues). In melanocytic cell types, MBP gene expression ... 47 (2): 614-6. doi:10.1111/j.1471-4159.1986.tb04544.x. PMID 2426402. Roth HJ, Kronquist K, Pretorius PJ, et al. (1986). " ... 24 (2): 113-34. doi:10.1016/0009-9120(91)90421-a. PMID 1710177. Inouye H, Kirschner DA (January 1991). "Folding and function of ...
... is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor. ... The effect of bucladesine as a cAMP analog has been studied on the pentylenetetrazol-induced seizure in the wild-type mice. The ... Bucladesine (50-100nM/mouse) showed significant attenuation in the morphine withdrawal syndrome in the wild-type mice. In ... 670 (2-3): 464-70. doi:10.1016/j.ejphar.2011.09.026. PMID 21946102. Seyedi SY, Salehi F, Payandemehr B, Hossein S, Hosseini- ...
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 ...
"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 ... Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit beta is the beta subunit of the protein complex PDE6 that is encoded ...
September 2003). "Cyclic nucleotide phosphodiesterase activity, expression, and targeting in cells of the cardiovascular system ... PDE3A can be either membrane-associated or cytosolic, depending on the variant and the cell type it is expressed in. PDE3A and ... Lugnier C (March 2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific ... WO 03012030, Movsesian M, "Isoform-Selective Inhibitors and Activators of PDE3 Cyclic Nucleotide Phosphodiesterases", published ...
Cyclic-nucleotide 3'-phosphodiesterase. Moreover, oligodendrocytes also developed and migrated into fiber bundles in mice when ... Using doses between 1 μM to 3 μM of RA can generate neurons as the most abundant cell type. Neurons under this treatment ... 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 ...
Sun L, Wu J, Du F, Chen X, Chen ZJ (February 2013). "Cyclic GMP-AMP synthase is a cytosolic DNA sensor that activates the type ... cGAMP was found to be much more potent than other cyclic di-nucleotides (c-di-GMP and c-di-AMP). cGAMP was shown to ... phosphodiesterases. Other advantages of the unique 2'-5' linkage may be that cGAMP is able to bind multiple allelic variants of ... Cyclic GMP-AMP (cGAMP) is a cyclic dinucleotide (CDN) and the first to be found in metazoans. Other CDNs (c-di-GMP and c-di-AMP ...
... by adenylyl cyclase and metabolized by cyclic nucleotide phosphodiesterases (PDEs). One manifestation of depression is an ... a type of glutamate receptor - produces rapid (within 2 hours), robust and sustained (lasting for up to a fortnight) ... Rodent studies have consistently shown upregulation of the 3, 5-cyclic adenosine monophosphate (cAMP) system induced by ... "Interaction between the antidepressant-like behavioral effects of beta adrenergic agonists and the cyclic AMP PDE inhibitor ...
... cyclic-GMP phosphodiesterase MeSH D08.811.277.352.640.150 - 3',5'-cyclic-nucleotide phosphodiesterase MeSH D08.811.277.352. ... myosin type iii MeSH D08.811.277.040.025.525.843 - myosin type iv MeSH D08.811.277.040.025.525.875 - myosin type v MeSH D08.811 ... cyclic-nucleotide phosphodiesterases MeSH D08.811.277.352.640.295 - glycerophosphoinositol inositolphosphodiesterase MeSH ... cyclic nucleotide-regulated protein kinases MeSH D08.811.913.696.620.682.700.150.125 - cyclic amp-dependent protein kinases ...
He is best known for his work with cyclic nucleotide phosphodiesterases. He was the first to propose, based on his experimental ... He showed that a single cell type may contain more than one form of phosphodiesterase [6,7] and that different forms of ... one on the potential therapeutic application of cyclic nucleotides: (Weiss, Benjamin, ed., Cyclic Nucleotides in Disease[1]), ... Cyclic Nucleotide Phosphodiesterases: Weiss and co-workers developed rapid phosphodiesterease assays [3, 4], separated ...
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 ...
"Functional and biochemical evidence for diazepam as a cyclic nucleotide phosphodiesterase type 4 inhibitor". British Journal of ... A phosphodiesterase type 4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action ... Barad M, Bourtchouladze R, Winder DG, Golan H, Kandel E (1998). "Rolipram, a type IV-specific phosphodiesterase inhibitor, ... Dinter, H (February 2000). "Phosphodiesterase type 4 inhibitors: potential in the treatment of multiple sclerosis?". BioDrugs. ...
The GTP form of the α subunit of transducin (Gt) activates the cyclic GMP phosphodiesterase from retinal rod outer segments, ... Fung BK, Hurley JB, Stryer L (January 1981). "Flow of information in the light-triggered cyclic nucleotide cascade of vision". ... More than one type of G protein co-exist in the same tissue. For example, in adipose tissues, two different G-proteins with ... When ligands bind a GPCR, the GPCR acquires GEF (guanine nucleotide exchange factor) ability, which activates the G-protein by ...
Lugnier, C. (2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: A new target for the development of specific ... "Phosphodiesterase type-5 inhibitor use in type 2 diabetes is associated with a reduction in all-cause mortality". Heart. 102 ( ... Yu, J. Y.; Kang, K. K. & Yoo, M. (2006). "Erectile potentials of a new phosphodiesterase type 5 inhibitor, DA-8159, in diet- ... McMahon, C. G.; McMahon, C. N.; Leow, L. J. & Winestock, C. G. (2006). "Efficacy of type-5 phosphodiesterase inhibitors in the ...
This G protein subunit activates a taste phosphodiesterase and decreases cyclic nucleotide levels. Further steps in the ... taste+receptors,+type+1 at the US National Library of Medicine Medical Subject Headings (MeSH) taste+receptors,+type+2 at the ... The HCN channels were such a proposal; as they are cyclic nucleotide-gated channels. The two ion channels now suggested to ... Type 1, sweet, first characterized in 2001: TAS1R2 - TAS1R3 Type 2, bitter, first characterized in 2000: In humans there are 25 ...
Unstimulated (in the dark), cyclic-nucleotide gated channels in the outer segment are open because cyclic GMP (cGMP) is bound ... One type of photosensitive pigment Three types of photosensitive pigment in humans ... Each transducin then activates the enzyme cGMP-specific phosphodiesterase (PDE).. *PDE then catalyzes the hydrolysis of cGMP to ... resulting in the closure of cyclic nucleotide-gated Na+ ion channels located in the photoreceptor outer segment membrane. ...
... resulting in the closing of Na+ cyclic nucleotide-gated ion channels (CNGs). Thus the cell is hyperpolarised. The amount of ... A third type of light-sensing cell, the photosensitive ganglion cell, is important for entrainment of circadian rhythms and ... This in turn causes the Ga-subunit of the protein to activate a phosphodiesterase (PDE6), which degrades cGMP, ... There are two types of centre-surround structures in the retina - on-centres and off-centres. On-centres have a positively ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... LIPE, AOMS4, FPLD6, HSL, LHS, lipase E, hormone sensitive type. External IDs. OMIM: 151750 MGI: 96790 HomoloGene: 3912 ... which is necessary for lipid mobilization in response to cyclic AMP, which itself is provided by the activation of Gs protein- ... 291 (2): 286-90. doi:10.1006/bbrc.2002.6427. PMID 11846402.. *. Ylitalo K, Nuotio I, Viikari J, et al. (2002). "C3, hormone- ...
Johner, A., Kunz, S., Linder, M., Shakur, Y. and Seebeck, T. (2006). "Cyclic nucleotide specific phosphodiesterases of ... http://www.garlandscience.com/textbooks/0815323042.asp?type=reviews. *Irwin H. Segel. Enzyme Kinetics: Behavior and Analysis of ... B enzm: 1.1/2/3/4/5/6/7/8/10/11/13/14/15-18, 2.1/2/3/4/5/6/7/8, 2.7.10, 2.7.11-12, 3.1/2/3/4/5/6/7, 3.1.3.48, 3.4.21/22/23/24, ... B enzm: 1.1/2/3/4/5/6/7/8/10/11/13/14/15-18, 2.1/2/3/4/5/6/7/8, 2.7.10, 2.7.11-12, 3.1/2/3/4/5/6/7, 3.1.3.48, 3.4.21/22/23/24, ...
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 is a protein that in humans is encoded by the GNB1 gene.[5] ... type 1 angiotensin receptor binding. • protein complex binding. • signal transducer activity. • protein binding. • GTPase ... 3',5'-cyclic-GMP phosphodiesterase. *Protein kinase G. *G alpha subunit Gα *GNAO1 ... retina development in camera-type eye. • Ras protein signal transduction. • cell proliferation. • cellular response to hypoxia ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... The third type of glucose 6-phosphatase deficiency, glucose 6-phosphatase-β deficiency, is characterized by a congenital ... 1993). "Glycogen Storage Disease Type I". PMID 20301489.. Cite journal requires ,journal=. (help). ... Chou JY, Matern D, Mansfield BC, Chen YT (March 2002). "Type I glycogen storage diseases: disorders of the glucose-6- ...
3 Types of G protein signaling *3.1 Heterotrimeric G proteins *3.1.1 Common mechanism *3.1.1.1 Activation ... 3',5'-cyclic-GMP phosphodiesterase. *Protein kinase G. *G alpha subunit Gα *GNAO1 ... G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside ... Types of G protein signaling[edit]. G protein can refer to two distinct families of proteins. Heterotrimeric G proteins, ...
... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... guanyl-nucleotide exchange factor activity. • RNA binding. Cellular component. • cytoplasm. • ciliary basal body. • centrosome ... "Analysis of the RPGR gene in 11 pedigrees with the retinitis pigmentosa type 3 genotype: paucity of mutations in the coding ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... It is suggested that 57 enzymes fall into the type I category whereas the rest fall into the type II group, including the ... and there are two classifications of these enzymes including type I and type II. ... Other types of PET degrading hydrolases have been known before this discovery.[2] These include hydrolases such as: lipases, ...
Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was ... Involved in growth and metastasis of some types of tumors.[24]. *Used in the endocrine system for peptide and amino-acid ... When a ligand binds to the GPCR it causes a conformational change in the GPCR, which allows it to act as a guanine nucleotide ... These signals then can be terminated by cAMP phosphodiesterase, which is an enzyme that degrades cAMP to 5'-AMP and inactivates ...
Because RETGC-1 produces cGMP, which keeps cyclic nucleotide-gated channels open allowing the influx of calcium, this mutation ... Types[edit]. There are membrane-bound (type 1, guanylate cyclase-coupled receptor) and soluble (type 2, soluble guanylate ... Once formed, cGMP can be degraded by phosphodiesterases, which themselves are under different forms of regulation, depending on ... Depending on cell type, it can drive adaptive/developmental changes requiring protein synthesis. In smooth muscle, cGMP is the ...
Essayan DM (November 2001). "Cyclic nucleotide phosphodiesterases". The Journal of Allergy and Clinical Immunology. 108 (5): ... Studies have found that Paraxanthine is a phosphodiesterase type 9 (PDE9) inhibitor[13] and It's sold as a research molecule ... "Phosphodiesterase-9 (PDE9) inhibition with BAY 73-6691 increases corpus cavernosum relaxations mediated by nitric oxide-cyclic ... PDE9 is a cGMP preferring phosphodiesterase and It's expressed in corpus cavernosum as high as PDE5 is.[15] ...
"Differential Activation and Inhibition of the Multiple Forms of Cyclic Nucleotide Phosphodiesterase". Advances in Cyclic ... is a drug used to block the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth ... Weiss, B; Hait, W N (1977). "Selective Cyclic Nucleotide Phosphodiesterase Inhibitors as Potential Therapeutic Agents". Annual ... Fertel, Richard; Weiss, Benjamin (1976). "Properties and Drug Responsiveness of Cyclic Nucleotide Phosphodiesterases of Rat ...
Yeast tRNA cyclic phosphodiesterase cleaves the cyclic phosphodiester group to form a 2'-phosphorylated 3' end. Yeast tRNA ... exon then performs a nucleophilic attack at the first nucleotide following the last nucleotide of the intron at the 3' splice ... This type of splicing is termed canonical splicing or termed the lariat pathway, which accounts for more than 99% of splicing. ... Splicing occurs in all the kingdoms or domains of life, however, the extent and types of splicing can be very different between ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Types. *EC1 Oxidoreductases (list). *EC2 Transferases (list). *EC3 Hydrolases (list). *EC4 Lyases (list) ... O-phospho-L(or D)-serine + H2O ⇌. {\displaystyle \rightleftharpoons }. L(or D)-serine + phosphate ion. This enzyme belongs to ...
Kaupp UB, Seifert R (July 2002). "Cyclic nucleotide-gated ion channels". Physiol. Rev. 82 (3): 769-824. CiteSeerX 10.1.1.319. ... cAMP phosphodiesterase converts cAMP into AMP by breaking the phosphodiester bond, in turn reducing the cAMP levels ... which vary based on the type of cell. ... cyclic nucleotide-gated ion channels[9]. *exchange proteins ... caffeine and theophylline inhibit cAMP phosphodiesterase, which degrades cAMP - thus enabling higher levels of cAMP than would ...
This compound is a potent inhibitor of cGMP specific phosphodiesterase type 5, the enzyme that degrades the signalling molecule ... This block of nucleotide biosynthesis is more toxic to rapidly growing cells than non-dividing cells, since a rapidly growing ... cyclic guanosine monophosphate.[40] This signalling molecule triggers smooth muscle relaxation and allows blood flow into the ... Although it is possible for mixed-type inhibitors to bind in the active site, this type of inhibition generally results from an ...
The cyclic AMP-regulatory dimers are degraded by phosphodiesterase and release 5'AMP. DNA in the cell nucleus binds to ... G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger. • activation of adenylate cyclase ... LHCGR have been found in many types of extragonadal tissues, and the physiologic role of some has remained largely unexplored. ... Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was ...
Known genetic causes of this are mutations in the cone cell cyclic nucleotide-gated ion channels CNGA3 (ACHM2) and CNGB3 (ACHM3 ... This α-subunit then activates a phosphodiesterase that catalyzes the conversion of cGMP to GMP, thereby reducing current ... though in some cases the truncated proteins may be able to coassemble with wild-type channels in a dominant negative fashion. ... There are at least four genetic causes of congenital ACHM, two of which involve cyclic nucleotide-gated ion channels (ACHM2/ ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Phosphodiesterase type 11 (PDE11) is a type of phosphodiesterase enzyme. An inhibitor is BC11-38. ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... "Demonstration of functionally different interactions between phospholipase C-gamma and the two types of platelet-derived growth ... For example, when activated by SRC, the encoded protein causes the Ras guanine nucleotide exchange factor RASGRP1 to ... 249 (2): 537-41. doi:10.1006/bbrc.1998.9177. PMID 9712732.. *^ Bedrin MS, Abolafia CM, Thompson JF (July 1997). "Cytoskeletal ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... 1994). "New type of linkage between a carbohydrate and a protein: C-glycosylation of a specific tryptophan residue in human ... "Entrez Gene: RNASE2 ribonuclease, RNase A family, 2 (liver, eosinophil-derived neurotoxin)".. ... to chromosome 19 and the human ribonuclease 2 (eosinophil-derived neurotoxin) and ribonuclease 3 (eosinophil cationic protein) ...
... acts as a phosphodiesterase (PDE) type-1 inhibitor in isolated rabbit aorta,[12] Independent of vinpocetine's ... Hagiwara M, Endo T, Hidaka H (February 1984). "Effects of vinpocetine on cyclic nucleotide metabolism in vascular smooth muscle ... 72 (2): 84-91. PMID 12498034.. *^ "Vinpocetine. Monograph" (PDF). Alternative Medicine Review. 7 (3): 240-3. June 2002. PMID ... 107 (22): 9921-2. Bibcode:2010PNAS..107.9921M. doi:10.1073/pnas.1005138107. PMC 2890434 . PMID 20495091.. ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Types. *EC1 Oxidoreductases (list). *EC2 Transferases (list). *EC3 Hydrolases (list). *EC4 Lyases (list) ... Low levels have also been detected in the lung, prostate and lymph nodes.[2] ... Universal protein resource accession number Q8WZ79 for "DNASE2B - Deoxyribonuclease-2-beta precursor - Homo sapiens (Human) - ...
Single-nucleotide polymorphisms (SNPs) in the P2RX7 receptor gene are associated with an increased risk of bone fracture. The ... There are two types of NTs: Concentrative nucleoside transporters (CNTs): Na+-dependent symporters Equilibrative nucleoside ... the ectonucleotide pyrophosphatase/phosphodiesterases (E-NPPs) and alkaline phosphatases (APs). Extracellular AMP is hydrolyzed ... for sustained platelet aggregation through the inhibition of adenylate cyclase and a corresponding decrease in cyclic adenosine ...
"Biologic regulation through opposing influences of cyclic GMP and cyclic AMP: the Yin Yang hypothesis". Adv Cyclic Nucleotide ... As different PDE types may affect different cAMP pools, the different PDEs may regulate different processes in the cell.[9]. ... cyclic nucleotide phosphodiesterase (PDE2) on guinea pig left atria in eu- and hyperthyroidism" (PDF). Gen Physiol Biophys. 22 ... "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacol. Rev. 58 (3): 488-520. doi:10.1124/pr. ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Types. *EC1 Oxidoreductases (list). *EC2 Transferases (list). *EC3 Hydrolases (list). *EC4 Lyases (list) ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Type II[edit]. Type II site-specific deoxyribonuclease. Structure of the homodimeric restriction enzyme EcoRI (cyan and green ... Type V[edit]. Type V restriction enzymes (e.g., the cas9-gRNA complex from CRISPRs[43]) utilize guide RNAs to target specific ... Type l[edit]. Type I restriction enzymes were the first to be identified and were first identified in two different strains (K- ...
... cGMP in turn activates cyclic nucleotide-dependent protein kinase G, which phosphorylates various proteins that play a role in ... Here is a list of examples of the nitrate type (in alphabetical order): Acesaniamide[citation needed] Diethylene glycol ... PDE5 inhibitors block deactivation of cGMP by the enzyme phosphodiesterase-5. In combination with the increased cGMP production ... Guanylate cyclase produces cyclic guanosine monophosphate (cGMP) from guanosine triphosphate (GTP). ...
... cyclic nucleotide 3 phosphodiesterase ELISA Kits from leading suppliers on Biocompare. View specifications, prices, citations ... cyclic nucleotide 3 phosphodiesterase ELISA Kits. The ELISA (enzyme-linked immunosorbent assay) is a well-established antibody ... cyclic nucleotide 3 phosphodiesterase ELISA ELISA Kit across 10 suppliers. ... C-Type Natriuretic Peptide ELISA Kit *. Detection Target: C-Type Natriuretic Peptide ...
Phosphodiesterase 3B, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene ... cyclic-nucleotide phosphodiesterase activity and cGMP-inhibited cyclic-nucleotide phosphodiesterase activity. An important ... Analysis of the insulin-sensitive phosphodiesterase 3B gene in type 2 diabetes. (PMID: 11640991) Sano R … Saito Y (Diabetes ... 3,5-cyclic-nucleotide phosphodiesterase activity. EXP,TAS. 17884339. GO:0004115. 3,5-cyclic-AMP phosphodiesterase activity ...
Cyclic GMP as substrate and regulator of cyclic nucleotide phosphodiesterases (PDEs). Rev. Physiol. Biochem. Pharmacol. 135:67- ... Concentration and regulation of cyclic nucleotides, cyclic-nucleotide-dependent protein kinases and one of their major ... Cyclic nucleotide phosphodiesterases: relating structure and function. Prog. Nucleic Acid. Res. Mol. Biol. 65:1-52. ... Phosphorylation of phosphodiesterase-5 by cyclic nucleotide-dependent protein kinase alters its catalytic and allosteric cGMP- ...
Cyclic nucleotides cAMP and cGMP cooperate to ensure memory acquisition and consolidation. Increasing their levels by ... In type 2 diabetes mellitus (T2DM), the beneficial effect of.... Sub-efficacious doses of phosphodiesterase 4 and 5 inhibitors ... A piperazine derivative, PHOSPHODIESTERASE 5 INHIBITOR and VASODILATOR AGENT that is used as a UROLOGICAL AGENT in the ... Could chronic Vardenafil administration influence the cardiovascular risk in men with type 2 diabetes mellitus? ...
... cyclic-nucleotide 3′-phosphodiesterase type I isoforms are specifically recognized by IgG autoantibodies in multiple sclerosis ... cyclic-nucleotide 3′-phosphodiesterase. CNS. central nervous system. MuS. multiple sclerosis. MS/MS. tandem mass spectrometry. ... cyclic nucleotide 3′ phosphodiesterase as major autoantigen and C3 complement-binding protein in the pathogenesis of multiple ... 2008) Designed glycopeptides with different beta-turn types as synthetic probes for the detection of autoantibodies as ...
"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 ... EHNA (erythro-9-(2-hydroxy-3-nonyl)adenine) is a potent adenosine deaminase inhibitor, ...
"Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... cyclic 3,5-nucleotide phosphodiesterase, cyclic 3,5-phosphodiesterase, 3,5-nucleotide phosphodiesterase, 3:5-cyclic ... monophosphate phosphodiesterase (cyclic CMP), cyclic 3,5-nucleotide monophosphate phosphodiesterase, nucleoside 3,5-cyclic ... cyclic AMP 3,5-cyclic dAMP 3,5-cyclic IMP 3,5-cyclic GMP 3,5-cyclic CMP There are 11 distinct phosphodiesterase ...
Belongs to the cyclic nucleotide phosphodiesterase family.. Contains 2 GAF domains.. * Cellular localization ... By product type. Proteins and Peptides. Proteomics tools. Agonists, activators, antagonists and inhibitors. Lysates. Multiplex ... By product type. Primary antibodies. Secondary antibodies. ELISA, Matched Antibody Pairs and Multiplex Immunoassays. Cell and ... Defects in PDE6B are the cause of retinitis pigmentosa type 40 (RP40) [MIM:613801]. RP40 is a retinal dystrophy belonging to ...
... determine the factors required for the activity of these compounds and also for the selectivity versus other phosphodiesterase ... and benzothienothiadiazines derivatives as phosphodiesterase 7 inhibitors has been carried out in order to ... 3,5-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors* * Cyclic Nucleotide Phosphodiesterases, Type 7 ... A CoMFA study of benzo- and benzothienothiadiazines derivatives as phosphodiesterase 7 inhibitors has been carried out in order ...
The range of OPC to OL present in FCD type II does not implicate a primary failure o … ... These findings indicate a reduction of myelinated axons in the WM of FCD type II rather than dysmyelination as the primary ... cyclic nucleotide 3-phosphodiesterase (CNPase) and OL precursor cell (OPC) densities with platelet derived growth factor ... The range of OPC to OL present in FCD type II does not implicate a primary failure of cell recruitment and differentiation of ...
Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ... Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ... Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ... Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using ...
Cyclic nucleotide 3′-phosphodiesterase Rn.31762 3163 373 8.5 Cdh2 Cadherin 2, type 1, N-cadherin (neuronal) Rn.17239 2342 289 ... Gut NCSCs are self-renewing and multipotent, give rise to diverse types of neurons and glia in vivo, and persist in the gut ... and endothelin receptor type B (EDNRB)(12) (Tables 1 and 2). ... Endothelin receptor type B Rn.11412 1159 117 9.9 Cart Cocaine ... 2, A to D). Cells also migrated in the general direction of beads soaked in GDNF (Fig. 2E). This is consistent with reports ...
Cyclic GMP as substrate and regulator of cyclic nucleotide phosphodiesterases (PDEs). Rev. Physiol. Biochem. Pharmacol ... Cyclic GMP as substrate and regulator of cyclic nucleotide phosphodiesterases (PDEs). Rev. Physiol. Biochem. Pharmacol ... Concentration and regulation of cyclic nucleotides, cyclic-nucleotide-dependent protein kinases and one of their major ... Concentration and regulation of cyclic nucleotides, cyclic-nucleotide-dependent protein kinases and one of their major ...
... cyclic nucleotide phosphodiesterase; K-ATP, ATP-sensitive potassium channel; VDCC, voltage-dependent calcium channel; NSCC, non ... The role of L-type and N-type Voltage-Dependent Calcium Channels as determinants of neuropeptide secretion was first ... High-throughput FRET assays for fast time-dependent detection of cyclic AMP in pancreatic beta cells. "Cyclic Nucleotide ... Chapter 3, Cyclic Nucleotide Signaling, 2015. This review describes the details of a novel FRET-based assay for use in the ...
... immobilized on agarose by an aminoethylcarbamoyl spacer attached to the ribose 2-position of the ligand. Free Rp-cAMPS is not ... The gel can be used for affinity chromatography of various cyclic nucleotide-responsive proteins, especially those which ... ribose hydroxyl group such as some phosphodiesterases. This type of gel is offered with a longer spacer (Rp-2-AHC-cAMPS- ... Free Rp-cAMPS is not metabolized by mammalian phosphodiesterases and thus represents an extraordinary stable ligand. In ...
"Type II glucocorticoid receptors are expressed in oligodendrocytes and astrocytes, Journal of Neuroscience Research" on ... cyclic nucleotide phosphodiesterase (CNP), or myelin basic protein (MBP). Double immunofluorescence microscopy revealed that ... In the brain, two types of high‐affinity receptors bind glucocorticoids, the type I, mineralocorticoid receptor and the type II ... In the brain, two types of high‐affinity receptors bind glucocorticoids, the type I, mineralocorticoid receptor and the type II ...
cyclic GMP-inhibited phosphodiesterase B. cyclic nucleotide phosphodiesterase. phosphodiesterase 3B, cGMP-inhibited. NP_ ... phosphodiesterase 3Bprovided by HGNC. Primary source. HGNC:HGNC:8779 See related. Ensembl:ENSG00000152270 MIM:602047 Gene type ... PDEase_I; 35-cyclic nucleotide phosphodiesterase. pfam06532. Location:136 → 282. DUF1109; Protein of unknown function ( ... PDEase_I; 35-cyclic nucleotide phosphodiesterase. pfam06532. Location:136 → 282. DUF1109; Protein of unknown function ( ...
A 003) immobilized on agarose by an aminohexylcarbamoyl spacer attached to the ribose 2-position of the ligand. The gel can be ... The gel can be used for affinity chromatography of various cyclic nucleotide-responsive proteins, especially those which ... ribose hydroxyl group such as some phosphodiesterases. This type of gel is offered with a shorter spacer (Sp-2-AEC-cAMPS- ... cyclic monophosphorothioate, Sp- isomer; immobilized on agarose gel ( Sp-2-AHC-cAMPS-Agarose ). ...
Emesis induced by inhibitors of type IV cyclic nucleotide phosphodiesterase (PDE IV) in the ferret. Neuropharmacology 1999. 38: ... Cyclic nucleotide phosphodiesterases. J Allergy Clin Immunol 2001. 108:671-680. View this article via: PubMed CrossRef Google ... The molecular biology of cyclic nucleotide phosphodiesterases. Prog Nucleic Acid Res Mol Biol 2000. 63:1-38. ... Cyclic nucleotides cAMP and cGMP are degraded by at least 11 families of phosphodiesterases (PDEs 1-11) classified according to ...
... and clinical studies related to type 1 and type 2 diabetes. The journal welcomes submissions focusing on the epidemiology, ... and the catalytic actions of cyclic nucleotide phosphodiesterase (PDE). Energy stress conditions like diet restriction, hypoxia ... Studies have shown that RSV improves biochemical and clinical parameters in both type 1 and type 2 animal models of diabetic ... IDDM-type 1) and non-insulin-dependent diabetes mellitus (NIDDM-type 2). The former is characterized by selective autoimmune ...
... a bi-functional compound with both phosphodiesterase 4 (PDE4) antagonist and long-acting β2-adrenoceptor agonist (LABA) ... Type 4 cyclic nucleotide phosphodiesterase inhibitors * Orphan Drug Status Orphan designation is assigned by a regulatory body ... Mechanism of Action Beta 2 adrenergic receptor agonists; ...
Cyclic Nucleotide Phosphodiesterases, Type 6/metabolism. *Fibroblast Growth Factor 2/metabolism. *Humans ... Endothelin-2-mediated protection of mutant photoreceptors in inherited photoreceptor degeneration. Bramall AN, Szego MJ, ... Endothelin-2-mediated protection of mutant photoreceptors in inherited photoreceptor degeneration. Bramall AN, Szego MJ, ... Expression of the Endothelin-2 (Edn2) mRNA is greatly increased in the photoreceptors (PRs) of mouse models of inherited PR ...
1995) Cyclic nucleotide phosphodiesterase type IV participates in the regulation of IL-10 and in the subsequent inhibition of ... Negative regulation of cysteine-type endopeptidase activity involved in apoptotic process. 66. ... Positive regulation of T-helper 2 cell differentiation. 14. Positive regulation of transcription from RNA polymerase II ...
Here we review recent developments in the understanding of the innate immune pathways that drive type I IFN responses in ... Here we review recent developments in the understanding of the innate immune pathways that drive type I IFN responses in ... tuberculosis infection have drawn significant attention to the roles of type I IFNs in the host response to mycobacterial ... tuberculosis infection have drawn significant attention to the roles of type I IFNs in the host response to mycobacterial ...
Type 3 Cyclic Nucleotide Phosphodiesterases * Cilostazol * Type 2 Diabetes Mellitus * Arachidonate 5-Lipoxygenase ... Type 2 diabetes and cardiovascular disease: A metabolic overview of recent clinical trials. Birnbaum, Y., Ye, Y. & Bajaj, M., ... Phosphodiesterase III Inhibition Increases cAMP levels and augments the infarct size limiting effect of a dpp-4 inhibitor in ... The effect of pioglitazone treatment on 15-epi-lipoxin A 4 levels in patients with type 2 diabetes. Gutierrez, A. D., ...
Cyclic Nucleotide Phosphodiesterases, Type 1; Epithelium; Glucose Transporter Type 4; Hair Cells, Auditory; Humans; Insulin; ... Review type: Peer Review Submission year: 2013 Scientific Level: Scientific ID: 241855921 ... Type: Journal article Language: English Published in: Cell and Tissue Research, 2013, Vol 352, Issue 3, p. 469-478 Keywords: ... which also exhibits expression of a calcium-sensitive cAMP/cGMP phosphodiesterase 1C (PDE1C) and the vasopressin type 2 ...
Cyclic Nucleotide Phosphodiesterases, Type 2. 1. 2008. 1. 0.430. Why? Guanylate Cyclase. 1 ...
... cyclic nucleotide 3-phosphodiesterase H41908 182295 cytochrome P450 IIB6 H43131 182987 keratin, type II cytoskeletal8 H43783 ... cyclic nucleotide 3-phosphodiesterase AA020847 363721 CD40 AA024754 364936 monocyte chemotactic protein 1 (IFN gamma-inducible ... Both the coding strand of the gene, the strand having the nucleotide sequence identical to the sequence of nucleotides in the ... cyclic phosphodiesterase beta- subunit H79047 233721 IGF binding protein 2 H95366 234487 beta-arrestin 2 H53620 236055 ...
... cyclic phosphodiester to an RNA 2-phosphomonoester (PubMed:25239919). In vitro, can also ligate 5 and 3 half-tRNA molecules ... cyclic phosphate and 5-hydroxyl termini, respectively, to the product containing the 2-5 phosphodiester linkage. This ... cyclic-nucleotide 3-phosphodiesterase activity Source: EcoCyc ,p>Inferred from Direct Assay,/p> ,p>Used to indicate a direct ... These various submissions may originate from different sequencing projects, different types of experiments, or different ...
B) Intracellular cAMP levels in the wild-type cells and pdeA, pdeB, and pdeC mutant cells growing at 30°C and 37°C. Wild-type ... Cyclic nucleotides, cyclic nucleotide phosphodiesterase, and development in Myxococcus xanthus. Can. J. Microbiol. 24:1475-1484 ... Sequential changes in the cyclic nucleotide levels and cyclic phosphodiesterase activities during development of M. xanthus. ... and PdeC have characteristics of cyclic nucleotide phosphodiesterases. We could not find homologues of eukaryotic cyclic ...
  • Are Phosphodiesterase-5 Inhibitors a New Frontier for Prevention of Colorectal Cancer? (harvard.edu)
  • Sub-efficacious doses of phosphodiesterase 4 and 5 inhibitors improve memory in a mouse model of Alzheimer's disease. (bioportfolio.com)
  • Increasing their levels by phosphodiesterase inhibitors (PDE-Is) enhanced cognitive functions and rescued mem. (bioportfolio.com)
  • A CoMFA study of benzo- and benzothienothiadiazines derivatives as phosphodiesterase 7 inhibitors has been carried out in order to determine the factors required for the activity of these compounds and also for the selectivity versus other phosphodiesterase isoenzymes. (nih.gov)
  • Although some studies showed the efficacy of phosphodiesterase (PDE) inhibitors as neuronal plasticity enhancers, little is known about the effectiveness of these drugs to improve plasticity in cases of mental retardation. (jneurosci.org)
  • Treatment opportunities involving phosphodiesterase inhibitors (PDEIs) and purinergic modulators may plausibly exist. (iacfsme.org)
  • Rodent studies have consistently shown upregulation of the 3, 5-cyclic adenosine monophosphate (cAMP) system induced by different types of chronic but not acute antidepressant treatment including serotonin and norepinephrine uptake inhibitors, monoamine oxidase inhibitors, tricyclic antidepressants, lithium and electroconvulsions. (clinicaltrials.gov)
  • The purified PDE was active, inhibited by both Type IV specific inhibitors (RO 20-1724 and rolipram) and the general PDE inhibitor MIX, and had normal kinetic characteristics for a PDE of the Type IV subfamily. (uwo.ca)
  • In addition, induction of PAI was enhanced by isobutyl-methylxanthine, a phosphodiesterase inhibitor, but not, however, by other phosphodiesterase inhibitors, or by forskolin or N(G)-nitro-L-arginine, suggesting an effect of isobutyl-methylxanthine other than through cyclic nucleotides. (tudelft.nl)
  • Theophylline and 3-isobutyl-1-methylxanthine, two cyclic nucleotide phosphodiesterase inhibitors, when fed to wild-type Drosophila adults, cause the rapid decay of learning index after training in a shock-odor learning paradigm. (springer.com)
  • The CO-induced increase in I Ba was blocked when cells were pretreated with 1H-[1,2,4]- oxadiazolo[4,3-a]quinoxalin-1-one (10 μM) or inhibitors of NO synthase (NOS). (elsevier.com)
  • Effect of phosphodiesterase (1B, 2A, 9A and 10A) inhibitors on central nervous system cyclic nucleotide levels of rats and mice. (annals.org)
  • Such as inhibitors can be used, for example, as a means of increasing cyclic AMP in neurons and thus treating neurological problems, such as long term memory loss, if not preventing such maladies entirely. (freepatentsonline.com)
  • Phosphodiesterase inhibitors, pentoxifylline and rolipram, increase bone mass mainly by promoting bone formation in normal mice. (naver.com)
  • Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present. (freepatentsonline.com)
  • The assignments of varied PDEs in the hypnotic aftereffect of the 2-adrenoceptorCmediated anesthetic program had been examined using selective and mixed-type PDE inhibitors. (techuniq.com)
  • Open up in another window Amount 2 Aftereffect of PDE inhibitors over the duration of anesthesia induced with the mix of xylazine (10 mg/kg) and ketamine (80 mg/kg) in C57BL/6 mice. (techuniq.com)
  • The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases. (patentsencyclopedia.com)
  • Phosphodiesterases (PDEs) are a family of phosphohydrolyases that catalyze the hydrolysis of 3' cyclic phosphate bonds in adenosine and/or guanine 3',5' cyclic monophosphate (cAMP and/or cGMP). (genecards.org)
  • cAMP is synthesized from adenosine 5-triphosphate (ATP) by adenylyl cyclase and metabolized by cyclic nucleotide phosphodiesterases (PDEs). (clinicaltrials.gov)
  • Phosphodiesterases (PDEs) are the only route for degrading cAMP and are thus poised to regulate intracellular cAMP gradients. (ox.ac.uk)
  • Intracellular cAMP concentration is regulated by the activities of at least two families of enzymes: adenylyl and guanylyl cyclases, responsible for cAMP and cGMP synthesis and cyclic nucleotide phosphodiesterases (PDEs) that mediate cAMP and cGMP hydrolysis.Among the PDE superfamily, PDE2 is a dual substrate enzyme that hydrolyzes both cAMP and cGMP and has the unique property to be stimulated by cGMP. (worldcat.org)
  • The cAMP-degrading enzymes, phosphodiesterases (PDEs), localise to specific subcellular domains within which they control local cAMP levels and are key regulators of signal compartmentalisation. (ox.ac.uk)
  • Cyclic nucleotide phosphodiesterases (PDEs) are enzymes that regulate the amplitude and duration of cAMP and cGMP signaling by controlling cyclic nucleotide (cNT) degradation. (pnas.org)
  • Specific functions for different cyclic nucleotide phosphodiesterases (PDEs) have not yet been identified in most cell types. (pnas.org)
  • The findings further suggest that the approach of using selective, inhibitor-dependent phosphoproteome analysis can provide a generalized methodology for understanding the roles of different PDEs in the regulation of cyclic nucleotide signaling. (pnas.org)
  • Cyclic nucleotide phosphodiesterases (PDEs), by catalyzing the hydrolysis of cyclic nucleotides, are critical in the homeostasis of intracellular cyclic nucleotide signaling and hold great therapeutic potential as drug targets. (mdpi.com)
  • A large family of enzymes named cyclic nucleotide phosphodiesterases (PDEs) inactivate cAMP and cGMP through their hydrolysis ( 11 - 14 ). (diabetesjournals.org)
  • Preimplant Phosphodiesterase-5 Inhibitor Use Is Associated With Higher Rates of Severe Early Right Heart Failure After Left Ventricular Assist Device Implantation. (harvard.edu)
  • Analysis of short-term treatment with the phosphodiesterase type 5 inhibitor tadalafil on long bone development in young rats. (harvard.edu)
  • EHNA (erythro-9-(2-hydroxy-3-nonyl)adenine) is a potent adenosine deaminase inhibitor, which also acts as a phosphodiesterase inhibitor that selectively inhibits phosphodiesterase type 2 (PDE2). (wikipedia.org)
  • A selective phosphodiesterase 3 inhibitor rescues low PO2-induced ATP release from erythrocytes of humans with type 2 diabetes: implication for vascular control. (nih.gov)
  • Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity. (nih.gov)
  • The effects of a novel Ca(2+)-sensitizer (EMD 60263, 10 microM, group 1) were compared with a phosphodiesterase (PDE) III-inhibitor (enoximon, 20 microM, group 2) on 14 isolated, blood-perfused rabbit hearts during reperfusion after a global ischemia of 20 min. (curehunter.com)
  • Using a combination of electrophysiological and optical imaging techniques, we show here that vinpocetine, a PDE type I inhibitor, restores ocular dominance plasticity in the ferret model of fetal alcohol exposure. (jneurosci.org)
  • Here, we try to restore ocular dominance plasticity in alcohol-exposed ferrets using the PDE type 1 inhibitor vinpocetine. (jneurosci.org)
  • Among components of the cAMP pathway, PDE4 appears to be critical for antidepressant effects because an inhibitor of PDE4, 4-[3-(cyclopenotoxyl)-4-methoxyphenyl]-2-pyrrolidone (rolipram), showed antidepressant effects both in animals and humans, and various forms of antidepressant treatment induced increase in PDE4 in rodents. (clinicaltrials.gov)
  • Pharmacological modulation of the in vivo induction of plasminogen activator inhibitor type-1 (PAI-1) synthesis was studied in rats using the induction of PAI-1 by endotoxin as a model system. (tudelft.nl)
  • Bucladesine is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor. (mark-e-murphy.com)
  • Since the activity of the cyclic nucleotide is also regulated by phosphodiesterase 5, we have examined the effect of zaprinast, an inhibitor of the enzyme, on the sheep isolated internal anal sphincter. (bmj.com)
  • The PKA inhibitor KT-5720 (0.5 μM) and milrinone (3 μM), a phosphodiesterase (PDE) III inhibitor, blocked the effect of CO on I Ba . (elsevier.com)
  • High-throughput development and characterization of a genomewide collection of gene-based single nucleotide polymorphism markers by chip-based matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. (naver.com)
  • Challenges of adjusting Single-Nucleotide Polymorphism effect sizes for linkage disequilibrium. (cf.ac.uk)
  • The phenotype was the opposite of that of the receptor-type adenylyl cyclase ( cyaA or cyaB ) mutant. (asm.org)
  • By contrast, Gα i/o can both modulate phosphodiesterase activity and inhibit adenylyl cyclase activity, reduce both intracellular cAMP levels and protein kinase A activity, leading to decreased depolarizing currents carried by HCN and L-type calcium channels. (ahajournals.org)
  • Generally, these enzymes hydrolyze some nucleoside 3',5'-cyclic phosphate to some nucleoside 5'-phosphate thus controlling the cellular levels of the cyclic second messengers and the rates of their degradation. (wikipedia.org)
  • Biochemical characterization of the inhibition of the two major phosphodiesterase isoenzymes in Drosophila by theophylline predicts only a slight inhibition of these enzymes in vivo , in accordance with the unchanged level of cAMP in wild-type fly heads during drug feeding. (springer.com)
  • KLF15-deficient mice also manifested a decrease in the expression of genes for enzymes that mediate amino acid degradation, including those for alanine aminotransferase 1 (ALT1), 4-hydroxyphenylpyruvate dioxygenase (HPD), proline dehydrogenase (ProDH), and tryptophan 2,3-dioxygenase (TDO2) ( 10 ). (diabetesjournals.org)
  • A phosphate-binding histidine of binuclear metallophosphodiesterase enzymes is a determinant of 2',3'-cyclic nucleotide phosphodiesterase activity. (ebi.ac.uk)
  • The activity of the oligodendrocyte-specific enzymes, cerebroside sulfotransferase (CST) and 2'3'-cyclic nucleotide 3'-phosphohydrolase (CNP), was 27% and 17% respectively of the activity in noninfected controls. (springernature.com)
  • VSMC cAMP hydrolysis is catalyzed by members of the phosphodiesterase 3 (PDE3) and PDE4 families ( 12 ), whereas VSMC cGMP is inactivated by PDE1 or PDE5 enzymes ( 15 ). (diabetesjournals.org)
  • Our results suggest that decreases in intracellular cyclic nucleotide levels in pulmonary arteries from pulmonary hypertensive rats are associated with increased PDE activity. (aspetjournals.org)
  • Cyclic adenosine monophosphate phosphodiesterase type 4 protects against atrial arrhythmias. (nih.gov)
  • A combination of pharmacological and genetic approaches was used to determine the role of type 4 cAMP-specific cyclic nucleotide phosphodiesterase 4 (PDE4) in reversing α 2 -adrenoceptor-mediated anesthesia, a behavioral correlate of emesis in non-vomiting species. (jci.org)
  • Anchored PDE4 regulates chloride conductance in wild-type and ΔF508-CFTR human airway epithelia. (nih.gov)
  • Type 4 PDE (PDE4) is selective to cAMP in the brain. (clinicaltrials.gov)
  • Baillie GS, Sood A, McPhee I, Gall I, Perry SJ, Lefkowitz RJ, Houslay MD (2003) Beta-Arrestin-mediated PDE4 cAMP phosphodiesterase recruitment regulates beta-adrenoceptor switching from Gs to Gi. (springer.com)
  • A combined mix of pharmacological and hereditary approaches was used to look for the function of type 4 cAMP-specific cyclic nucleotide phosphodiesterase 4 (PDE4) in reversing 2-adrenoceptorCmediated anesthesia, a behavioral correlate of emesis in non-vomiting types. (techuniq.com)
  • We found that mice deficient in IL-17A, IL-17 receptor C (IL-17RC), and adaptor protein Act1 (of IL-17R) all had reduced demyelination accompanied by lessened microglial and polydendrocyte cellular reactivity compared with that in wild-type mice in response to cuprizone feeding, demonstrating the essential role of IL-17-induced Act1-mediated signaling in cuprizone-induced demyelination. (jneurosci.org)
  • Phosphodiesterase 4B in the cardiac L-type Ca²⁺ channel complex regulates Ca²⁺ current and protects against ventricular arrhythmias in mice. (nih.gov)
  • This includes a few exogenous, vertically transmitted and endogenous viruses of mice (type B) and some primate and sheep viruses (type D). MAMMARY TUMOR VIRUS, MOUSE is the type species. (bioportfolio.com)
  • Using immunoblotting and radioenzymatic assay we showed that total cardiac cAMP and cGMP PDE activity and specific PDE2 activity was strongly increased in PDE2 TG compared to wild type (WT) mice. (worldcat.org)
  • Sarcomere shortening, Ca2+ transients and the whole L-type Ca2+ current (ICa,L) were recorded in adult ventricular myocytes from WT and PDE2 TG mice and isoprenaline (ISO) was used to examine and compare the [beta]-adrenergic ([beta]-AR) response of these parameters. (worldcat.org)
  • Conscious freely moving RGS4-null mice showed increased bradycardic responses to parasympathetic agonists compared to wild-type animals. (ahajournals.org)
  • The effect of bucladesine as a cAMP analog has been studied on the pentylenetetrazol-induced seizure in the wild-type mice. (wikipedia.org)
  • Bucladesine (50-100nM/mouse) showed significant attenuation in the morphine withdrawal syndrome in the wild-type mice. (wikipedia.org)
  • PDE3B (Phosphodiesterase 3B) is a Protein Coding gene. (genecards.org)
  • Gene Ontology (GO) annotations related to this gene include 3',5'-cyclic-nucleotide phosphodiesterase activity and cGMP-inhibited cyclic-nucleotide phosphodiesterase activity . (genecards.org)
  • Gene expression profiles have been described for uncultured hematopoietic stem cells and cultured central nervous system neurospheres ( 2 - 8 ), but not for prospectively identified, uncultured neural stem cells. (sciencemag.org)
  • Systematic search for single nucleotide polymorphisms in the 5' flanking region of the human phosphodiesterase 3B gene: absence of evidence for major effects of identified polymorphisms on susceptibility to Japanese type 2 diabetes. (nih.gov)
  • A cAMP phosphodiesterase gene ( cpdA )-disrupted Escherichia coli or Salmonella enterica serovar Typhimurium strain showed about 2- or 1.3-fold higher intracellular cAMP than the wild-type strain, respectively ( 2 , 6 ). (asm.org)
  • Prominent interferon (IFN) inducible gene signatures in TB patients and animal models of Mycobacterium tuberculosis infection have drawn significant attention to the roles of type I IFNs in the host response to mycobacterial infections. (frontiersin.org)
  • Additionally, the discovery of IFN-related gene signatures in patients with active TB disease ( 3 - 9 ) has created significant momentum behind investigation of the innate immune pathways and pathophysiological consequences of type I IFN expression during M. tuberculosis infection. (frontiersin.org)
  • A cyclic nucleotide phosphodiesterase subfamily that is inhibited by the binding of CYCLIC GMP to an allosteric domain found on the enzyme and through phosphorylation by regulatory kinases such as PROTEIN KINASE A and PROTEIN KINASE B. The two members of this family are referred to as type 3A, and type 3B, and are each product of a distinct gene. (uams.edu)
  • Context Convergent data make 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNP) a candidate gene for schizophrenia. (cf.ac.uk)
  • The relationship observed between gene expression profiles of both types of receptors in healthy subjects was lost in the hyperthyroid group, whereas was partially retained in euthyroid patients. (acmbcb.org)
  • Colicelli J, Birchmeier C, Michaeli T, O'Neill K, Riggs M, Wigler M (1989) Isolation and characterization of a mammalian gene encoding a high-affinity cAMP phosphodiesterase. (springer.com)
  • Vitamin D-inducible calcium transport and gene expression in three Caco-2 cell lines. (biomedsearch.com)
  • Association between a variation in the phosphodiesterase 4D gene and bone mineral density. (naver.com)
  • An enzyme that catalyzes the hydrolysis of cyclic AMP to form adenosine 5'-phosphate. (termsciences.fr)
  • The gel can be used for affinity chromatography of various cyclic nucleotide-responsive proteins, especially those which tolerate modification of the 2'-ribose hydroxyl group such as some phosphodiesterases. (biolog.de)
  • A tBLASTn search of the Myxococcus xanthus genome database at The Institute for Genomic Research (TIGR) identified three genes ( pdeA , pdeB , and pdeC ) that encode proteins homologous to 3′,5′-cyclic nucleotide phosphodiesterase. (asm.org)
  • The R 2 homodimer is formed by an N-terminal dimerization/docking (DD) domain that also mediates sub-cellular localization via A kinase anchoring proteins (AKAPs). (nature.com)
  • 7500 members that confers ligand-dependent allosteric regulation to a diverse range of proteins 2 . (nature.com)
  • Two C-terminal cyclic nucleotide binding (CNB) domains cooperatively bind two molecules of cAMP, resulting in a conformational change of the R subunit that releases the active catalytic kinase subunit(s) from the inhibitory pseudo-substrate or substrate site of PKAR. (nature.com)
  • Here, we review recent developments in the understanding of the innate immune pathways that drive type I IFN responses in mycobacteria-infected host cells and the functional consequences for the host defense against M. tuberculosis , with a view that such insights might be exploited for the development of targeted host-directed immunotherapies and development of reliable biomarkers. (frontiersin.org)
  • The overall aim is to measure zinc signals and understand their function in the respective signal transduction pathways, and they were even able to identify molecular targets for zinc signals, such as cyclic nucleotide phosphodiesterases and protein tyrosine phosphatases. (uni-potsdam.de)
  • Identification of the signaling pathways that regulate cyclic nucleotide microdomains is essential to our understanding of cardiac physiology and pathophysiology. (ox.ac.uk)
  • Bjorgo E, Solheim SA, Abrahamsen H, Baillie GS, Brown KM, Berge T, Okkenhaug K, Houslay MD, Tasken K (2010) Cross talk between phosphatidylinositol 3-kinase and cyclic AMP (cAMP)-protein kinase a signaling pathways at the level of a protein kinase B/beta-arrestin/cAMP phosphodiesterase 4 complex. (springer.com)
  • None of the natural or synthetic molecules tested so far, including enExecutethelins, bombesins, and related analogs, produce either specific binding or activation of intracellular signaling pathways on expression of mammalian GPR37 receptors in tissue culture cells or Xenopus oocytes (2, 4, 5). (lw90.com)
  • Our results demonstrate that NO inhibits Cl-/OH- exchange activity in Caco-2 cells via cGMP-dependent protein kinases G (PKG) and C (PKC) signal-transduction pathways. (biomedsearch.com)
  • Recent studies have revealed that the inhibition of the PDE family member PDE1 plays a protective role in pathological cardiac remodeling and dysfunction by the modulation of distinct cyclic nucleotide signaling pathways. (mdpi.com)
  • Data indicate that genome-wide significant associations were found both at age 6 and 14 with single nucleotide polymorphisms (SNPs) on chromosome 11p15 in phosphodiesterase 3B, cGMP-inhibited protein PDE3B/cytochrome P-450 CYP2R1 genes. (nih.gov)
  • We quantified axonal and myelin density using immunohistochemistry for neurofilament, myelin basic protein and quantified mature OL with NogoA, cyclic nucleotide 3-phosphodiesterase (CNPase) and OL precursor cell (OPC) densities with platelet derived growth factor receptor (PDGFR)α, β and NG-2 in each region. (nih.gov)
  • Glial cell types were identified by morphology and immunoreactivity (IR) with antibodies directed against glial fibrillary acidic protein (GFAP), cyclic nucleotide phosphodiesterase (CNP), or myelin basic protein (MBP). (deepdyve.com)
  • Cyclic Nucleotide Phosphodiesterases, Type 5" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • Phosphodiesterase 5 (PDE5), which hydrolyzes cGMP in the inactive form, 5ʹGMP, is present throughout the body and brain and has emerged as a potential therapeutic target for diseases related to neuroinflammatory and neurodegenerative processes, since their inhibition leads to accumulation of cGMP. (intechopen.com)
  • Vardenafil has higher affinity to phosphodiesterase-5 (PDE5) than sildenafil and lower administered dosage for the treatment of erectile dysfunction. (aspetjournals.org)
  • Plasma membrane calcium pump (PMCA4)-neuronal nitric-oxide synthase complex regulates cardiac contractility through modulation of a compartmentalized cyclic nucleotide microdomain. (ox.ac.uk)
  • Using pharmacological and genetic approaches combined with real-time FRET imaging and high resolution microscopy, we demonstrate that in rat cardiac myocytes and other cell types mitochondrial PDE2A2 regulates local cAMP levels and PKA-dependent phosphorylation of Drp1. (ox.ac.uk)
  • Cyclic nucleotide signaling regulates several cardiac functions including contractility, remodeling, and fibrosis. (mdpi.com)
  • The upstream conserved regions (UCRs) mediate homo- and hetero-oligomerization of type 4 cyclic nucleotide phosphodiesterases (PDE4s). (nih.gov)
  • Here, we provide evidence that type 4 cyclic nucleotide phosphodiesterases (PDE4s) are critical regulators of the cAMP/PKA-dependent activation of CFTR in primary human bronchial epithelial cells. (elsevier.com)
  • Phosphodiesterase 5 Inhibition Limits Doxorubicin-induced Heart Failure by Attenuating Protein Kinase G Ia Oxidation. (harvard.edu)
  • p>This indicates the type of evidence that supports the existence of the protein. (uniprot.org)
  • PROTEIN SEQUENCE OF 2-23 , FUNCTION AS A LIGASE, DISRUPTION PHENOTYPE. (uniprot.org)
  • Our immunohistochemistry approach has shown that the insulin receptor, insulin receptor substrate 1 (IRS1), protein kinase B (PKB) and insulin-sensitive glucose transporter (GLUT4) are expressed in the sensory epithelium of the human saccule, which also exhibits expression of a calcium-sensitive cAMP/cGMP phosphodiesterase 1C (PDE1C) and the vasopressin type 2 receptor. (forskningsdatabasen.dk)
  • IRS1 and PDE1C are selectively expressed in sensory epithelial hair cells, whereas the other components are expressed in sensory epithelial supporting cells or in both cell types, as judged from co-expression or non-co-expression with glial fibrillary acidic protein, a marker for supporting cells. (forskningsdatabasen.dk)
  • A quantitative model for the kinetics of cAMP-dependent protein kinase (type II) activity. (springer.com)
  • Cyclic AMP-induced phosphorylation of 27.5 kDa protein(s) in larval brains of normal and memory-mutant Drosophila melanogaster . (springer.com)
  • A potent, cell-permeable, and reversible metabolically-stable cAMP antagonist that inhibits cAMP-dependent protein kinase and shows preference for PKA type I. (merckmillipore.com)
  • cAMP coordinates the regulation of these cellular responses by activating cAMP-dependent protein kinases (PKAs) ( 4 ), specific guanine nucleotide exchange factors (EPACs) ( 5 ), and cyclic nucleotide-gated ion channels ( 6 ). (pnas.org)
  • However, when intact platelets were incubated with NO and then lysed, enhanced activity of phosphodiesterase type 5 was detected in the cytosol. (rupress.org)
  • Thus, our data suggest that NO-induced desensitization of the cGMP response is caused by the phosphorylation and subsequent activity increase of phosphodiesterase type 5. (rupress.org)
  • This methodology is employed to gain clues on the design of new fused thiadiazines with improved activity and selectivity on phosphodiesterase 7. (nih.gov)
  • Using the information achieved from the three CoMFA models, new structures have been designed in silico and their inhibitory activity on phosphodiesterase 7 was predicted. (nih.gov)
  • This resulted in increased L-type calcium channel activity and ryanodine receptor phosphorylation and hence increased contractility. (ox.ac.uk)
  • Ahmad F, Shen W, Vandeput F, Szabo-Fresnais N, Krall J, Degerman E, Goetz F, Klussmann E, Movsesian M, Manganiello V (2015) Regulation of sarcoplasmic reticulum Ca2+ ATPase 2 (SERCA2) activity by phosphodiesterase 3A (PDE3A) in human myocardium: phosphorylation-dependent interaction of PDE3A1 with SERCA2. (springer.com)
  • Furthermore, in intact HL-60 cells, PDE1B2 activity can be regulated by changes in Ca +2 levels. (pnas.org)
  • Parasympathetic activity on nodal myocytes is mediated by acetylcholine-dependent stimulation of M 2 muscarinic receptors and activation of Gα i/o signaling. (ahajournals.org)
  • As a result, cAMP-regulated effectors such as hyperpolarization-activated cyclic nucleotide-gated cation (HCN) channels, delayed rectifier, and voltage-gated Ca 2+ channels are enlisted by sympathetic activity to increase pacemaker cell firing rate. (ahajournals.org)
  • 1,2 By contrast, vagal parasympathetic activity decreases HR via Gα i/o -coupled cholinergic M 2 muscarinic receptors (M 2 Rs). (ahajournals.org)
  • 2-5 Because dysregulation of parasympathetic activity occurs in heart failure, sick sinus syndrome, and selected cardiac arrhythmias, 6 it is of clinical interest to identify key molecular regulators of parasympathetic signaling. (ahajournals.org)
  • Modulation of Cl-/OH- exchange activity in Caco-2 cells by nitric oxide. (biomedsearch.com)
  • The present studies were undertaken to determine the direct effects of nitric oxide (NO) released from an exogenous donor, S-nitroso-N-acetyl pencillamine (SNAP) on Cl-/OH- exchange activity in human Caco-2 cells. (biomedsearch.com)
  • N-Phenyl-N-pyrimidin-2-yl-ureas with herbicidal and plant-growth regulating activity. (freepatentsonline.com)
  • littermates, display an " activated" phenotype in vitro and in vivo and have an elevated level of cAMP phosphodiesterase (PDE) activity. (diabetesjournals.org)
  • Phosphodiesterase (PDE) activity was determined in pulmonary arteries removed from control and chronic hypoxia-induced pulmonary hypertensive rats. (aspetjournals.org)
  • It is based on adenosine triphosphate (ATP) and its derivatives, ADP and adenosine as well as the purine nucleotide UTP. (iacfsme.org)
  • 1995) Cyclic nucleotide phosphodiesterase type IV participates in the regulation of IL-10 and in the subsequent inhibition of TNF alpha and IL-6 release by endotoxin-stimulated macrophages. (avivasysbio.com)
  • Most of the effects of the signaling molecule nitric oxide (NO) are mediated by cGMP, which is synthesized by soluble guanylyl cyclase and degraded by phosphodiesterases. (rupress.org)
  • The Haase team could show that they are fine tuning signaling by Toll-like receptor 4, promoting the secretion of pro-inflammatory cytokines, whereas they downregulate the production of type-1 interferons and nitric monoxide. (uni-potsdam.de)
  • Neurogenic relaxation of the internal anal sphincter is mediated by elevation of cyclic GMP, following activation of soluble guanylyl cyclase by nitric oxide. (bmj.com)
  • The nitric oxide/cyclic guanosine monophosphate (NO/cGMP) signaling appears to play a key role in inhibiting neuroinflammation and preventing the activation of a proapoptotic pathway, thereby promoting neural cell survival. (intechopen.com)
  • The inhibition of T-cell proliferation in the presence of MEL 174 was followed by a decrease in IL-2 production, which was partly abrogated by exogenous IL-2, a decrease in nitric oxide (NO) production and increased apoptosis. (blogspot.com)
  • Endothelium-derived relaxing factors, such as nitric oxide or prostacyclin, relax blood vessels and inhibit the proliferation and migration of VSMCs by increasing the synthesis of the cyclic nucleotides cAMP or cGMP ( 7 - 10 ). (diabetesjournals.org)
  • This has profound consequences for the regulation of local cyclic nucleotide and hence cardiac β-adrenergic signaling. (ox.ac.uk)
  • A Type IV PDE isozyme was identified in L6 myoblasts using consensus sequence PCR primers, and its regulation by cAMP studied. (uwo.ca)
  • Cyclic AMP (cAMP) and cyclic GMP (cGMP) are critical second messengers for the regulation of cardiac function. (worldcat.org)
  • Novel Mechanism for Cyclic Dinucleotide Degradation Revealed by Structural Studies of Vibrio Phosphodiesterase V-cGAP3. (harvard.edu)
  • Furthermore, this increase in cGMP degradation is paralleled by the phosphorylation of phosphodiesterase type 5 at Ser-92. (rupress.org)
  • The degradation of cAMP is achieved by 3′,5′-cyclic nucleotide phosphodiesterases, which catalyze cleavage of 3′,5′-cAMP to 5′-cAMP. (asm.org)
  • While IFN-γ is the sole type II IFN, type I IFNs in humans comprise several IFN-α subtypes, IFN-β, IFN-ω, IFN-ε, IFN-τ, and IFN-κ ( 10 ). (frontiersin.org)
  • Is inhibition of PDE3B a possible target for treatment of obesity or type 2 diabetes mellitus? (nih.gov)
  • Another project has shown that Interleukin-2-dependent signal transduction and proliferation of T-cells is based on inhibition of MAPK-phosphatases and PTEN by Zn. (uni-potsdam.de)
  • It is well established that inhibition of dipeptidyl peptidase (DPP)-IV reduces glucose levels and preserves pancreatic beta cell function in patients with type 2 diabetes. (bioportfolio.com)
  • Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. (genecards.org)
  • Cyclic nucleotides cAMP and cGMP cooperate to ensure memory acquisition and consolidation. (bioportfolio.com)
  • Reported here are collaborative studies of the Holz and Thurmond labs working with Dr. Frank Schwede of the BIOLOG Life Sciences Institute to establish that in human islets from T2DM donors, the Epac selective cAMP analog 8-pCPT-2'- O -Me-cAMP-AM enables F-acting cytoskeletal remodeling so that insulin secretion is restored. (upstate.edu)
  • Intracellular cyclic AMP (cAMP) levels of pdeA or pdeB mutant cells under these stressful conditions were about 1.3-fold to 2.0-fold higher than those of wild-type cells. (asm.org)
  • We also report that an M. xanthus CbpB containing two cyclic AMP (cAMP)-binding domains is involved in osmotic and temperature tolerance ( 11 ). (asm.org)
  • A potential role for cAMP in regulating the differentiation of myoblasts has lead to the examination of the components of the cAMP signalling system, in this case a cyclic nucleotide phosphodiesterase (PDE). (uwo.ca)
  • Phosphodiesterases and compartmentalized cAMP signalling in the heart. (ox.ac.uk)
  • cAMP-phosphodiesterase in the synaptic regions of Drosophila brains. (springer.com)
  • The resulting holoenzyme isoforms differ in cell type-specificity, developmental expression, sub-cellular localization, and affinity to cAMP, thereby accounting for the pleiotropic functions of cAMP signalling. (nature.com)
  • Human, rat and mouse cAMP phosphodiesterase isoforms (denoted PDE4D7s), as well as the DNA (RNA) encoding such polypeptides, are disclosed. (freepatentsonline.com)
  • Since its original discovery nearly 60 y ago ( 1 , 2 ), cAMP has been shown to regulate many different biological processes in multiple cell types ( 3 ). (pnas.org)
  • Could chronic Vardenafil administration influence the cardiovascular risk in men with type 2 diabetes mellitus? (bioportfolio.com)
  • In type 2 diabetes mellitus (T2DM), the beneficial effect of. (bioportfolio.com)
  • Type II glucocorticoid receptors are expressed in oligodendrocytes and astrocytes Vielkind, U. (deepdyve.com)
  • This immunocytochemical study was undertaken to determine which of the different classes of glial cells express type II GR. Primary cultures of mixed glial cells from rat cerebrum and cerebellum, purified oligodendrocytes and astrocytes. (deepdyve.com)
  • Double immunofluorescence microscopy revealed that all GFAP‐IR cells (type 1 and type 2 astrocytes), all CNP‐ or MBP‐IR cells (oligodendrocytes), as well as immature and intermediate cell types expressed GR, although at different levels. (deepdyve.com)
  • Immunohistochemical labeling has Displayn that, whereas most of the mouse GPR37-positive cells are 2′,3′-cyclic nucleotide 3′-phosphodiesterase-positive oligodendrocytes of fiber tracts, they also include distinct populations of neurons such as the SN Executepaminergic neurons, hippocampal neurons in the CA3 Location, and cerebellar Purkinje cells (6). (lw90.com)
  • A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. (harvard.edu)
  • Further, these changes may reflect alterations at the level of specific types of PDE isoforms. (aspetjournals.org)
  • 2. What are the primary uses of Ca++ channel antagonists? (brainscape.com)
  • A partial characterization of the cyclic nucleotide phosphodiesterases of Drosophila melanogaster. (springer.com)
  • The systematic for this enzyme is 3',5'-cyclic-nucleotide 5'-nucleotidohydrolase. (wikipedia.org)
  • The enzyme is widely distributed in animal tissue and controls the level of intracellular cyclic AMP. (termsciences.fr)
  • The existence of eukaryotic CNB domains not associated with binding of cyclic nucleotides suggests that orphan CNB domains in other eukaryotes may bind undiscovered signalling molecules. (nature.com)
  • Clinical effects of phosphodiesterase 3A mutations in inherited hypertension with brachydactyly. (nih.gov)
  • clinical nutrition as a specialty goes here HN - 2008 BX - Nutrition FX - Diet FX - Food DH - Child Nutrition DI - 052504 MN - SP6.021.062 MS - Nutrition of children aged 2-10 years. (bvsalud.org)
  • In the brain, two types of high‐affinity receptors bind glucocorticoids, the type I, mineralocorticoid receptor and the type II, glucocorticoid receptor (GR). Both receptor types are expressed by many types of neurons. (deepdyve.com)
  • All known type I IFNs signal through a common receptor, IFNAR, which consists of the low-affinity IFNAR1 and the high-affinity IFNAR2 ( 11 , 12 ). (frontiersin.org)
  • These p75 + α 4 + cells represent only 1 to 2% of cells in the E14.5 (embryonic day 14.5) rat gut ( 14 ). (sciencemag.org)
  • These colonies typically contained 1 × 10 5 to 2 × 10 5 cells after 14 days of culture. (sciencemag.org)
  • The cbpB mutant was more sensitive to osmotic stress than wild-type cells were, and when cultured under high- or low-temperature conditions, the cbpB mutant exhibited a marked reduction in growth compared to wild-type cells. (asm.org)
  • Furthermore, IRS1 appears to be localized in association with sensory nerves, whereas GLUT4 is expressed in the peri-nuclear area of stromal cells, as is the case for aquaporin 2. (forskningsdatabasen.dk)
  • Type 1 diabetes (T1D) is caused by the immune system inappropriately attacking the cells in the pancreas that produce insulin, the hormone that controls blood sugar levels. (psychcentral.com)
  • 2',3'-Cyclic nucleotide 3'-phosphodiesterase is used as a marker of myelin-forming cells and is detectable in cells of oligodendrocyte lineage throughout life. (cf.ac.uk)
  • In summary, we have demonstrated that neurospheres isolated from skin and adipose tissues are able to differentiate in glial/neuron-like cells, without any chromosomal imbalance in two scaffold types, useful for tissue engineering application: hyaluronan based membrane and fibrin-glue meshes. (mdpi.com)
  • Indeed, stem cells seem to give the best chance for human tissue engineering, and particularly, mesenchymal stem cells (MSCs) represent a great tool in regenerative medicine because of their ability to differentiate into a variety of specialized cells in addition to their immuno-privileged characteristics [ 1 , 2 ]. (mdpi.com)
  • Monocytes are peripheral immune cells that have the potential to differentiate into a variety of cell types depending on the combination of cytokines and stimuli to which they are exposed. (pnas.org)
  • The differentiated cell types range from professional antigen-presenting dendritic cells to osteoclasts to various macrophage populations found throughout the body ( 1 - 3 ). (pnas.org)
  • The aim of this study was to determine the effect of CO on the human intestinal L-type Ca 2+ channel expressed in HEK cells and in native cells using the patch-clamp technique. (elsevier.com)
  • Differentiation therapy has been shown effective in treatment of several types of cancer cells and may prove to be effective in treatment of glioblastoma multiforme, the most common and most aggressive primary brain tumor. (beds.ac.uk)
  • 7) SO/OH- exchange in Caco-2 cells was unaffected by SNAP. (biomedsearch.com)
  • Instead, nonreflective and Contributed by Ira Herskowitz ArticleFigures SIInfo overexpression of ASH1 inhibits mating type switching in mothers (3, 4). (lw90.com)
  • However, RSV is present at very low concentration [ 2 ], suggesting that the tag on RSV, "the red wine molecule," was overhyped. (hindawi.com)