Cyclic Nucleotide Phosphodiesterases, Type 1
A CALCIUM and CALMODULIN-dependent cyclic nucleotide phosphodiesterase subfamily. The three members of this family are referred to as type 1A, type 1B, and type 1C and are each product of a distinct gene. In addition, multiple enzyme variants of each subtype can be produced due to multiple alternative mRNA splicing. Although the type 1 enzymes are classified as 3',5'-cyclic-AMP phosphodiesterases (EC 220.127.116.11), 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.
Cyclic Nucleotide Phosphodiesterases, Type 4
A cyclic nucleotide phosphodiesterase subfamily that is found predominantly in inflammatory cells and may play a role in the regulation of CELL-MEDIATED IMMUNITY. The enzyme family includes over twenty different variants that occur due to multiple ALTERNATIVE SPLICING of the mRNA of at least four different genes.
Cyclic Nucleotide Phosphodiesterases, Type 3
A cyclic nucleotide phosphodiesterase subfamily that is inhibited by the binding of CYCLIC GMP to an allosteric domain found on the enzyme and through phosphorylation by regulatory kinases such as PROTEIN KINASE A and PROTEIN KINASE B. The two members of this family are referred to as type 3A, and type 3B, and are each product of a distinct gene. In addition multiple enzyme variants of each subtype can be produced due to multiple alternative mRNA splicing.
Cyclic Nucleotide Phosphodiesterases, Type 2
A cyclic nucleotide phosphodiesterase subfamily that is activated by the binding of CYCLIC GMP to an allosteric domain found on the enzyme. Multiple enzyme variants of this subtype can be produced due to multiple alternative mRNA splicing. The subfamily is expressed in a broad variety of tissues and may play a role in mediating cross-talk between CYCLIC GMP and CYCLIC CMP pathways. Although the type 2 enzymes are classified as 3',5'-cyclic-AMP phosphodiesterases (EC 18.104.22.168), members of this class have additional specificity for CYCLIC GMP.
Phosphoric Diester Hydrolases
Cyclic Nucleotide Phosphodiesterases, Type 5
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
Cyclic Nucleotide Phosphodiesterases, Type 7
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
A heat-stable, low-molecular-weight activator protein found mainly in the brain and heart. The binding of calcium ions to this protein allows this protein to bind to cyclic nucleotide phosphodiesterases and to adenyl cyclase with subsequent activation. Thereby this protein modulates cyclic AMP and cyclic GMP levels.
Amino Acid Sequence
Cyclic Nucleotide Phosphodiesterases, Type 6
A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. It is found predominantly in the outer segment PHOTORECEPTOR CELLS of the RETINA. It is comprised of two catalytic subunits, referred to as alpha and beta, that form a dimer. In addition two regulatory subunits, referred to as gamma and delta, modulate the activity and localization of the enzyme.
Dibutyryl 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.
Cyclic Nucleotide-Gated Cation Channels
Cyclic AMP-Dependent Protein Kinases
Cyclic GMP-Dependent Protein Kinases
Second Messenger Systems
Systems in which an intracellular signal is generated in response to an intercellular primary messenger such as a hormone or neurotransmitter. They are intermediate signals in cellular processes such as metabolism, secretion, contraction, phototransduction, and cell growth. Examples of second messenger systems are the adenyl cyclase-cyclic AMP system, the phosphatidylinositol diphosphate-inositol triphosphate system, and the cyclic GMP system.
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.
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.
Polymorphism, Single Nucleotide
8-Bromo Cyclic Adenosine Monophosphate
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.
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.
Cloning and characterization of PDE7B, a cAMP-specific phosphodiesterase. (1/27)A member of the phosphodiesterase (PDE)7 family with high affinity and specificity for cAMP has been identified. Based on sequence homologies, we designate this PDE as PDE7B. The full-length cDNA of PDE7B is 2399 bp, and its ORF sequence predicts a protein of 446 amino acids with a molecular mass of 50.1 kDa. Comparison of the predicted protein sequences of PDE7A and PDE7B reveals an identity of 70% in the catalytic domain. Northern blotting indicates that the mRNA of PDE7B is 5.6 kb. It is most highly expressed in pancreas followed by brain, heart, thyroid, skeletal muscle, eye, ovary, submaxillary gland, epididymus, and liver. Recombinant PDE7B protein expressed in a Baculovirus expression system is specific for cAMP with a K(m) of 0.03 microM. Within a series of common PDE inhibitors, it is most potently inhibited by 3-isobutyl-1-methylxanthine with an IC(50) of 2.1 microM. It is also inhibited by papaverine, dipyridamole, and SCH51866 at higher doses. PDE7A and PDE7B exhibit the same general pattern of inhibitor specificity among the several drugs tested. However, differences in IC(50) for some of the drugs suggest that isozyme selective inhibitors can be developed. (+info)
Novel alternative splice variants of rat phosphodiesterase 7B showing unique tissue-specific expression and phosphorylation. (2/27)cDNA species coding for novel variants of cyclic-AMP-specific phosphodiesterases (PDEs), namely the PDE7B family, were isolated from rats and characterized. Rat PDE7B1 (RNPDE7B1) was composed of 446 amino acid residues. Rat PDE7B2 (RNPDE7B2) and PDE7B3 (RNPDE7B3), which possessed unique N-terminal sequences, consisted of 359 and 459 residues respectively. Northern hybridization analysis showed that rat PDE7B transcripts were particularly abundant in the striatum and testis. PCR analyses revealed that rat PDE7B2 transcripts were restricted to the testis and that low levels of PDE7B3 transcripts were expressed in the heart, lung and skeletal muscle. In situ hybridization analysis demonstrated that rat PDE7B transcripts were expressed in striatal neurons and spermatocytes. In spermatocytes, rat PDE7B transcripts were expressed in a stage-specific manner during spermatogenesis. The K(m) values of recombinant rat PDE7B1, PDE7B2 and PDE7B3 for cAMP were 0.05, 0.07 and 0.05 microM respectively. Each rat PDE7B variant was the most sensitive to 3-isobutyl-1-methylxanthine (IC(50) 1.5-2.1 microM). Two phosphorylation sites for cAMP-dependent protein kinase (PKA) were found in rat PDE7B1 and PDE7B3, whereas rat PDE7B2 possessed one site. PKA-dependent phosphorylation was observed in C-terminal phosphorylation sites of three rat PDE7B variants, in addition to unique N-terminal regions of rat PDE7B1 and PDE7B3. Unique tissue distribution and PKA-dependent phosphorylation of PDE7B variants suggested that each variant has a specific role for cellular functions via cAMP signalling in various tissues. (+info)
Inhibition of PDE3B augments PDE4 inhibitor-induced apoptosis in a subset of patients with chronic lymphocytic leukemia. (3/27)PURPOSE: cAMP phosphodiesterase (PDE) 4 is a family of enzymes the inhibition of which induces chronic lymphocytic leukemia (CLL) apoptosis. However, leukemic cells from a subset of CLL patients are relatively resistant to treatment with the PDE4 inhibitor rolipram, particularly when this drug is used in the absence of an adenylate cyclase stimulus such as forskolin. Elevated cAMP levels induce compensatory up-regulation of several cyclic nucleotide PDE families in other model systems. We here examine the hypothesis that CLL cells that survive treatment with rolipram do so as a result of residual PDE activity that is not inhibited by this drug. EXPERIMENTAL DESIGN: We examined by Western analysis the effect of rolipram treatment on CLL expression of PDE3B, PDE4A, PDE4B, PDE4D, and PDE7A. We also examined the ability of rolipram (PDE4 inhibitor) or cilostamide (PDE3 inhibitor), alone or together, to induce apoptosis or elevate cyclic AMP in leukemic cells from patients with CLL. RESULTS: Rolipram increased levels of PDE4B and, to a variable extent, PDE4D. When combined with forskolin, rolipram also increased levels of a second family of PDEs, PDE3B. Addition of the specific PDE3 inhibitor, cilostamide, modestly augmented rolipram-induced apoptosis in five of seven "rolipram-resistant" CLL samples. CONCLUSIONS: Although this work confirms that PDE4 appears to be the most important PDE target for induction of apoptosis in CLL, combination therapy with PDE3 and PDE4 inhibitors or use of dual-selective drugs may be of benefit in a subset of relatively PDE4-inhibitor resistant CLL patients. (+info)
Potential role of phosphodiesterase 7 in human T cell function: comparative effects of two phosphodiesterase inhibitors. (4/27)Even though the existence of phosphodiesterase (PDE) 7 in T cells has been proved, the lack of a selective PDE7 inhibitor has confounded an accurate assessment of PDE7 function in such cells. In order to elucidate the role of PDE7 in human T cell function, the effects of two PDE inhibitors on PDE7A activity, cytokine synthesis, proliferation and CD25 expression of human peripheral blood mononuclear cells (PBMC) were determined. Recombinant human PDE7A was obtained and subjected to cyclic AMP-hydrolysis assay. PBMC of Dermatophagoides farinae mite extract (Df)-sensitive donors were stimulated with the relevant antigen or an anti-CD3 monoclonal antibody (MoAb). PBMC produced IL-5 and proliferated in response to stimulation with Df, while stimulation with anti-CD3 MoAb induced CD25 expression and messenger RNA (mRNA) synthesis of IL-2, IL-4 and IL-5 in peripheral T cells. A PDE inhibitor, T-2585, which suppressed PDE4 isoenzyme with high potency (IC50 = 0.00013 microM) and PDE7A with low potency (IC50 = 1.7 microM) inhibited cytokine synthesis, proliferation and CD25 expression in the dose range at which the drug suppressed PDE7A activity. A potent selective inhibitor of PDE4 (IC50 = 0.00031 microM), RP 73401, which did not effectively suppress PDE7A (IC50 > 10 microM), inhibited the Df- and anti-CD3 MoAb-stimulated responses only weakly, even at 10 microM. PDE7 may play a critical role in the regulation of human T cell function, and thereby selective PDE7 inhibitors have the potential to be used to treat immunological and inflammatory disorders. (+info)
Ubiquitous expression of phosphodiesterase 7A in human proinflammatory and immune cells. (5/27)We have determined the expression of phosphodiesterase (PDE) 7A1 and PDE7A2 in human cells that have been implicated in the pathogenesis of chronic obstructive pulmonary disease and asthma. Messenger RNA transcripts were detected by RT-PCR in T lymphocytes, monocytes, neutrophils, airway and vascular smooth muscle cells, lung fibroblasts, epithelial cells, and cardiac myocytes. Human epithelial, T cell, eosinophil, and lung fibroblast cell lines were also positive for PDE7A1 and PDE7A2 mRNA transcripts. By Western immunoblot analyses the amount of PDE7A1 was greatest in T cell lines, peripheral blood T lymphocytes, epithelial cell lines, airway and vascular smooth muscle cells, lung fibroblasts, and eosinophils but was not detected in neutrophils. In contrast, PDE7A2 protein, which was identified in human cardiac myocytes, was not found in any of the other cell types investigated. Immunoconfocal analyses showed that PDE7A was expressed in neutrophils and alveolar macrophages. As the expression of PDE7A mirrors the distribution of PDE4 we speculate that this enzyme could be a target for novel anti-inflammatory drugs. (+info)
Functional characterization of the human phosphodiesterase 7A1 promoter. (6/27)In this paper, the human phosphodiesterase 7A1 (h PDE7A1 ) promoter region was identified and functionally characterized. Transient transfection experiments indicated that a 2.9 kb fragment of the h PDE7A1 5'-flanking region, to position -2907, has strong promoter activity in Jurkat T-cells. Deletion analysis showed that the proximal region, up to position -988, contains major cis -regulatory elements of the h PDE7A1 promoter. This minimal promoter region contains a regulatory CpG island which is essential for promoter activity. The CpG island contains three potential cAMP-response-element-binding protein (CREB)-binding sites that, as judged by in vivo dimethyl sulphate (DMS) footprinting, are occupied in Jurkat T-cells. Moreover, over-expression of CREB results in increased promoter activity, but, on the other hand, promoter activity decreases when a dominant-negative form of CREB (KCREB) is over-expressed. In vivo DMS footprinting strongly indicates that other transcription factors, such Ets-2, nuclear factor of activated T-cells 1 (NFAT-1) and nuclear factor kappaB (NF-kappaB), might also contribute to the regulation of h PDE7A1 promoter. Finally, h PDE7A1 promoter was found to be induced by treatment with PMA, but not by treatment with dibutyryl cAMP or forskolin. These results provide insights into the factors and mechanisms that regulate expression of the h PDE7A gene. (+info)
Phosphodiesterase 7A-deficient mice have functional T cells. (7/27)Phosphodiesterases (PDEs) are enzymes which hydrolyze the cyclic nucleotide second messengers, cAMP and cGMP. In leukocytes, PDEs are responsible for depletion of cAMP which broadly suppresses cell functions and cellular responses to many activation stimuli. PDE7A has been proposed to be essential for T lymphocyte activation based on its induction during cell activation and the suppression of proliferation and IL-2 production observed following inhibition of PDE7A expression using a PDE7A antisense oligonucleotide. These observations have led to the suggestion that selective PDE7 inhibitors could be useful in the treatment of T cell-mediated autoimmune diseases. In the present report, we have used targeted gene disruption to examine the role PDE7A plays in T cell activation. In our studies, PDE7A knockout mice (PDE7A(-/-)) showed no deficiencies in T cell proliferation or Th1- and Th2-cytokine production driven by CD3 and CD28 costimulation. Unexpectedly, the Ab response to the T cell-dependent Ag, keyhole limpet hemocyanin, in the PDE7A(-/-) mice was found to be significantly elevated. The results from our studies strongly support the notion that PDE7A is not essential for T cell activation. (+info)
Genome annotation of a 1.5 Mb region of human chromosome 6q23 encompassing a quantitative trait locus for fetal hemoglobin expression in adults. (8/27)BACKGROUND: Heterocellular hereditary persistence of fetal hemoglobin (HPFH) is a common multifactorial trait characterized by a modest increase of fetal hemoglobin levels in adults. We previously localized a Quantitative Trait Locus for HPFH in an extensive Asian-Indian kindred to chromosome 6q23. As part of the strategy of positional cloning and a means towards identification of the specific genetic alteration in this family, a thorough annotation of the candidate interval based on a strategy of in silico / wet biology approach with comparative genomics was conducted. RESULTS: The ~1.5 Mb candidate region was shown to contain five protein-coding genes. We discovered a very large uncharacterized gene containing WD40 and SH3 domains (AHI1), and extended the annotation of four previously characterized genes (MYB, ALDH8A1, HBS1L and PDE7B). We also identified several genes that do not appear to be protein coding, and generated 17 kb of novel transcript sequence data from re-sequencing 97 EST clones. CONCLUSION: Detailed and thorough annotation of this 1.5 Mb interval in 6q confirms a high level of aberrant transcripts in testicular tissue. The candidate interval was shown to exhibit an extraordinary level of alternate splicing - 19 transcripts were identified for the 5 protein coding genes, but it appears that a significant portion (14/19) of these alternate transcripts did not have an open reading frame, hence their functional role is questionable. These transcripts may result from aberrant rather than regulated splicing. (+info)
Cosmic dust shows we were wrong about ancient atmosphere
A new study looking at cosmic dust that fell on Earth billions of years ago shows that the planets ancient atmosphere was a lot different than we thought.
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and Paddy with his words at will.: May...
But as I consider our Gospel reading today, where our Lord tells us he is the gate of the sheepfold, meaning that he is the right way for all to enter into the kingdom of God, I can not help thinking of how we are all called to be as Christ-like as possible; meaning that we must follow the example of Christ in helping others find the path to their salvation. What great benefit it would be to the salvation of souls if we encouraged others to stay on the right path, calling them back when they go wrong, tempted off course by what looks like an easier path, when the true path begins to look tough. And what benefit to us if others would help us also in a similar fashion, calling out to us. whenever we meet Buen Camino, meaning not that rocky road in Spain, but the Way that Christ laid before us. In such a way they would be as angels to us - even as we could be as angels to them. My prayer as I end is that all here will do their best to be as angels to all they meet, doing their best to guide them ...
"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 ... 7 (7): 733-8. doi:10.1016/0898-6568(95)00042-N. PMID 8519602. Méry PF, Pavoine C, Pecker F, Fischmeister R (July 1995). " ...
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 ...
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 ... 34 (7): 1874-82. doi:10.1097/01.CCM.0000221921.71300.BF. PMID 16715036. S2CID 71135736. Okunieff P, Xu J, Hu D, Liu W, Zhang L ...
Cyclic nucleotide phosphodiesterase
"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 ...
CGMP-specific phosphodiesterase type 5
"Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Advances in Cyclic ... Fertel R, Weiss B (July 1976). "Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung" ( ... cGMP-specific phosphodiesterase type 5 is an enzyme (EC 22.214.171.124) from the phosphodiesterase class. It is found in various ... Weiss B, Hait WN (1977). "Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annual ...
Benjamin Weiss (scientist)
He is best known for his work with cyclic nucleotide phosphodiesterases. He was the first to propose, based on his experimental ... He showed that a single cell type may contain more than one form of phosphodiesterase [6,7] and that different forms of ... one on the potential therapeutic application of cyclic nucleotides: (Weiss, Benjamin, ed., Cyclic Nucleotides in Disease), ... Cyclic Nucleotide Phosphodiesterases: Weiss and co-workers developed rapid phosphodiesterease assays [3, 4], separated ...
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 ...
Discovery and development of phosphodiesterase 5 inhibitors
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 ...
White matter Schwann cells 2',3'-Cyclic-nucleotide 3'-phosphodiesterase (CNPase) List of human cell types derived from the germ ... 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 ...
"Myomegalin is a novel protein of the golgi/centrosome that interacts with a cyclic nucleotide phosphodiesterase". The Journal ... These proteins degrade the second messenger cAMP, which is a key signal transduction molecule in multiple cell types, including ... "Myomegalin is a novel protein of the golgi/centrosome that interacts with a cyclic nucleotide phosphodiesterase". The Journal ... cAMP-specific 3',5'-cyclic phosphodiesterase 4D is an enzyme that in humans is encoded by the PDE4D gene. The PDE4D gene is ...
"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 ...
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 ...
2',3'-Cyclic-nucleotide 3'-phosphodiesterase (CNPase). *List of human cell types derived from the germ layers ... Oligodendrocytes are a type of glial cell. They arise during development from oligodendrocyte precursor cells (OPCs), which ... Oligodendrocytes (from Greek 'cells with a few branches'), or oligodendroglia, are a type of neuroglia whose main functions are ... Precursors and both mature types are typically identified by their expression of the transcription factor OLIG2. ...
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. ...
In mammals, GAF domains are found in five members of the cyclic nucleotide phosphodiesterase superfamily: PDE2, PDE5, and PDE6 ... The GAF domain is a type of protein domain that is found in a wide range of proteins from all species. The GAF domain is named ... a ubiquitous signaling motif and a new class of cyclic GMP receptor". The EMBO Journal. 19 (20): 5288-99. doi:10.1093/emboj/ ... "The two GAF domains in phosphodiesterase 2A have distinct roles in dimerization and in cGMP binding". Proceedings of the ...
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 ...
"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 ...
This export contributes to the degradation of phosphodiesterases and possibly an elimination pathway for cyclic nucleotides. ... "cDNA cloning of a short type of multidrug resistance protein homologue, SMRP, from a human lung cancer cell line". Biochemical ... This protein functions in the cellular export of its substrate, cyclic nucleotides. ... a transporter for cyclic nucleotides, in human placenta and cultured human trophoblasts: effects of gestational age and ...
1998). "Identification and characterization of a novel cyclic nucleotide phosphodiesterase gene (PDE9A) that maps to 21q22.3: ... "Identification and characterization of a new human type 9 cGMP-specific phosphodiesterase splice variant (PDE9A5). Differential ... High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A is an enzyme that in humans is encoded by the PDE9A gene. The ... "Entrez Gene: PDE9A phosphodiesterase 9A". Verhoest PR, Fonseca KR, Hou X, et al. (2012). "Design and discovery of 6-[(3S,4S)-4- ...
"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 ...
Lugnier C (March 2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific ... PDE1 (phosphodiesterase type 1) is a phosphodiesterase enzyme also known as calcium- and calmodulin-dependent phosphodiesterase ... Kakkar R, Raju RV, Sharma RK (July 1999). "Calmodulin-dependent cyclic nucleotide phosphodiesterase (PDE1)". Cell. Mol. Life ... Dousa TP (January 1999). "Cyclic-3',5'-nucleotide phosphodiesterase isozymes in cell biology and pathophysiology of the kidney ...
Myelin basic protein
Cyclic-nucleotide 3'-phosphodiesterase and multiple molecules of the Immune system. GRCh38: Ensembl release 89: ENSG00000197971 ... In general, the major form of MBP is a protein of about 18.5 Kd (170 residues). In melanocytic cell types, MBP gene expression ... 35 (7): 503-542. doi:10.1016/j.micron.2004.04.005. Boylan KB, Ayres TM, Popko B, et al. (1990). "Repetitive DNA (TGGA)n 5' to ... 264 (9): 5121-7. PMID 2466844. Edwards AM, Ross NW, Ulmer JB, Braun PE (1989). "Interaction of myelin basic protein and ...
This gene is a member of the type IV, cyclic AMP (cAMP)-specific, cyclic nucleotide phosphodiesterase (PDE) family. Cyclic ... The cyclic nucleotide phosphodiesterases (PDEs) regulate the cellular concentrations of cyclic nucleotides and thereby play a ... "Pivotal role of cyclic nucleoside phosphodiesterase 4 in Tat-mediated CD4+ T cell hyperactivation and HIV type 1 replication". ... cAMP-specific 3',5'-cyclic phosphodiesterase 4B is an enzyme that in humans is encoded by the PDE4B gene. ...
Cyclic GMP possibly opens cyclic nucleotide-gated (CNG) K+-selective channels, thereby causing hyperpolarization of the ... Kong, N., Xu, X., Zhang, Y., Wang, Y., Hao, X., Zhao, Y., Qiao, J., Xia, G. and Zhang, M. (2017) Natriuretic peptide type C ... The cGMP signal is terminated by the hydrolysis of cGMP through phosphodiesterase (PDE) activity and inactivation of GC. On ... The consequential hyperpolarization activates hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels. The ...
List of EC numbers (EC 3)
... cyclic-nucleotide 2'-phosphodiesterase EC 126.96.36.199: 3',5'-cyclic-nucleotide phosphodiesterase EC 188.8.131.52: now EC 184.108.40.206 EC ... type I site-specific deoxyribonuclease EC 220.127.116.11: type II site-specific deoxyribonuclease EC 18.104.22.168: type III site-specific ... cyclic-GMP phosphodiesterase EC 22.214.171.124: now with EC 126.96.36.199 EC 188.8.131.52: 2',3'-cyclic-nucleotide 3'-phosphodiesterase EC 3.1 ... cyclic-guanylate-specific phosphodiesterase EC 184.108.40.206: 3',5'-cyclic-AMP phosphodiesterase EC 220.127.116.11: N- ...
"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.. ... 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. ...
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 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. ...
"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. ...
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- ... 53 (5): 1110-7. doi:10.1095/biolreprod53.5.1110. PMID 8527515.. *^ Langin D, Laurell H, Holst LS, Belfrage P, Holm C (June 1993 ...
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, 18.104.22.168, 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, 22.214.171.124, 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. ... 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 *126.96.36.199 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. G protein can refer to two distinct families of proteins. Heterotrimeric G proteins, ...
Retinitis pigmentosa GTPase regulator
... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... guanyl-nucleotide exchange factor activity. • RNA binding. Cellular component. • cytoplasm. • ciliary basal body. • centrosome ... "Analysis of the RPGR gene in 11 pedigrees with the retinitis pigmentosa type 3 genotype: paucity of mutations in the coding ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ...
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. These include hydrolases such as: lipases, ...
G protein-coupled receptor
Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was ... Involved in growth and metastasis of some types of tumors.. *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. 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 ...
"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 ...
cGMP-specifična fosfodiesteraza, tip 5
Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Adv Cyclic Nucleotide Res ... http://www.garlandscience.com/textbooks/0815323042.asp?type=reviews. *Irwin H. Segel. Enzyme Kinetics: Behavior and Analysis of ... Fertel R, Weiss B (1976). „Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung" (abstract). ... Weiss B, Hait WN (1977). „Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annu. Rev ...
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. *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. This signalling molecule triggers smooth muscle relaxation and allows blood flow into the ... Although it is possible for mixed-type inhibitors to bind in the active site, this type of inhibition generally results from an ...
Luteinizing hormone/choriogonadotropin receptor
The cyclic AMP-regulatory dimers are degraded by phosphodiesterase and release 5'AMP. DNA in the cell nucleus binds to ... G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger. • activation of adenylate cyclase ... LHCGR have been found in many types of extragonadal tissues, and the physiologic role of some has remained largely unexplored. ... Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was ...
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 ... "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 ... 33 (7): 402-6. doi:10.1055/s-2001-16227. PMID 11507676.. *^ Holgado-Madruga M, Emlet DR, Moscatello DK, Godwin AK, Wong AJ ( ...
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 ... Eosinophil-derived neurotoxin is an enzyme that in humans is encoded by the RNASE2 gene. ... "The hexopyranosyl residue that is C-glycosidically linked to the side chain of tryptophan-7 in human RNase Us is alpha- ...
... acts as a phosphodiesterase (PDE) type-1 inhibitor in isolated rabbit aorta, Independent of vinpocetine's ... Hagiwara M, Endo T, Hidaka H (February 1984). "Effects of vinpocetine on cyclic nucleotide metabolism in vascular smooth muscle ... 7 (3): 240-3. June 2002. PMID 12126465.. *^ Shimizu Y, Saitoh K, Nakayama M, Suto K, Raikohara R, Nemoto T. "Agranulocytosis ... 7,10-13H2,1-2H3/t20-,22+/m1/s1 Y ... 7] In vitro and animal studies. Kindling models in rats ...
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) ... This page was last edited on 7 January 2018, at 17:31. ...
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 ...
Cyclic nucleotide phosphodiesterase. 3.1.6: Sulfatase. *arylsulfatase *Arylsulfatase A. *Arylsulfatase B. *Arylsulfatase E ... Type II. Type II site-specific deoxyribonuclease. Structure of the homodimeric restriction enzyme EcoRI (cyan and green ... Type V. Type V restriction enzymes (e.g., the cas9-gRNA complex from CRISPRs) utilize guide RNAs to target specific ... Type l. Type I restriction enzymes were the first to be identified and were first identified in two different strains (K- ...
Cloning and characterization of the human and mouse PDE7B, a novel cAMP-specific cyclic nucleotide phosphodiesterase
We have identified and characterised a novel member of the PDE7 family of cyclic nucleotide phosphodiesterases (PDE), which we ... Cyclic AMP * 3,5-Cyclic-AMP Phosphodiesterases * Cyclic Nucleotide Phosphodiesterases, Type 7 ... Cloning and characterization of the human and mouse PDE7B, a novel cAMP-specific cyclic nucleotide phosphodiesterase Biochem ... We have identified and characterised a novel member of the PDE7 family of cyclic nucleotide phosphodiesterases (PDE), which we ...
3'5'-cyclic nucleotide phosphodiesterase, catalytic domain superfamily (IPR036971) | InterPro | EMBL-EBI
Type 3 phosphodiesterase inhibitors may be protective against cerebrovascular events in patients with claudication.. null 17 ... The cyclic nucleotide phosphodiesterases (PDE) comprise a group of enzymes that degrade the phosphodiester bond in the second ... 35-cyclic nucleotide phosphodiesterase, catalytic domain superfamily (IPR036971). Short name: PDEase_catalytic_dom_sf ... They regulate the localisation, duration and amplitude of cyclic nucleotide signalling within subcellular domains. PDEs are ...
Identification of human PDE7B, a cAMP-specific phosphodiesterase
We isolated a human cAMP-specific phosphodiesterase (PDE7B) cDNA from human caudate nucleus. The human PDE7B was composed of ... 3,5-Cyclic-AMP Phosphodiesterases * Cyclic Nucleotide Phosphodiesterases, Type 7 * PDE7A protein, human ... Identification of human PDE7B, a cAMP-specific phosphodiesterase Biochem Biophys Res Commun. 2000 May 19;271(3):575-83. doi: ... We isolated a human cAMP-specific phosphodiesterase (PDE7B) cDNA from human caudate nucleus. The human PDE7B was composed of ...
Cyclic nucleotide phosphodiesterase - Wikipedia
"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 ...
EHNA - Wikipedia
"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 ... 7 (7): 733-8. doi:10.1016/0898-6568(95)00042-N. PMID 8519602. Méry PF, Pavoine C, Pecker F, Fischmeister R (July 1995). " ...
DIGITAL.CSIC: Phosphodiesterase 7 inhibition preserves dopaminergic neurons in cellular and rodent models of Parkinson disease
Cyclic-nucleotide phosphodiesterases. Nonsteroidal antiinflammatory drugs. Neuroblastoma sh-sy5y cells. Binding-protein-beta. ... This cyclic nucleotide plays a key role in signal transduction in a wide variety of cellular responses. In the brain, cAMP has ... Background]: Phosphodiesterase 7 plays a major role in down-regulation of protein kinase A activity by hydrolyzing cAMP in many ... cell types. ... Here we show a novel function of phosphodiesterase 7 inhibition ...
Publications - Mayo Clinic
Inhibitors of cyclic nucleotide phosphodiesterase isozymes type-III and type-IV suppress mitogenesis of rat mesangial cells. J ... Formation of reactive oxygen metabolites in glomeruli is suppressed by inhibition of cAMP phosphodiesterase isozyme type IV. ... Specific modulation of cyclic ADP-ribose-induced Ca2+ release by polyamines. Am J Physiol. 1995 Oct; 269 (4 Pt 1):C1042-7 View ... Metabolism of cyclic ADP-ribose in opossum kidney renal epithelial cells. Am J Physiol. 1995 Mar; 268 (3 Pt 1):C741-6 View ...
Alpha Actinin is Specifically Recognized by Multiple Sclerosis Autoantibodies Isolated Using an N-Glucosylated Peptide Epitope ...
2008) Transketolase and 2′,3′-cyclic-nucleotide 3′-phosphodiesterase type I isoforms are specifically recognized by IgG ... 2′,3′-cyclic-nucleotide 3′-phosphodiesterase. CNS. central nervous system. MuS. multiple sclerosis. MS/MS. tandem mass ... 1998) Dual implication of 2′,3′-cyclic nucleotide 3′ phosphodiesterase as major autoantigen and C3 complement-binding protein ... 2008) Designed glycopeptides with different beta-turn types as synthetic probes for the detection of autoantibodies as ...
PDE - Esterases (Phosphodi-) - Hydrolases - Enzymes - Products
Phosphodiesterases listed: PDE, PLC, PLD.  Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases ... They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. Roughly, the sub-types can ... No less than eleven sub-types of the enzyme family of phosphodiesterases (PDE; EC 3.1.4.-) are known to date, many of which ... 2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug ...
Human Liver CYP2B6-Catalyzed Hydroxylation of RP 73401 | Journal of Pharmacology and Experimental Therapeutics
RP 73401 is a potent inhibitor of cyclic nucleotide phosphodiesterase type IV. RP 73401 is metabolized by human liver ... 1) is a potent inhibitor of cyclic nucleotide PDE IV. Inhibition of PDE IV by RP 73401 results in an increase in cAMP levels in ... The cyclic nucleotide PDE isozymes have been classified into seven families based on sequence homology and functional ... 1994) Anti-inflammatory and bronchodilator properties of RP 73401, a novel and selective phosphodiesterase type IV inhibitor. ...
Type 5 Cyclic Nucleotide Phosphodiesterases Transient Receptor Potential Channels Calcineurin Pulmonary Artery ... Inhibition of phosphodiesterase-5 suppresses calcineurin/NFAT-mediated TRPC6 expression in pulmonary artery smooth muscle cells ... Liu, Q., Li, D., Berger, A. E., Johns, R. A. & Gao, L. Dec 1 2017 In : Scientific Reports. 7, 1, 11957. Research output: ... 36-42 7 p.. Research output: Research - peer-review › Article ... Single Nucleotide Polymorphism Medicine & Life Sciences Acute ...
Effect of type-selective inhibitors on cyclic nucleotide phosphodiesterase activity and insulin secretion in the clonal insulin...
... cyclic AMP, cyclic nucleotide phosphodiesterases, type 1, glucose, humans, insulin, insulin-like growth factor I, islets of ... Effect of type-selective inhibitors on cyclic nucleotide phosphodiesterase activity and insulin secretion in the clonal insulin ... Effect of type-selective inhibitors on cyclic nucleotide phosphodiesterase activity and insulin secretion in the clonal insulin ... 1. The cyclic nucleotide phosphodiesterases (PDEs) present in an insulin secreting cell line, BRIN - BD11, were characterized ...
Rapid nitric oxide-induced desensitization of the cGMP response is caused by increased activity of phosphodiesterase type 5...
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- ...
JoVE Search Results: Cyclic Nucleotide Phosphodiesterases%2C Type 5
The roles of cyclic nucleotide phosphodiesterases (PDEs) in steroidogenesis. Abstract Baillie, George S. University of Glasgow ... Cyclic adenosine monophosphate phosphodiesterase type 4 protects against atrial arrhythmias. Abstract Parent, Carole A. ... Cyclic nucleotide compartmentalization: contributions of phosphodiesterases and ATP-binding cassette transporters. Abstract ... Cyclic AMP-specific phosphodiesterase, PDE8A1, is activated by protein kinase A-mediated phosphorylation. Abstract ...
IL12B | Cancer Genetics Web
... cyclic-nucleotide phosphodiesterase). Enriched pathways include hsa04512 (ECM-receptor interaction), hsa04510 (Focal adhesion ... Type I diabetes mellitus KEGG. Data from KEGG and BioCarta [BIOCARTA terms] via CGAP [Hide] ... Nucleotide variation in IL-10 and IL-12 and their receptors and cervical and vulvar cancer risk: a hybrid case-parent triad and ... T-helper 1 type immune response - T-helper cell differentiation Data from Gene Ontology via CGAP [Hide] ...
LRP1B | Cancer Genetics Web
... cyclic-nucleotide phosphodiesterase). Enriched pathways include hsa04512 (ECM-receptor interaction), hsa04510 (Focal adhesion ... These two types of alterations occurring in multiple large CFS genes may contribute significantly to the heterogeneity observed ... Our results indicate that adult WT is a biological entity distinct from the corresponding pediatric tumor type.. Related: ... We here present the first published high-resolution genomic analysis of a mixed-type adult WT. This revealed a more pronounced ...
Tehranolide inhibits cell proliferation via calmodulin inhibition, PDE, and PKA activation | SpringerLink
Cyclic nucleotide phosphodiesterases: relating structure and function. Prog Nucleic Acid Res Mol Biol. 2001;65:1-52.PubMed ... Marika S, Ve´ronique M, Sylvie B, Manuel R. Sildenafil and vardenafil, types 5 and 6 phosphodiesterase inhibitors, induce ... 3,5-cyclic-nucleotide PDE, 2-mM cyclic AMP, and 100 μM CaM in 0.5 ml of Tris buffer solution (40 mM Tris-chloride, 0.1 mM MnCl2 ... Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents. Ann Rev Pharmacol Toxicol. 1977;17: ...
Immunologie, Immunopathologie et Chimie Thérapeutique - 2012
... a specific cyclic nucleotide phosphodiesterase type 4 (PDE4) inhibitor. PLos ONE, 7, e28899 (doi : 10.1371/journal.pone.0028899 ... Singh, P., Venkatesh, V., Nagapradeep, N., Verma, S. & Bianco A. (2012) G-quartet type self-assembly of guanine functionalized ... Novel glycolipid TLR2 ligands of the type Pam2Cys-α-Gal : Synthesis and biological properties. Eur. J. Med. Chem 51, 174-183 ( ... Mueller, Hess : Emerging functions of RANKL in lymphoid tissues, Frontiers in Immunology (2012) 3, article 261 : 1-7 (Review) ...
Find Research Outputs - Johns Hopkins University
11C](R)-Rolipram positron emission tomography detects DISC1 inhibition of phosphodiesterase type 4 in live Disc1 locus-impaired ... Hill-Briggs, F., Mar 1 2019, In : Diabetes care. 42, 3, p. 352-358 7 p.. Research output: Contribution to journal › Review ... Quigley, H. A., Feb 1 2019, In : Eye (Basingstoke). 33, 2, p. 254-260 7 p.. Research output: Contribution to journal › Review ... Valle, D., Mar 7 2019, In : American journal of human genetics. 104, 3, p. 389-390 2 p.. Research output: Contribution to ...
JCI Insight - Blocking MHC class II on human endothelium mitigates acute rejection
Functional regulatory T cells produced by inhibiting cyclic nucleotide phosphodiesterase type 3 prevent allograft rejection. ... If development into CTL occurs within the graft, the question arises as to which types of graft cells stimulate this process. ... Immunocompetent T-cells with a memory-like phenotype are the dominant cell type following antibody-mediated T-cell depletion. ... or type III (transmural arteritis) (44). The presence and degree of such vascular lesions is reported to correlate with the ...
Effect of sildenafil on ocular haemodynamics | Eye
Effects of sildenafil, a type-5 cGMP phosphodiesterase inhibitor, and papaverine on cyclic GMP and cyclic AMP levels in the ... Beova JA . Cyclic nucleotide phosphodiesterases: functional implications of multiple isoforms. Physiol Rev 1995;75:725-48. ... Sildenafil: an orally type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. ... Monitor recipients of phosphodiesterase type 5 inhibitors for glaucoma, pending more clinical evidence of risk Drugs & Therapy ...
Multiple cAMP phosphodiesterases act together to prevent premature oocyte meiosis and ovulation - Fingerprint -...
Type 4 Cyclic Nucleotide Phosphodiesterase 25% * Progesterone Receptors 18% * Progesterone 16% Powered by Pure, Scopus & ... Multiple cAMP phosphodiesterases act together to prevent premature oocyte meiosis and ovulation. ... Dive into the research topics of Multiple cAMP phosphodiesterases act together to prevent premature oocyte meiosis and ...
Phosphodiesterase 4B is essential for lipopolysaccharide-induced CC chemokine ligand 3 production in mouse macrophages.( ... Original Article, Report) by Journal of Medical Sciences; Health, general Gel electrophoresis Analysis Phosphodiesterases ... Biochemistry and physiology of cyclic nucleotide phosphodiesterases: Essential components in cyclic nucleotide signaling. Annu ... Regulation of distinct cyclic AMP-specific phosphodiesterase (phosphodiesterase type 4) isozymes in human monocytic cells. Mol ...
Effect of icariin on cyclic GMP levels and on the mRNA expression of cGMP-binding cGMP-specific phosphodiesterase (PDE5) in...
... a type-5 cGMP phosphodiesterase inhibitor, and papaverine on cyclic GMP and cyclic AMP levels in the rabbit corpus cavernosum ... Francis S H, Turko I V, Corbin J D. Cyclic nucleotide phosphodiesterases: relating structure and function. Prog Nucleic Acid ... penis erectile dysfunction icariin nitric oxide phosphodiesterase type 5 JIANG Zhaojian, male, born in 1968, Associate ... Effect of icariin on cyclic GMP levels and on the mRNA expression of cGMP-binding cGMP-specific phosphodiesterase (PDE5) in ...
Cyclic Nucleotide Phosphodiesterase PDE7 Family. Cyclic Nucleotide Phosphodiesterases, Type 7A. Cyclic Nucleotide ... Cyclic Nucleotide Phosphodiesterases, Type 7A - Narrower Concept UI. M0507070. Preferred term. Cyclic Nucleotide ... Cyclic Nucleotide Phosphodiesterases, Type 7B - Narrower Concept UI. M0507071. Preferred term. Cyclic Nucleotide ... A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type ...
Type 3 Cyclic Nucleotide Phosphodiesterases Medicine & Life Sciences Knockout Mice Medicine & Life Sciences ... XIA, W., Pessentheiner, A., Walenta, E., Rülicke, T., Schreiber, R., Hofer, D., Amor, M. & Bogner-Strauß, J. G., 7 Mar 2017, ( ... 7, p. 1948-1961 14 p.. Research output: Contribution to journal › Article › Research › peer-review ...
Find Research Outputs - Montclair State University
Type 3 Cyclic Nucleotide Phosphodiesterases * Apoptosis * Somatomedins * Cardiac Myocytes 46 Scopus citations ... Gao, Y. Q., Gao, N. Y., Deng, Y., Gu, J. S., Shen, Y. C. & Wang, S. X., 1 Jan 2012, In : Water Environment Research. 84, 7, p. ... Yang, Y., Gao, N., Deng, Y. & Zhou, S., 1 Sep 2012, In : Applied Clay Science. 65-66, p. 80-86 7 p.. Research output: ... of extracellular signal-regulated kinase 5 reduces cardiac apoptosis and dysfunction via inhibition of a phosphodiesterase 3A/ ...
Fine mapping of AHI1 as a schizophrenia susceptibility gene: from association to evolutionary evidence - PubMed
Cyclic Nucleotide Phosphodiesterases, Type 7 / genetics Actions. * Search in PubMed * Search in MeSH ... Our strongest findings lay within the AHI1 gene: single-nucleotide polymorphisms rs11154801 and rs7759971 showed significant ... 2009 Oct 5;150B(7):914-25. doi: 10.1002/ajmg.b.30918. Am J Med Genet B Neuropsychiatr Genet. 2009. PMID: 19152384 ...
A genome-wide scan for common variants affecting the rate of age-related cognitive decline - PubMed
Cyclic Nucleotide Phosphodiesterases, Type 7 / genetics Actions. * Search in PubMed * Search in MeSH ... Using aggregate measures of genetic risk, we find that known susceptibility loci for cardiovascular disease, type 2 diabetes, ... 2013 Sep 1;70(9):1150-7. doi: 10.1001/jamaneurol.2013.2815. JAMA Neurol. 2013. PMID: 23836404 Free PMC article. ...
Biology - Research Output - Montclair State University
Type 3 Cyclic Nucleotide Phosphodiesterases * Phosphoric Diester Hydrolases * Cardiac Myocytes * Apoptosis * Isoproterenol ... Antiviral activity of theaflavin digallate against herpes simplex virus type 1. De Oliveira, A., Prince, D., Lo, C. Y., Lee, L ... Analysis of the population structure of Anaplasma phagocytophilum using multilocus sequence typing. Huhn, C., Winter, C., ... A positive feedback loop of phosphodiesterase 3 (PDE3) and inducible cAMP early repressor (ICER) leads to cardiomyocyte ...
InhibitorsInhibitionPDEsAdenosinePDE5PDE4GuanosineSingle Nucleotide PIntracellularMonophosphateHydrolysisNitricMolecularActivitySuperfamilySpecific phosphodiesteraseFamily of phosphodiesterasesProteinsSubunitDegradationInhibitor of phosphodiesteraseCyclasesSildenafilEnzymeNeuronsMetabolismHomologPotentCellsPhysiologicalSubfamilyRecombinantGlial cellEnzymes that degradePhenotypeRegulatesRetinalCAMPConcentrationsTadalafilCardiacHumanCalcium
- Type 3 phosphodiesterase inhibitors may be protective against cerebrovascular events in patients with claudication. (ebi.ac.uk)
- Finally, S14 neuroprotective effects were reversed by blocking the cAMP signaling pathways that operate through cAMP-dependent protein kinase A. [Conclusions/Significance]: Our findings demonstrate that phosphodiesterase 7 inhibition can protect dopaminergic neurons against different insults, and they provide support for the therapeutic potential of phosphodiesterase 7 inhibitors in the treatment of neurodegenerative disorders, particularly Parkinson disease. (csic.es)
- 1. The cyclic nucleotide phosphodiesterases (PDEs) present in an insulin secreting cell line, BRIN - BD11, were characterized using calcium/calmodulin, IGF-1, isoenzyme-selective PDE inhibitors and RT - PCR. (strath.ac.uk)
- Background: Phosphodiesterase 4 (PDE4) inhibitors negatively modulate many inflammatory responses, and some of these pharmacological effects are mediated by inhibition of PDE4B in inflammatory cells. (thefreelibrary.com)
- sup] By increasing intracellular cAMP level, phosphodiesterase 4 (PDE4) inhibitors are being developed as anti-inflammatory agents for the treatment of chronic inflammatory disorders such as asthma, chronic obstructive pulmonary disease, and psoriasis. (thefreelibrary.com)
- Are Phosphodiesterase-5 Inhibitors a New Frontier for Prevention of Colorectal Cancer? (harvard.edu)
- Several different lines of evidence suggest that a COX-independent mechanism may be fully or partially responsible for the antineoplastic activities of NSAIDs and COX-2-selective inhibitors ( 7 - 12 ). (aacrjournals.org)
- 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)
- Using phosphodiesterase type 5 (PDE5) inhibitors, we and others have provided evidence of rescued F508del-CFTR trafficking and corrected deficient chloride transport activity. (frontiersin.org)
- Treatment opportunities involving phosphodiesterase inhibitors (PDEIs) and purinergic modulators may plausibly exist. (iacfsme.org)
- Inhibition of cyclic nucleotide PDEs allow cAMP/cGMP concentrations to increase within cells  and inhibition of PDE by PDE inhibitors can cause a variety of cellular effects and can influence various physiological functions. (spotidoc.com)
- 15 Volume 1 Issue 3 2012 Phosphodiesterase type 5 (PDE5) inhibitors are the most efficient oral drugs in the treatment of ED[40,41] and should be considered first-line therapy. (spotidoc.com)
- 2 , 3 The therapeutic utility of controlling the intracellular levels of cyclic-AMP, and of cyclic guanosine monophosphate (cyclic-GMP), with PDE inhibitors is well established. (bloodjournal.org)
- These data suggest that phosphodiesterase type 5 inhibitors may have effects that distinguish them from other treatments for pulmonary hypertension and merit further study. (ersjournals.com)
- Even though cGMP binding to the catalytic site stimulates cyclic-nucleotide binding to the allosteric [ 5 ] sites, inhibitors do not elicit the same function. (ijddr.in)
- Currently there are three (Sildenafil, vardenafil and tadalafil) Phosphodiesterase type-5 inhibitors (PDE5-i) used in the treatment of male ED [ 6 ]. (ijddr.in)
- Our earliest understanding of phosphodiesterase (PDE) inhibitors began with a series of publications by Sutherland and Rall in the 1950s, describing the properties of cyclic adenosine monophosphate (cAMP). (beds.ac.uk)
- By the 1960s, the role of cyclic nucleotide second messengers, such as cAMP, in cell signaling and homeostasis was established, and regulation of this pathway by PDE inhibitors arose as a field of considerable interest. (beds.ac.uk)
- Given that phototransduction relies on the hydrolysis of cGMP via phosphodiesterase 6 (PDE6), we examined ROS growth and shedding in zebrafish treated with cGMP-specific PDE inhibitors. (arvojournals.org)
- We aimed to determine which mechanism possibly accounts for the beneficial effect by investigating its vascular action in different in vitro preparations in comparison with other coxibs and reference phosphodiesterase-5 (PDE5) inhibitors. (unboundmedicine.com)
- The article from Oliver et al 2 published in this issue of Hypertension represents the first study performed with an accurate experimental design and methodology demonstrating that inhibitors of isoform 5 of phosphodiesterase (PDE) might be potentially used as a new drug class for the treatment of essential hypertension. (ahajournals.org)
- Furthermore, a description of recent research on this pathway through the use of phosphodiesterase inhibitors is emphasized. (intechopen.com)
- Poor understanding of the topography of cyclic nucleotide (CN) phosphodiesterase (PDE) catalytic sites compromises development of potent, selective inhibitors for therapeutic use. (aspetjournals.org)
- Both cAMP and cGMP have been shown to have antiproliferative and proapoptotic effects in many cell types ( 15 , 16 ), and numerous studies have described the growth-inhibitory and apoptosis-inducing effects of various PDE inhibitors on certain tumor cell types, including colorectal cancer cells ( 17 - 20 ). (aacrjournals.org)
- Phosphodiesterase 5 inhibition in essential hypertension. (ebi.ac.uk)
- Methodology/Principal Findings]: Here we show a novel function of phosphodiesterase 7 inhibition on nigrostriatal dopaminergic neuronal death. (csic.es)
- Phosphodiesterase 5 Inhibition Limits Doxorubicin-induced Heart Failure by Attenuating Protein Kinase G Ia Oxidation. (harvard.edu)
- The inhibitory effect of ANP on glutamate release is reversed by selectively activating protein kinase A. These results demonstrate strong presynaptic inhibition by natriuretic peptides in the brain and suggest important physiological and behavioral roles of PDE2A in modulating neurotransmitter release by negative crosstalk between cGMP-signaling and cyclic adenosine monophosphate-signaling pathways. (pnas.org)
- Phosphodiesterase 4 (PDE4) inhibition restores the suppressive effects of 3′,5′-cyclic adenosine monophosphate in lymphocytes. (bloodjournal.org)
- 6 Mechanistically, PDE4 inhibition resulted in elevation of intracellular cyclic-AMP levels and suppression of PI3K and AKT activity. (bloodjournal.org)
- In the search for therapeutic strategies that engage the cGMP signalling pathway for the treatment of pulmonary arterial hypertension (PAH), inhibition of cGMP metabolism by phosphodiesterase type 5 (PDE5)-targeted compounds has proven most successful to date. (ersjournals.com)
- This was supported by studies for vasorelaxation, interaction with the NO/cGMP pathway, and measurement of cyclic nucleotide amounts released from rat aortic rings, and inhibition of human PDE5 as well as PDE4 activity. (unboundmedicine.com)
- 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)
- PDE terminates second messenger signaling by degrading cyclic nucleotides, whereas inhibition of PDE activity blocks cyclic nucleotide degradation to mimic or amplify cyclic nucleotide signaling. (aacrjournals.org)
- Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling. (bvsalud.org)
- Screening of AMP- and GMP-producing enzymes such as phosphodiesterases (PDEs), ligases, and synthetases would be simplified by the ability to directly detect unmodified nucleoside monophosphates. (nih.gov)
- This project aims to unite global efforts to target the highly druggable class of enzymes called cyclic nucleotide phosphodiesterases (PDEs) in the fight for neglected parasitic diseases (NPD). (europa.eu)
- The level of intracellular cAMP is controlled through its production by adenylyl cyclases and its breakdown by cyclic nucleotide phosphodiesterases (PDEs). (lu.se)
- INTRODUCTION Phosphodiesterases (PDEs) are a superfamily of enzymes that degrade cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) [1-3]. (spotidoc.com)
- In animals across taxa, cGMP signals influence cellular physiology by acting on cGMP-stimulated protein kinase G (PKG), cyclic nucleotide-gated (CNG) channels, or cGMP-sensitive phosphodiesterases (PDEs) ( 3 , 4 ). (pnas.org)
- 1 The synthesis and degradation of cyclic-AMP are tightly controlled by 2 classes of enzymes, adenylyl cyclases and phosphodiesterases (PDEs), respectively. (bloodjournal.org)
- Functions of cyclic GMP include the regulation of cation channels and PDEs and activation of cyclic GMP-dependent protein kinase (PKG). (ersjournals.com)
- PKG), cGMP-regulated phosphodiesterases (PDEs) and cyclic nucleotide-gated ion channels 4 . (ersjournals.com)
- The levels of these intracellular cyclic nucleotides are regulated by the cyclases that synthesize and phosphodiesterases (PDEs) that degrades them into inactive metabolite [ 1 ]. (ijddr.in)
- 8 These and other studies 9,10 also underlined the importance of cAMP phosphodiesterases (PDEs) for the spatiotemporal control of cAMP signals. (ahajournals.org)
- 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)
- Elevation of the second messenger cyclic adenosine monophosphate (cAMP) in macrophages suppresses several inflammatory responses, including inflammatory mediator production and receptor-mediated phagocytosis. (thefreelibrary.com)
- Cyclic adenosine monophosphate phosphodiesterase type 4 protects against atrial arrhythmias. (nih.gov)
- It is based on adenosine triphosphate (ATP) and its derivatives, ADP and adenosine as well as the purine nucleotide UTP. (iacfsme.org)
- PDE2A is richly expressed in the axonal terminals of MHb neurons, and its activation by cGMP depletes cyclic adenosine monophosphates. (pnas.org)
- The second messenger 3′,5′-cyclic adenosine monophosphate (cyclic-AMP) uses effector proteins to influence cell function and fate. (bloodjournal.org)
- There are two important secondary messengers that regulate many physiological processes i.e., 3′,5′-cyclic adenosine monophosphate (cAMP) and 3′,5′-cyclic guanosine monophosphate (cGMP). (ijddr.in)
- 3. The PDE1/PDE5 inhibitor zaprinast inhibited both cyclic AMP and cyclic GMP PDE activity in both pellet and supernatant fractions of cell homogenates by a maximum of around 25% (IC(50) 1 - 5 microM), while rolipram (PDE4 selective) inhibited only cyclic AMP hydrolysis. (strath.ac.uk)
- Furthermore, the effects of ICA on the mRNA expression of specific cGMP-binding phosphodiesterase type V (PDE5) in rat penis were also observed. (springer.com)
- Expression of three isoforms of cGMP-biding cGMP-Specific phosphodiesterase (PDE5) in human penile cavernosum. (springer.com)
- Phosphodiesterase type 5 (PDE5) hydrolyses cyclic guanylate monophosphate (cGMP) specifically to 5' GMP. (spotidoc.com)
- In vascular smooth muscle cells, NO interacts with soluble guanylyl cyclase (sGC) to convert guanosine triphosphate (GTP) to cyclic GMP, which is hydrolysed and inactivated by phosphodiesterase type 5 (PDE5). (ersjournals.com)
- PKG is the most important of these intracellular mediators, whereas the cGMP-regulated PDE type 5 (PDE5) is mainly responsible for modulating intracellular cGMP levels and PKG-dependent signalling produced by NO and natriuretic peptides 5 - 7 . (ersjournals.com)
- In addition to these feedback mechanisms, there is the potential for gene regulation, as the promoter region of human PDE5 contains sites responsive to cyclic nucleotides 11 , 12 . (ersjournals.com)
- Vardenafil has higher affinity to phosphodiesterase-5 (PDE5) than sildenafil and lower administered dosage for the treatment of erectile dysfunction. (aspetjournals.org)
- While inactivation of PDE4B, but not other PDE4 isotypes, is known to inhibit lipopolysaccharide (LPS)-induced tumor necrosis factor-a (TNF-a) production in macrophages, a cell type critical in mediating innate immunity, the impact of PDE4B on many other inflammatory responses in these cells remains largely unknown. (thefreelibrary.com)
- Anchored PDE4 regulates chloride conductance in wild-type and ΔF508-CFTR human airway epithelia. (nih.gov)
- Recently, EHNA was shown to block the activity of purified soluble cGMPstimulated phosphodiesterase (PDE2) from frog, human, and porcine heart with an apparent Ki value of approximately 1 microM and with negligible effects on Ca2+/calmodulin PDE (PDE1), cGMP-inhibited PDE (PDE3), and low Km cAMP-specific PDE (PDE4) (Méry, P.F., C. Pavoine, F. Pecker, and R. Fischmeister. (ubi.pt)
- Here, we review a decade-long exploration of the contribution of cyclic-AMP and PDE4 to the pathogenesis of B-cell lymphoma, 5 ⇓ ⇓ ⇓ - 9 culminating with the first-in-cancer clinical trial of a PDE4 inhibitor in advanced B-cell malignancies. (bloodjournal.org)
- 6 These data linked the cyclic-AMP/PDE4 axis to the essential tonic BCR signals, highlighting the potential impact of PDE4 modulation in malignant B cells ( Figure 1 ). (bloodjournal.org)
- 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)
- Penile erection is caused through vascular pressure changes within the corpora cavernosa wherein the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) pathway plays the key physiological mediator of erection. (spotidoc.com)
- The heart peptide hormone atrial natriuretic peptide (ANP) regulates blood pressure by stimulating guanylyl cyclase-A to produce cyclic guanosine monophosphate (cGMP). (pnas.org)
- In addition to GPCRs, a unique family of receptors known as membrane guanylyl cyclases (GCs) can be activated by neuropeptides such as natriuretic peptides to catalyze the intracellular production of cyclic guanosine monophosphate (cGMP) ( 2 , 3 ). (pnas.org)
- Among the most important for pulmonary vascular homeostasis are factors that utilise cyclic guanosine monophosphate (cGMP) as an intracellular second messenger. (ersjournals.com)
- Schematic diagram of the nitric oxide (NO)-cyclic guanosine monophosphate (GMP) signalling pathway. (ersjournals.com)
- Two subtypes of natriuretic peptide receptor (NPR), NPR-A and NPR-B, are transmembrane guanylyl cyclases (particulate guanylyl cyclases), where the extracellular domain binds atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP) or C-type natriuretic peptide and the intracellular domain hydrolyses guanosine triphosphate (GTP) to cGMP. (ersjournals.com)
- A vast number of studies have focused on understanding the nitric oxide (NO) signaling pathway, which culminates with the phosphorylation of the transcription factor cAMP-responsive element-binding protein (CREB) through the increase of the second messenger cyclic guanosine monophosphate (cGMP) and activation of cGMP-dependent protein kinase. (intechopen.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)
- Mechanistic studies have shown that sulindac sulfone and several structurally related analogues can inhibit cyclic guanosine 3′,5′-monophosphate (cGMP) phosphodiesterase (PDE) activity at concentrations that are comparable with those required to inhibit colon tumor cell growth and induce apoptosis ( 12 - 14 ). (aacrjournals.org)
- Lighting up cGMP signaling The second messenger cyclic guanosine monophosphate (cGMP) alters ion channel activity to mediate processes such as smooth muscle relaxation, transduction of light, and apoptosis. (semanticscholar.org)
Single Nucleotide P2
- A study of alveolar rhabdomyosarcoma copy number alterations by single nucleotide polymorphism analysis. (cancerindex.org)
- Although both SLC30A8 rs13266634 single nucleotide polymorphism and plasma zinc concentrations have been associated with impaired glucose regulation (IGR) and type 2 diabetes (T2D), their interactions for IGR and T2D remain unclear. (diabetesjournals.org)
- Sahauran, kharar, Distt-Mohali (Punjab), India ABSTRACT Phosphodiesterases are enzymes that catalyzes the hydrolysis of cAMP and /or cGMP and thereby regulates intracellular levels of second messangers. (spotidoc.com)
- Steady-state activation of cardiac β-adrenergic receptors leads to an intracellular compartmentation of cAMP resulting from localized cyclic nucleotide phosphodiesterase (PDE) activity. (ahajournals.org)
- To address this need, we developed polyclonal and monoclonal antibodies that recognize AMP and GMP with nanomolar sensitivity and high selectivity vs. the corresponding triphosphate and 3',5'-cyclic monophosphate nucleotides that serve as substrates for many enzymes in these classes. (nih.gov)
- PDE is a metallophosphohydrolase that specifically hydrolyzes the 3′,5′-cyclic phosphate moiety on cyclic nucleotides to a 5′-monophosphate, thereby deactivating cyclic AMP (cAMP) or cGMP. (aacrjournals.org)
- 2. Calmodulin activated cyclic AMP or cyclic GMP PDE activity in pellet and was 3 fold (P=0.002) more potent in activating cyclic nucleotide hydrolysis in pellet compared with supernatant fractions. (strath.ac.uk)
- Here, we show that sulindac sulfide (SS) induces apoptosis and inhibits the growth of human breast tumor cells with IC 50 values of 60 to 85 μmol/L. Within the same concentration range, SS inhibited cyclic GMP (cGMP) hydrolysis in tumor cell lysates but did not affect cyclic AMP hydrolysis. (aacrjournals.org)
- The enzymatic activity of CNPase, the hydrolysis of 2',3'-cyclic nucleotides to 2'-nucleotides, was the basis of the discovery of the enzyme from brain tissue in the 1960s [ 12 ]. (biomedcentral.com)
- According to their specificity toward hydrolysis of cyclic AMP (CAMP) or cyclic GMP (cGMP) can be grouped into 11 families [ 2 ]. (ijddr.in)
- 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)
- McDonald L G, Murad F. Nitric oxide and cyclic GMP signaling. (springer.com)
- These include nitric oxide and the natriuretic peptide family (atrial, brain and C-type natriuretic peptides). (ersjournals.com)
- 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)
- Background]: Phosphodiesterase 7 plays a major role in down-regulation of protein kinase A activity by hydrolyzing cAMP in many cell types. (csic.es)
- 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)
- In order to determine the role of tehranolide on calmodulin (CaM) structure and activity, its effects were evaluated with fluorescence emission spectra and CaM-mediated activation of phosphodiesterase (PDE1), in comparison with artemisinin. (springer.com)
- SS did not induce apoptosis of normal human mammary epithelial cells (HMEC) nor did it inhibit phosphodiesterase (PDE) activity in HMEC lysates. (aacrjournals.org)
- The effect of cGMP (cyclic GMP) dependent protein kinase 1-β (PKG1-β) and cGMP analogues on transcriptional activity and replication of human immunodeficiency virus type 1 (HIV-1) was investigated. (biomedcentral.com)
- 42 , 43 Cyclic-AMP (cAMP) downmodulates this positive signaling wave by suppressing SYK and PI3Kδ activity. (bloodjournal.org)
- Site-specific mutagenesis of the catalytic subunit of cholera toxin: substituting lysine for arginine 7 causes loss of activity. (usc.edu)
- The baseline luciferase activity in PC-3 cells transfected with the wild-type DR5 reporter was significantly augmented in cells transfected with DR5 constructs carrying deletions or mutation in the YY1-binding site. (aacrjournals.org)
- Treatment with drug enhanced DR5 wild-type luciferase activity, with no increase in cells transfected with the YY1-deleted or YY1-mutated constructs. (aacrjournals.org)
- It has been shown to exhibit potent tumoricidal activity against a variety of human cancer cell lines in vitro and in vivo with minimal or no toxicity to nonmalignant human cells ( 7 ). (aacrjournals.org)
- Earlier work has suggested that a human exopolyphosphatase, Prune, might exhibit cyclic nucleotide phosphodiesterase activity. (biomedcentral.com)
- Finally, the study investigates the potential cyclic nucleotide phosphodiesterase activity of TbrPPX1. (biomedcentral.com)
- Importantly, TbrPPX1 does not exhibit any cyclic nucleotide specific phosphodiesterase activity, which definitively eliminates it as an additional player in cAMP signalling of the kinetoplastida. (biomedcentral.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 polyphosphatases belong to the large superfamily of the DHH phosphoesterases [ 7 ]. (biomedcentral.com)
- We isolated a human cAMP-specific phosphodiesterase (PDE7B) cDNA from human caudate nucleus. (nih.gov)
- Sildenafil: an orally type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. (nature.com)
- 1. A method for treating erectile dysfunction in a male individual, comprising locally administering to the individual an effective amount of a pharmaceutical composition consisting essentially of a Type V, cGMP-specific phosphodiesterase inhibitor or a pharmaceutically acceptable salt, ester, amide or prodrug thereof. (google.com.au)
- 18. A pharmaceutical formulation for treating erectile dysfunction in an individual, comprising a urethral dosage form of a phosphodiesterase inhibitor, a carrier suitable for transurethral drug administration, and, optionally, a transurethral permeation enhancer, wherein the phosphodiesterase inhibitor is a Type V, cGMP-specific phosphodiesterase inhibitor, or a pharmaceutically acceptable salt ester, amide or prodrug thereof. (google.com.au)
Family of phosphodiesterases1
- 3'5'-cyclic nucleotide phosphodiesterases are a family of phosphodiesterases. (wikipedia.org)
- The large array of CaM targets identified to date includes protein kinases, the ubiquitous protein phosphatase calcineurin, adenyl cyclase, cyclic nucleotide phosphodiesterase, and cytoskeletal proteins such as spectrin and adducin. (genetics.org)
- The energetic type of Rab protein, which contains GTP, can recruit particular binding partners such as for example sorting adaptors, tethering elements, kinases, motor and phosphatases proteins, and impact vesicle formation, transportation, and tethering [9C12]. (antibodyassay.com)
- The GTP-bound energetic type of Rab could be recruited to membrane vesicles, where it promotes membrane trafficking by getting together with UNC-1999 supplier particular effector proteins (Shape 1A) [18,19]. (antibodyassay.com)
- The protein consists of two domains: an uncharacterized N-terminal domain with little homology to other proteins, and a C-terminal phosphodiesterase domain. (biomedcentral.com)
- They arise during development from oligodendrocyte precursor cells (OPCs),  which can be identified by their expression of a number of antigens , including the ganglioside GD3,  the NG2 chondroitin sulfate proteoglycan , and the platelet-derived growth factor-alpha receptor subunit (PDGF-alphaR). (wikipedia.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)
- Furthermore, this increase in cGMP degradation is paralleled by the phosphorylation of phosphodiesterase type 5 at Ser-92. (rupress.org)
- Novel Mechanism for Cyclic Dinucleotide Degradation Revealed by Structural Studies of Vibrio Phosphodiesterase V-cGAP3. (harvard.edu)
Inhibitor of phosphodiesterase2
- We found that S14, a heterocyclic small molecule inhibitor of phosphodiesterase 7, conferred significant neuronal protection against different insults both in the human dopaminergic cell line SH-SY5Y and in primary rat mesencephalic cultures. (csic.es)
- Moreland RB, Goldstein I, Traish A . Sildenafil, a novel inhibitor of phosphodiesterase type 5 human corpus cavernosum smooth muscle cells. (nature.com)
- Guanylyl cyclases and signaling by cyclic GMP. (semanticscholar.org)
- Sildenafil (Viagra), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction. (nature.com)
- Effects of sildenafil on the relaxation of human corpus cavernosum tissue in vitro and on the activities of cyclic nucleotide phosphodiesterase isozymes. (nature.com)
- Effects of sildenafil, a type-5 cGMP phosphodiesterase inhibitor, and papaverine on cyclic GMP and cyclic AMP levels in the rabbit corpus cavernosum in vitro . (nature.com)
- Recently FDA approved sildenafil for the treatment of pulmonary hypertension due to its vasodilatory and antiproliferative effect on the pulmonary [ 7 ] vasculature. (ijddr.in)
- 6. The method of claim 5, wherein the Type V phosphodiesterase is sildenafil or a pharmaceutically acceptable salt thereof. (google.com.au)
- The systematic for this enzyme is 3',5'-cyclic-nucleotide 5'-nucleotidohydrolase. (wikipedia.org)
- Several isoforms of the enzyme type exist, each with its own tissue localization. (bvsalud.org)
- 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNPase) is an enigmatic enzyme specifically expressed at high levels in the vertebrate myelin sheath, whose function and physiological substrates are unknown. (biomedcentral.com)
- 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNPase) is an enzyme expressed abundantly in myelin. (biomedcentral.com)
- Gut NCSCs are self-renewing and multipotent, give rise to diverse types of neurons and glia in vivo, and persist in the gut throughout adult life ( 13 - 15 ). (sciencemag.org)
- Murad F. Cyclic GMP: synthesis, metabolism, and function. (springer.com)
- Origin of Exopolyphosphatase Processivity: Fusion of an ASKHA Phosphotransferase and a Cyclic Nucleotide Phosphodiesterase Homolog. (purdue.edu)
- Recombinant PDE7B expressed in transfected COS-7 cells had a low cAMP K(m) value of 0. (nih.gov)
- 13 microM, which is similar to the K(m) value of recombinant human PDE7A expressed in transfected COS-7 cells. (nih.gov)
- 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)
- Vertebrates rely on retinal rods and cones for the conventional, image-forming vision while non-image-forming vision is mediated by intrinsically photosensitive retinal ganglion cells (ipRGCs) (see Part II Chapter 7). (utah.edu)
- Depolarization-induced insulin secretion was assessed and in models where PDE3B was overexpressed [islets from transgenic RIP-PDE3B/7 mice and adenovirally (AdPDE3B) infected INS-I (832/13) cells], the first phase of. (lu.se)
- Depolarization-induced insulin secretion was assessed and in models where PDE3B was overexpressed [islets from transgenic RIP-PDE3B/7 mice and adenovirally (AdPDE3B) infected INS-I (832/13) cells], the first phase of insulin secretion, occurring in response to stimulation with high K+ for 5 min, was significantly reduced (similar to 25% compared to controls). (lu.se)
- Further, stimulation of isolated beta-cells from RIP-PDE3B/7 islets, using successive trains of voltage-clamped depolarizations, resulted in reduced Ca2+-triggered first phase exocytotic response as well as reduced granule mobilization-dependent second phase, compared to wild-type beta-cells. (lu.se)
- Human immunodeficiency virus type 1 vectors with alphavirus envelope glycoproteins produced from stable packaging cells. (purdue.edu)
- Oligodendrocytes (from Greek ' cells with a few branches'), or oligodendroglia , are a type of neuroglia whose main functions are to provide support and insulation to axons in the central nervous system of some vertebrates , equivalent to the function performed by Schwann cells in the peripheral nervous system . (wikipedia.org)
- Adams SR, Harootunian AT, Buechler YJ, Taylor SS, Tsien RY (1991) Fluorescence ratio imaging of cyclic AMP in single cells. (springer.com)
- They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. (axonmedchem.com)
- The physiological substrate for the enzymatic reaction of CNPase has been a mystery, because 2',3'-cyclic nucleotides have not been discovered in vivo . (biomedcentral.com)
- Any extracellular stimulation causes a rapid change in the level of cyclic nucleotide, producing the physiological responses elicited by the stimulus. (ijddr.in)
- A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. (harvard.edu)
- Subfamily 1 includes the bacterial RecJ nucleases, while subfamily 2 members fall into three functional groups, the pyrophosphatases, the exopolyphosphatases and the closely related "prune-type" exopolyphosphatases. (biomedcentral.com)
- We performed direct measurements of the cyclic nucleotide level in the subsarcolemmal and cytosolic compartments using a recombinant CNG channel 12 and the FRET-based Epac2-camps sensor, 13 respectively. (ahajournals.org)
- Oligodendrocytes are a type of glial cell . (wikipedia.org)
Enzymes that degrade1
- The cyclic nucleotide phosphodiesterases (PDE) comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. (ebi.ac.uk)
- Prior to death in the first larval instar, Cam nulls show a striking behavioral abnormality (spontaneous backward movement) whereas a mutation, Cam 7 , that results in a single amino acid change (V91G) produces a very different phenotype: short indented pupal cases and pupal death with head eversion defects. (genetics.org)
- Genetic interaction studies suggest that failed regulation of the muscle calcium release channel, the ryanodine receptor, is the major defect underlying the Cam 7 phenotype. (genetics.org)
- Phosphodiesterase 4B in the cardiac L-type Ca²⁺ channel complex regulates Ca²⁺ current and protects against ventricular arrhythmias in mice. (nih.gov)
- Retinal 3',5'-cGMP phosphodiesterase is located in photoreceptor outer segments: it is light activated, playing a pivotal role in signal transduction. (ebi.ac.uk)
- Soderling S H, Beavo J A. Regulation of cAMP and cGMP signaling: new phosphodiesterases and new functions. (springer.com)
- In this chapter, we review some of the evidence in support of compartmentalisation of cAMP/PKA signalling, and we summarise recent findings indicating that distinct pools of cAMP, under the control of different phosphodiesterases, have opposing effects on cardiac myocytes hypertrophic growth. (springer.com)
- To evaluate the time course of the cAMP changes in the different compartments, brief (15 seconds) pulses of isoprenaline (100 nmol/L) were applied to adult rat ventricular myocytes (ARVMs) while monitoring cAMP changes beneath the membrane using engineered cyclic nucleotide-gated channels and within the cytosol with the fluorescence resonance energy transfer-based sensor, Epac2-camps. (ahajournals.org)
- cAMP kinetics in the two compartments were compared to the time course of the L-type Ca 2+ channel current ( I Ca,L ) amplitude. (ahajournals.org)
- Indeed, the presence of subcellular compartments with different cAMP concentrations, also called cAMP microdomains, are inferred from L-type Ca 2+ channel current ( I Ca,L ) measurements in response to local β-AR stimulation in cardiomyocytes 5 and by direct monitoring of cAMP using fluorescence resonance energy transfer (FRET)-based sensors 6,7 or cyclic nucleotide-gated (CNG) channels. (ahajournals.org)
- Both PDE2 and PDE3 may contribute to keep the cyclic nucleotides concentrations at minimum in the absence of adenylyl and/or guanylyl cyclase stimulation. (ubi.pt)
- Analysis of short-term treatment with the phosphodiesterase type 5 inhibitor tadalafil on long bone development in young rats. (harvard.edu)
- To investigate the role of PDE2 in the regulation of cardiac L-type Ca2+ current (ICa), we have examined the effect of EHNA on ICa in freshly isolated human atrial myocytes. (ubi.pt)
- It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. (bvsalud.org)
- Human immunodeficiency virus type 1-derived lentivirus vectors pseudotyped with envelope glycoproteins derived from Ross River virus and Semliki Forest virus. (purdue.edu)
- There are 11 human cyclic nucleotide phosphodiesterase (PDE) families. (aspetjournals.org)
- For example, studies have shown that the non-COX-inhibitory sulfone metabolite of the NSAID sulindac can inhibit human colon tumor cell growth and induce apoptosis in vitro ( 7 , 8 ). (aacrjournals.org)
- Bolger G, Michaeli T, Martins T, St John T, Steiner B, Rodgers L, Riggs M, Wigler M, Ferguson K: A family of human phosphodiesterases homologous to the dunce learning and memory gene product of Drosophila melanogaster are potential targets for antidepressant drugs. (drugbank.ca)
- Two pairs of EF-hand-type calcium-binding sites are present in each of its two globular domains and conformational changes produced by calcium binding dramatically alter the target interaction properties of the protein. (genetics.org)