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)
Enzymes that catalyze the hydrolysis of CYCLIC AMP to form adenosine 5'-phosphate. The enzymes are widely distributed in animal tissue and control the level of intracellular cyclic AMP. Many specific enzymes classified under this heading demonstrate additional spcificity for 3',5'-cyclic IMP and CYCLIC GMP.
A cyclic nucleotide phosphodiesterase subfamily that is found predominantly in inflammatory cells and may play a role in the regulation of CELL-MEDIATED IMMUNITY. The enzyme family includes over twenty different variants that occur due to multiple ALTERNATIVE SPLICING of the mRNA of at least four different genes.
A cyclic nucleotide phosphodiesterase subfamily that is inhibited by the binding of CYCLIC GMP to an allosteric domain found on the enzyme and through phosphorylation by regulatory kinases such as PROTEIN KINASE A and PROTEIN KINASE B. The two members of this family are referred to as type 3A, and type 3B, and are each product of a distinct gene. In addition multiple enzyme variants of each subtype can be produced due to multiple alternative mRNA splicing.
A class of enzymes that catalyze the hydrolysis of one of the two ester bonds in a phosphodiester compound. EC 3.1.4.
Enzymes that catalyze the hydrolysis of cyclic GMP to yield guanosine-5'-phosphate.
A CALCIUM and CALMODULIN-dependent cyclic nucleotide phosphodiesterase subfamily. The three members of this family are referred to as type 1A, type 1B, and type 1C and are each product of a distinct gene. In addition, multiple enzyme variants of each subtype can be produced due to multiple alternative mRNA splicing. Although the type 1 enzymes are classified as 3',5'-cyclic-AMP phosphodiesterases (EC 3.1.4.17), some members of this class have additional specificity for CYCLIC GMP.
A cyclic nucleotide phosphodiesterase subfamily that is activated by the binding of CYCLIC GMP to an allosteric domain found on the enzyme. Multiple enzyme variants of this subtype can be produced due to multiple alternative mRNA splicing. The subfamily is expressed in a broad variety of tissues and may play a role in mediating cross-talk between CYCLIC GMP and CYCLIC CMP pathways. Although the type 2 enzymes are classified as 3',5'-cyclic-AMP phosphodiesterases (EC 3.1.4.17), members of this class have additional specificity for CYCLIC GMP.
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
Nucleoside-2',3'-cyclic phosphate nucleotidohydrolase. Enzymes that catalyze the hydrolysis of the 2'- or 3'- phosphate bonds of 2',3'-cyclic nucleotides. Also hydrolyzes nucleoside monophosphates. Includes EC 3.1.4.16 and EC 3.1.4.37. EC 3.1.4.-.
A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC GMP. It is found predominantly in vascular tissue and plays an important role in regulating VASCULAR SMOOTH MUSCLE contraction.
A phosphodiesterase 4 inhibitor with antidepressant properties.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
N-(1-Oxobutyl)-cyclic 3',5'-(hydrogen phosphate)-2'-butanoate guanosine. A derivative of cyclic GMP. It has a higher resistance to extracellular and intracellular phosphodiesterase than cyclic GMP.
A cyclic nucleotide phosphodiesterase subfamily that is highly specific for CYCLIC AMP. Several isoforms of the enzyme type exist, each with its own tissue localization. The isoforms are encoded by at least two genes and are a product of multiple alternative splicing of their mRNAs.
A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES
An enzyme that catalyzes the conversion of GTP to 3',5'-cyclic GMP and pyrophosphate. It also acts on ITP and dGTP. (From Enzyme Nomenclature, 1992) EC 4.6.1.2.
Compounds that specifically inhibit PHOSPHODIESTERASE 4.
Compounds that specifically inhibit PHOSPHODIESTERASE 3.
Enzymes that catalyze the cleavage of a phosphorus-oxygen bond by means other than hydrolysis or oxidation. EC 4.6.
A phosphoric diester hydrolase that removes 5'-nucleotides from the 3'-hydroxy termini of 3'-hydroxy-terminated OLIGONUCLEOTIDES. It has low activity towards POLYNUCLEOTIDES and the presence of 3'-phosphate terminus on the substrate may inhibit hydrolysis.
A group of cyclic GMP-dependent enzymes that catalyze the phosphorylation of SERINE or THREONINE residues of proteins.
A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed)
A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.
Inhibitor of phosphodiesterases.
A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase type 3 activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the inotropic potency of amrinone.
A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
Compounds that specifically inhibit PHOSPHODIESTERASE 5.
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.
The rate dynamics in chemical or physical systems.
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.
A powerful vasodilator used in emergencies to lower blood pressure or to improve cardiac function. It is also an indicator for free sulfhydryl groups in proteins.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
A group of indole-indoline dimers which are ALKALOIDS obtained from the VINCA genus of plants. They inhibit polymerization of TUBULIN into MICROTUBULES thus blocking spindle formation and arresting cells in METAPHASE. They are some of the most useful ANTINEOPLASTIC AGENTS.
A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
A guanine nucleotide containing one phosphate group esterified to the sugar moiety and found widely in nature.
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.
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.
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
A component of PHOSPHATIDYLCHOLINES or LECITHINS, in which the two hydroxy groups of GLYCEROL are esterified with fatty acids. (From Stedman, 26th ed) It counteracts the effects of urea on enzymes and other macromolecules.
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.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
The region of an enzyme that interacts with its substrate to cause the enzymatic reaction.
The portion of a retinal rod cell situated between the ROD INNER SEGMENT and the RETINAL PIGMENT EPITHELIUM. It contains a stack of photosensitive disk membranes laden with RHODOPSIN.
Purine bases found in body tissues and fluids and in some plants.
The process of cleaving a chemical compound by the addition of a molecule of water.
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.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
A group of enzymes within the class EC 3.6.1.- that catalyze the hydrolysis of diphosphate bonds, chiefly in nucleoside di- and triphosphates. They may liberate either a mono- or diphosphate. EC 3.6.1.-.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
That phase of a muscle twitch during which a muscle returns to a resting position.
Specialized cells that detect and transduce light. They are classified into two types based on their light reception structure, the ciliary photoreceptors and the rhabdomeric photoreceptors with MICROVILLI. Ciliary photoreceptor cells use OPSINS that activate a PHOSPHODIESTERASE phosphodiesterase cascade. Rhabdomeric photoreceptor cells use opsins that activate a PHOSPHOLIPASE C cascade.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
The relationship between the dose of an administered drug and the response of the organism to the drug.
The nonstriated involuntary muscle tissue of blood vessels.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
A structurally-diverse family of intracellular-signaling adaptor proteins that selectively tether specific protein kinase A subtypes to distinct subcellular sites. They play a role in focusing the PROTEIN KINASE A activity toward relevant substrates. Over fifty members of this family exist, most of which bind specifically to regulatory subunits of CYCLIC AMP-DEPENDENT PROTEIN KINASE TYPE II such as CAMP PROTEIN KINASE RIIALPHA or CAMP PROTEIN KINASE RIIBETA.
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.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
Drugs used to cause dilation of the blood vessels.
Cell surface proteins that bind ATRIAL NATRIURETIC FACTOR with high affinity and trigger intracellular changes influencing the behavior of cells. They contain intrinsic guanylyl cyclase activity.
A genus of protozoa, formerly also considered a fungus. Its natural habitat is decaying forest leaves, where it feeds on bacteria. D. discoideum is the best-known species and is widely used in biomedical research.
The portion of the descending aorta proceeding from the arch of the aorta and extending to the DIAPHRAGM, eventually connecting to the ABDOMINAL AORTA.
A sulfur-containing alkyl thionitrite that is one of the NITRIC OXIDE DONORS.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in enzyme synthesis.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
An essential amino acid that is physiologically active in the L-form.
Components of a cell produced by various separation techniques which, though they disrupt the delicate anatomy of a cell, preserve the structure and physiology of its functioning constituents for biochemical and ultrastructural analysis. (From Alberts et al., Molecular Biology of the Cell, 2d ed, p163)
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles.
A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.
Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.
A morpholinyl sydnone imine ethyl ester, having a nitrogen in place of the keto oxygen. It acts as NITRIC OXIDE DONORS and is a vasodilator that has been used in ANGINA PECTORIS.
An enzyme that catalyzes the reversible oxidation of inosine 5'-phosphate (IMP) to guanosine 5'-phosphate (GMP) in the presence of AMMONIA and NADP+. This enzyme was formerly classified as EC 1.6.6.8.
A diverse group of agents, with unique chemical structures and biochemical requirements, which generate NITRIC OXIDE. These compounds have been used in the treatment of cardiovascular diseases and the management of acute myocardial infarction, acute and chronic congestive heart failure, and surgical control of blood pressure. (Adv Pharmacol 1995;34:361-81)
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
An NADPH-dependent enzyme that catalyzes the conversion of L-ARGININE and OXYGEN to produce CITRULLINE and NITRIC OXIDE.
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
A species of the family Ranidae (true frogs). The only anuran properly referred to by the common name "bullfrog", it is the largest native anuran in North America.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)
Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.
A cyclic GMP-dependent protein kinase subtype that is expressed in SMOOTH MUSCLE tissues and plays a role in regulation of smooth muscle contraction. Two isoforms, PKGIalpha and PKGIbeta, of the type I protein kinase exist due to alternative splicing of its mRNA.
Quinolines substituted in any position by one or more amino groups.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
A group of compounds which consist of a nucleotide molecule to which an additional nucleoside is attached through the phosphate molecule(s). The nucleotide can contain any number of phosphates.
An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6)
Peptides that regulate the WATER-ELECTROLYTE BALANCE in the body, also known as natriuretic peptide hormones. Several have been sequenced (ATRIAL NATRIURETIC FACTOR; BRAIN NATRIURETIC PEPTIDE; C-TYPE NATRIURETIC PEPTIDE).
The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
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.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
Established cell cultures that have the potential to propagate indefinitely.
A competitive inhibitor of nitric oxide synthetase.
Proteins found in any species of bacterium.
A PEPTIDE of 22 amino acids, derived mainly from cells of VASCULAR ENDOTHELIUM. It is also found in the BRAIN, major endocrine glands, and other tissues. It shares structural homology with ATRIAL NATRIURETIC FACTOR. It has vasorelaxant activity thus is important in the regulation of vascular tone and blood flow. Several high molecular weight forms containing the 22 amino acids have been identified.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A sulfur-containing alkyl thionitrite that is one of the NITRIC OXIDE DONORS.
Separation technique in which the stationary phase consists of ion exchange resins. The resins contain loosely held small ions that easily exchange places with other small ions of like charge present in solutions washed over the resins.
Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.
Contractile activity of the MYOCARDIUM.
Striated muscle cells found in the heart. They are derived from cardiac myoblasts (MYOBLASTS, CARDIAC).
The sum of the weight of all the atoms in a molecule.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Elements of limited time intervals, contributing to particular results or situations.
A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.
A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309)
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A type of FLUORESCENCE SPECTROSCOPY using two FLUORESCENT DYES with overlapping emission and absorption spectra, which is used to indicate proximity of labeled molecules. This technique is useful for studying interactions of molecules and PROTEIN FOLDING.
The conformation, properties, reaction processes, and the properties of the reactions of carbon compounds.
One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.
A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.
The lower right and left chambers of the heart. The right ventricle pumps venous BLOOD into the LUNGS and the left ventricle pumps oxygenated blood into the systemic arterial circulation.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Chromatography on non-ionic gels without regard to the mechanism of solute discrimination.
The main trunk of the systemic arteries.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A species of the true toads, Bufonidae, becoming fairly common in the southern United States and almost pantropical. The secretions from the skin glands of this species are very toxic to animals.
Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
Proteins prepared by recombinant DNA technology.
That portion of the electromagnetic spectrum in the visible, ultraviolet, and infrared range.
Proteins obtained from ESCHERICHIA COLI.
A group of hydrolases which catalyze the hydrolysis of monophosphoric esters with the production of one mole of orthophosphate. EC 3.1.3.
Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.
A sequence of amino acids in a polypeptide or of nucleotides in DNA or RNA that is similar across multiple species. A known set of conserved sequences is represented by a CONSENSUS SEQUENCE. AMINO ACID MOTIFS are often composed of conserved sequences.
Inosine 5'-(tetrahydrogen triphosphate). An inosine nucleotide containing three phosphate groups esterified to the sugar moiety. Synonym: IRPPP.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
Encrustations, formed from microbes (bacteria, algae, fungi, plankton, or protozoa) embedding in extracellular polymers, that adhere to surfaces such as teeth (DENTAL DEPOSITS); PROSTHESES AND IMPLANTS; and catheters. Biofilms are prevented from forming by treating surfaces with DENTIFRICES; DISINFECTANTS; ANTI-INFECTIVE AGENTS; and antifouling agents.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
A heterotrimeric GTP-binding protein that mediates the light activation signal from photolyzed rhodopsin to cyclic GMP phosphodiesterase and is pivotal in the visual excitation process. Activation of rhodopsin on the outer membrane of rod and cone cells causes GTP to bind to transducin followed by dissociation of the alpha subunit-GTP complex from the beta/gamma subunits of transducin. The alpha subunit-GTP complex activates the cyclic GMP phosphodiesterase which catalyzes the hydrolysis of cyclic GMP to 5'-GMP. This leads to closure of the sodium and calcium channels and therefore hyperpolarization of the rod cells. EC 3.6.1.-.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood.
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
Long-lasting voltage-gated CALCIUM CHANNELS found in both excitable and nonexcitable tissue. They are responsible for normal myocardial and vascular smooth muscle contractility. Five subunits (alpha-1, alpha-2, beta, gamma, and delta) make up the L-type channel. The alpha-1 subunit is the binding site for calcium-based antagonists. Dihydropyridine-based calcium antagonists are used as markers for these binding sites.
A class of enzymes that catalyze oxidation-reduction reactions of amino acids.
A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352)
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
A compound formed by the combination of hemoglobin and oxygen. It is a complex in which the oxygen is bound directly to the iron without causing a change from the ferrous to the ferric state.
A group of compounds that are derivatives of beta-methylacetylcholine (methacholine).
The external reproductive organ of males. It is composed of a mass of erectile tissue enclosed in three cylindrical fibrous compartments. Two of the three compartments, the corpus cavernosa, are placed side-by-side along the upper part of the organ. The third compartment below, the corpus spongiosum, houses the urethra.
Mixtures of closely related hypotensive alkaloids from Veratrum album (Liliaceae). They have been used in the treatment of hypertension but have largely been replaced by drugs with fewer adverse effects.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
... cyclic-AMP and -GMP phosphodiesterase 11A is an enzyme that in humans is encoded by the PDE11A gene. The 3',5'-cyclic ... Yuasa K, Ohgaru T, Asahina M, Omori K (2001). "Identification of rat cyclic nucleotide phosphodiesterase 11A (PDE11A): ... Beavo JA, Conti M, Heaslip RJ (1994). "Multiple cyclic nucleotide phosphodiesterases". Mol. Pharmacol. 46 (3): 399-405. PMID ... cyclic nucleotide phosphodiesterase 11A: localization in human tissues". Int. J. Impot. Res. 17 (4): 320-5. doi:10.1038/sj.ijir ...
... cyclic di-GMP). Degradation of cyclic di-GMP to guanosine monophosphate (GMP) is catalyzed by a phosphodiesterase (PDE). ... Cyclic di-GMP binds to interface between the DGC and D2 domains stabilizing the open structure and preventing catalysis. Strong ... Often, GGDEF domains with DGC activity are found in the same proteins as c-di-GMP-specific phosphodiesterase (PDE) EAL (Glu-Ala ... Jenal U, Malone J (2006). "Mechanisms of cyclic-di-GMP signaling in bacteria". Annual Review of Genetics. 40: 385-407. doi: ...
... cyclic-GMP phosphodiesterase MeSH D08.811.277.352.640.150 - 3',5'-cyclic-nucleotide phosphodiesterase MeSH D08.811.277.352. ... cyclic gmp-dependent protein kinases MeSH D08.811.913.696.620.682.700.150.575 - protamine kinase MeSH D08.811.913.696.620.682. ... cyclic-nucleotide phosphodiesterases MeSH D08.811.277.352.640.295 - glycerophosphoinositol inositolphosphodiesterase MeSH ... cyclic nucleotide-regulated protein kinases MeSH D08.811.913.696.620.682.700.150.125 - cyclic amp-dependent protein kinases ...
Numerous cyclic nucleotide phosphodiesterases (PDE) can degrade cGMP by hydrolyzing cGMP into 5'-GMP. PDE 5, -6 and -9 are cGMP ... Cyclic guanosine monophosphate (cGMP) is a cyclic nucleotide derived from guanosine triphosphate (GTP). cGMP acts as a second ... cyclic monophosphate (8-Br-cGMP) Francis SH, Corbin JD (August 1999). "Cyclic nucleotide-dependent protein kinases: ... Phosphodiesterase inhibitors prevent the degradation of cGMP, thereby enhancing and/or prolonging its effects. For example, ...
1975). "Biologic regulation through opposing influences of cyclic GMP and cyclic AMP: the Yin Yang hypothesis". Adv Cyclic ... June 1997). "cGMP-stimulated cyclic nucleotide phosphodiesterase regulates the basal calcium current in human atrial myocytes ... Bender AT, Beavo JA (September 2006). "Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use". Pharmacol. ... The PDE2 (phosphodiesterase 2) enzyme is one of 21 different phosphodiesterases (PDE) found in mammals. These different PDEs ...
... phosphate phosphodiesterase, cyclic GMP phosphodiesterase, cyclic 3′,5′-GMP phosphodiesterase, cyclic guanosine 3′,5′- ... Cyclic AMP and cyclic GMP phosphodiesterase". Biochim. Biophys. Acta. 334: 368-377. doi:10.1016/0005-2744(74)90180-6. Portal: ... cyclic-GMP phosphodiesterase (EC 3.1.4.35) catalyzes the reaction guanosine 3′,5′-cyclic phosphate + H2O ⇌ {\displaystyle \ ... phosphate phosphodiesterase, cGMP phosphodiesterase, cGMP-PDE, and cyclic guanosine 3′,5′-phosphate phosphodiesterase. As of ...
... a Specific Inhibitor of Cyclic GMP Phosphodiesterase, on Human Platelet Aggregation". The Journal of Pharmacology and ... Aubin, C; Webster, L; Rebeyka, IM; Ross, DB; Light, PE; Dyck, JR; Michelakis, ED (17 July 2007). "Phosphodiesterase Type 5 is ... MY-5445 is a relatively specific phosphodiesterase 5 inhibitor. Vatalanib - a structurally related angiogenesis inhibitor ... Phosphodiesterase inhibitors, Phthalazines, Chloroarenes, All stub articles, Organic compound stubs). ...
In mammals, GAF domains are found in five members of the cyclic nucleotide phosphodiesterase superfamily: PDE2, PDE5, and PDE6 ... a ubiquitous signaling motif and a new class of cyclic GMP receptor". The EMBO Journal. 19 (20): 5288-99. doi:10.1093/emboj/ ... The GAF domain is named after some of the proteins it is found in: cGMP-specific phosphodiesterases, adenylyl cyclases and FhlA ... "The two GAF domains in phosphodiesterase 2A have distinct roles in dimerization and in cGMP binding". Proceedings of the ...
The two most well-studied cyclic nucleotides are cyclic AMP (cAMP) and cyclic GMP (cGMP), while cyclic CMP (cCMP) and cyclic ... cAMP's role in this process terminates upon hydrolysis to AMP by phosphodiesterase. Cyclic nucleotides are well-suited to act ... Lincoln, TM; Cornwell TL (1991). "Towards an understanding of the mechanism of action of cyclic AMP and cyclic GMP in smooth ... As can be seen in the cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) images, the 'cyclic' ...
Cyclic GMP-AMP (cGAMP) is a cyclic dinucleotide (CDN) and the first to be found in metazoans. Other CDNs (c-di-GMP and c-di-AMP ... phosphodiesterases. Other advantages of the unique 2'-5' linkage may be that cGAMP is able to bind multiple allelic variants of ... Upon binding DNA, the protein cyclic GMP-AMP Synthase (cGAS) triggers reaction of GTP and ATP to form cyclic GMP-AMP (cGAMP). ... specifically by the cyclic-GMP-AMP synthase (cGAS). Upon DNA recognition, cGAS dimerizes and stimulates the formation of cyclic ...
Linari M, Hanzal-Bayer M, Becker J (Sep 1999). "The delta subunit of rod specific cyclic GMP phosphodiesterase, PDE delta, ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... cyclic phosphodiesterase subunit delta is an enzyme that in humans is encoded by the PDE6D gene. PDE6D was originally ...
Nitric oxide and cyclic GMP in cell signaling and drug development". The New England Journal of Medicine. 355 (19): 2003-11. ... Phosphodiesterase type 5 (PDE5), which is abundant in the pulmonary tissue, hydrolyzes the cyclic bond of cGMP. Consequently, ... s The U.S. FDA approved sildenafil, a selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5), for the treatment ... Levels of cAMP (which mediates most of the biological effects of prostacyclin) are reduced by phosphodiesterases 3 and 4. The ...
Organization of the gene for the beta-subunit of human photoreceptor cyclic GMP phosphodiesterase]". Bioorganicheskaia Khimiia ... "In vivo differential prenylation of retinal cyclic GMP phosphodiesterase catalytic subunits". The Journal of Biological ... "Enzymic basis for cyclic GMP accumulation in degenerative photoreceptor cells of mouse retina". Journal of Cyclic Nucleotide ... cyclic phosphodiesterase subunit beta is the beta subunit of the protein complex PDE6 that is encoded by the PDE6B gene. PDE6 ...
... c-di-GMP-specific phosphodiesterase, c-di-GMP phosphodiesterase, phosphodiesterase, phosphodiesterase A1, PDEA1, VieA) is an ... Cyclic-guanylate-specific phosphodiesterase (EC 3.1.4.52, cyclic bis(3′→5')diguanylate phosphodiesterase, ... "Identification and characterization of a cyclic di-GMP-specific phosphodiesterase and its allosteric control by GTP". J. Biol. ... Cyclic-guanylate-specific+phosphodiesterase at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: ...
Kroll S, Phillips WJ, Cerione RA (March 1989). "The regulation of the cyclic GMP phosphodiesterase by the GDP-bound form of the ... cyclic-nucleotide phosphodiesterases (EC 3.1.4.17) are a family of phosphodiesterases. Generally, these enzymes hydrolyze a ... monophosphate phosphodiesterase (cyclic CMP), cyclic 3′,5-nucleotide monophosphate phosphodiesterase, nucleoside 3′,5′-cyclic ... cyclic-nucleotide phosphodiesterases in rod cells are oligomeric, made up of two heavy catalytic subunits, α (90 kDa) and β (85 ...
"Localization of the human gene for the type I cyclic GMP-dependent protein kinase to chromosome 10". Cytogenetics and Cell ... and kinase-directed regulation of phosphorylation of a cGMP-binding phosphodiesterase by cGMP". The Journal of Biological ... 27 (3 Pt 2): 552-7. doi:10.1161/01.hyp.27.3.552. PMID 8613202. Salih E, Zhou HY, Glimcher MJ (Jul 1996). "Phosphorylation of ... 96 (5): 2467-72. Bibcode:1999PNAS...96.2467E. doi:10.1073/pnas.96.5.2467. PMC 26808. PMID 10051666. Wang X, Bruderer S, Rafi Z ...
... for instance a bond in a molecule of cyclic AMP or cyclic GMP. An enzyme that plays an important role in the repair of ... Phosphodiesterase Phosphodiesterase inhibitor DNA replication, DNA, ATP Teichoic acid, DNase I PDE5 Nick (DNA) "Phosphodiester ... A phosphodiesterase is an enzyme that catalyzes the hydrolysis of phosphodiester bonds, ... Hydrolysis of phosphodiester bonds is catalyzed by phosphodiesterases, which are involved in repairing DNA sequences. The ...
... inhibition with BAY 73-6691 increases corpus cavernosum relaxations mediated by nitric oxide-cyclic GMP pathway in mice". ... Effects of phosphodiesterase 10 inhibition on striatal cyclic AMP and peripheral physiology in rats; An Torremans, Abdellah ... 2001). "Cyclic nucleotide phosphodiesterases". The Journal of Allergy and Clinical Immunology. 108 (5): 671-80. doi:10.1067/mai ... A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), ...
... cyclic-GMP phosphodiesterase. *Protein kinase G. *G alpha subunit Gα *GNAO1 ... Gαs activates the cAMP-dependent pathway by stimulating the production of cyclic AMP (cAMP) from ATP. This is accomplished by ... An example is adenylate cyclase, which produces the second messenger cyclic AMP.[9] For this discovery, they won the 1994 Nobel ... 0-8053-6624-5. .. *^ Neves SR, Ram PT, Iyengar R (May 2002). "G protein pathways". Science. 296 (5573): 1636-9. Bibcode:2002Sci ...
... cyclic-GMP-forming)) is a lyase enzyme that converts guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP) and ... Once formed, cGMP can be degraded by phosphodiesterases, which themselves are under different forms of regulation, depending on ... cyclic GMP + diphosphate It is often part of the G protein signaling cascade that is activated by low intracellular calcium ... Adenylyl cyclase Cyclic guanosine monophosphate Guanylyl cyclase activator (protein) Martin, Emil; Berka, Vladimir; Tsai, Ah‐ ...
... protects cyclic guanosine monophosphate (cGMP) from degradation by cGMP-specific phosphodiesterase type 5 (PDE5) in ... Phosphodiesterase inhibitors (e.g., sildenafil) can also improve [Raynaud's phenomenon] symptoms and ulcer healing Nieto ... Laties AM (January 2009). "Vision disorders and phosphodiesterase type 5 inhibitors: a review of the evidence to date". Drug ... Sildenafil acts by blocking phosphodiesterase 5 (PDE5), an enzyme that promotes breakdown of cGMP, which regulates blood flow ...
Cyclic GMP binds to the cGMP-dependent protein kinase (PKG1) which phosphorylates several proteins that results in decreased ... Lugnier, C. (2006). "Cyclic nucleotide phosphodiesterase (PDE) superfamily: A new target for the development of specific ... Their function is to degrade intracellular second messengers such as cyclic adenine monophosphate (cAMP) and cyclic guanosine ... GMP is an inactive molecule with no second messenger activity. Phosphorylation of a single serine by PKG1 and the allosteric ...
... cyclic phosphodiesterase subunit alpha is an enzyme that in humans is encoded by the PDE6A gene. PDE6A encodes the cyclic-GMP ( ... cGMP) specific phosphodiesterase 6A alpha subunit, expressed in cells of the retinal rod outer segment. The phosphodiesterase 6 ... "Cryo-EM structure of phosphodiesterase 6 reveals insights into the allosteric regulation of type I phosphodiesterases". Science ... "Entrez Gene: PDE6A phosphodiesterase 6A, cGMP-specific, rod, alpha". Gulati S, Palczewski K, Engel A, Stahlberg H, Kovacik L ( ...
... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... interacts with the delta subunit of rod cyclic GMP phosphodiesterase". Proceedings of the National Academy of Sciences of the ... 38 (13): 2750-5. PMID 9418727. Yan D, Swain PK, Breuer D, Tucker RM, Wu W, Fujita R, Rehemtulla A, Burke D, Swaroop A (Jul 1998 ... 5 (7): 1035-41. doi:10.1093/hmg/5.7.1035. PMID 8817343. Murga-Zamalloa CA, Atkins SJ, Peranen J, Swaroop A, Khanna H (Sep 2010 ...
... cyclic-GMP phosphodiesterase EC 3.1.4.36: Now with EC 3.1.4.43 EC 3.1.4.37: 2′,3′-cyclic-nucleotide 3'-phosphodiesterase EC 3.1 ... phosphodiesterase * EC 3.1.4.59: cyclic-di-AMP phosphodiesterase * EC 3.1.4.60: pApA phosphodiesterase * EC 3.1.4.61: cyclic 2, ... CMP-N-acylneuraminate phosphodiesterase EC 3.1.4.41: sphingomyelin phosphodiesterase D EC 3.1.4.42: glycerol-1,2-cyclic- ... cyclic phosphate phosphodiesterase EC 3.1.4.57: phosphoribosyl 1,2-cyclic phosphate 1,2-diphosphodiesterase * EC 3.1.4.58: RNA ...
Linari M, Hanzal-Bayer M, Becker J (1999). "The delta subunit of rod specific cyclic GMP phosphodiesterase, PDE delta, ... 377 (6547 Suppl): 3-174. PMID 7566098. Andersson B, Wentland MA, Ricafrente JY, Liu W, Gibbs RA (1996). "A "double adaptor" ... 17 (5): 2476-87. doi:10.1091/mbc.E05-10-0929. PMC 1446103. PMID 16525022. v t e (Articles with short description, Short ... ADP-ribosylation factor-like protein 3 is a protein that in humans is encoded by the ARL3 gene. ADP-ribosylation factor-like 3 ...
"Physical and genetic localization of the gamma subunit of the cyclic GMP phosphodiesterase on the long arm of chromosome 17 ( ... The organization of the gamma-subunit gene of human photoreceptor cyclic GMP phosphodiesterase]" [The organization of the gamma ... of patients with retinitis pigmentosa using a cloned cDNA probe for the human gamma subunit of cyclic GMP phosphodiesterase". ... gene of human photoreceptor cyclic GMP phosphodiesterase]. Doklady Akademii Nauk SSSR. 315 (1): 229-31. PMID 1965799. Tuteja N ...
... but an inhibition of the enzyme phosphodiesterase causing elevation of cyclic AMP and cyclic GMP[clarification needed] levels ... Papaverine has also been demonstrated to be a selective phosphodiesterase inhibitor for the PDE10A subtype found mainly in the ... August 2006). "Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis". ... Hebb AL, Robertson HA, Denovan-Wright EM (May 2008). "Phosphodiesterase 10A inhibition is associated with locomotor and ...
... cyclic guanosine monophosphate (cGMP), guanosine pentaphosphate ((p)ppGpp), and cyclic di-GMP (c-di-GMP). c-di-AMP is a ... Phosphodiesterase (PDE) enzymes degrade cyclic di-AMP to the linear molecule 5'-pApA (phosphadenylyl adenosine). 5'-pApA is ... Cyclic di-GMP Dey B, Dey RJ, Cheung LS, Pokkali S, Guo H, Lee JH, Bishai WR (April 2015). "A bacterial cyclic dinucleotide ... December 2012). "The helicase DDX41 recognizes the bacterial secondary messengers cyclic di-GMP and cyclic di-AMP to activate a ...
... which stimulates the synthesis of cyclic guanosine monophosphate (more commonly known as cyclic GMP or cGMP) in smooth muscle ... The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. Tadalafil (and ... Penedones A, Alves C, Batel Marques F (2020). "Risk of nonarteritic ischaemic optic neuropathy with phosphodiesterase type 5 ... In 1993, the Bothell, Washington, biotechnology company ICOS Corporation began studying compound IC351, a phosphodiesterase ...
July 5 - Dolly the sheep, the first mammal to be successfully cloned from an adult cell, is born at The Roslin Institute in ... October 3 - Reinhard Genzel and Andrea Ghez demonstrate the existence of a supermassive compact object at the centre of our ... April 3 - Jennifer Ringley becomes an early practitioner of lifecasting (video stream), from her dorm room at Dickinson College ... 4 (3): 389-398. doi:10.1534/g3.113.008995. PMC 3962479. PMID 24374639. Hofmann, S.; Ninov, V.; Heßberger, F. P.; Armbruster, P ...
Cyclic GMP possibly opens cyclic nucleotide-gated (CNG) K+-selective channels, thereby causing hyperpolarization of the ... The cGMP signal is terminated by the hydrolysis of cGMP through phosphodiesterase (PDE) activity and inactivation of GC. On ... Yoshida, M., Inaba, K., Ishida, K. and Morisawa, M. (1994) Calcium and cyclic AMP mediate sperm activation, but Ca2+ alone ... The consequential hyperpolarization activates hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels. The ...
... inhibition with BAY 73-6691 increases corpus cavernosum relaxations mediated by nitric oxide-cyclic GMP pathway in mice". ... A phosphodiesterase (PDE) is an enzyme that breaks a phosphodiester bond. Usually, phosphodiesterase refers to cyclic ... "Ontogenetic development of a phosphodiesterase activator and the multiple forms of cyclic AMP phosphodiesterase of rat brain". ... "Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase". Advances in Cyclic ...
... which changes the conformation of the opsin GPCR leading to signal transduction cascades which causes closure of cyclic GMP- ... and thus halts the action of phosphodiesterase, stopping the transformation of cGMP to GMP. This deactivation step of the ... The alpha subunit-GTP complex activates phosphodiesterase, also known as PDE6. It binds to one of two regulatory subunits of ... PDE hydrolyzes cGMP, forming GMP. This lowers the intracellular concentration of cGMP and therefore the sodium channels close. ...
"Cyclic GMP from the surrounding somatic cells regulates cyclic AMP and meiosis in the mouse oocyte". Development. 136 (11): ... and are regulated by the phosphodiesterase (PDE). This pathway can be triggered via two mechanisms: physiological stimulus ( ... Vaccari, S; Weeks JL, 2nd (September 2009). Hsieh, M; Menniti, FS; Conti, M. "Cyclic GMP signaling is involved in the ... Then, it converts adenosine triphosphate into cyclic AMP, which activates Protein kinase A. PKA leads to protein tyrosine ...
Unstimulated (in the dark), cyclic-nucleotide gated channels in the outer segment are open because cyclic GMP (cGMP) is bound ... Each transducin then activates the enzyme cGMP-specific phosphodiesterase (PDE). PDE then catalyzes the hydrolysis of cGMP to 5 ... GMP via PDE), resulting in the closure of cyclic nucleotide-gated Na+ ion channels located in the photoreceptor outer segment ... In the dark, cells have a relatively high concentration of cyclic guanosine 3'-5' monophosphate (cGMP), which opens cGMP-gated ...
... and cyclic GMP (cGMP) levels fall in vascular smooth muscle. This impairs relaxation in the vasculature and is a part of the ... Amrinone, also known as inamrinone, and sold as Inocor, is a pyridine phosphodiesterase 3 inhibitor. It is a drug that may ... Acts by inhibiting the breakdown of both cAMP and cGMP by the phosphodiesterase (PDE3) enzyme. There is a long-standing ... A loss in sensitivity to phosphodiesterase 3 inhibitors, including amrinone, has been observed in end stage heart failure in ...
Kroll, S.; Phillips, W. J.; Cerione, R. A. (1989). "The regulation of the cyclic GMP phosphodiesterase by the GDP-bound form of ... cyclic GMP Phosphodiesterase. The Tα subunit of transducin contains three functional domains: one for rhodopsin/Tβγ interaction ... Transducin activates phosphodiesterase, which results in the breakdown of cyclic guanosine monophosphate (cGMP). The intensity ... Phosphodiesterase hydrolyzes cGMP to 5'-GMP. Decrease in cGMP concentration leads to decreased opening of cation channels and ...
Differential Activation and Inhibition of the Multiple Forms of Cyclic Nucleotide Phosphodiesterase. Advances in Cyclic ... on cyclic GMP in the smooth muscle cells lining the blood vessels supplying various tissues. These drugs dilate the corpora ... Fertel R, Weiss B (July 1976). "Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung". ... Weiss B, Hait WN (1977). "Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents". Annual ...
Sadhu K, Hensley K, Florio VA, Wolda SL (1999). "Differential expression of the cyclic GMP-stimulated phosphodiesterase PDE2A ... cyclic phosphodiesterase is an enzyme that in humans is encoded by the PDE2A gene. GRCh38: Ensembl release 89: ENSG00000186642 ... cyclic nucleotide phosphodiesterase". Gene. 191 (1): 89-95. doi:10.1016/S0378-1119(97)00046-2. PMID 9210593. "Entrez Gene: ... PDE2A phosphodiesterase 2A, cGMP-stimulated". Witzenrath M, Gutbier B, Schmeck B, et al. (2005). "Phosphodiesterase 2 ...
... reducing cyclic GMP degradation. Endothelin receptor antagonist, another class of drugs used in PAH Riociguat FDA Professional ... Nitrates and phosphodiesterase inhibitors (including PDE5 inhibitors) increase the hypotensive (blood pressure lowering) effect ... NO binds to soluble guanylate cyclase (sGC) and mediates the synthesis of the secondary messenger cyclic guanosine ... Therefore, the concomitant use of riociguat with phosphodiesterase-5 inhibitors is contraindicated. Cinaciguat, a sGC activator ...
"Intercellular signaling via cyclic GMP diffusion through gap junctions restarts meiosis in mouse ovarian follicles". ... produced by these granulosa cells rapidly diffuse into the oocyte through gap junctions and inhibits cAMP-phosphodiesterase 3A ... 10 (1): 1-5. doi:10.1093/molehr/gah009. ISSN 1360-9947. PMID 14665700. Mehlmann, Lisa M.; Jones, Teresa L. Z.; Jaffe, Laurinda ... 17 (3): 415-20. doi:10.4103/1008-682X.148077. ISSN 1008-682X. PMC 4430939. PMID 25652637. Liang, Cheng-Guang; Su, You-Qiang; ...
... phosphate phosphodiesterase, cyclic GMP phosphodiesterase, cyclic 3′,5′-GMP phosphodiesterase, cyclic guanosine 3′,5′- ... Cyclic AMP and cyclic GMP phosphodiesterase". Biochim. Biophys. Acta. 334: 368-377. doi:10.1016/0005-2744(74)90180-6. Portal: ... cyclic-GMP phosphodiesterase (EC 3.1.4.35) catalyzes the reaction guanosine 3′,5′-cyclic phosphate + H2O ⇌ {\displaystyle \ ... phosphate phosphodiesterase, cGMP phosphodiesterase, cGMP-PDE, and cyclic guanosine 3′,5′-phosphate phosphodiesterase. As of ...
... phosphate phosphodiesterase;. cyclic GMP phosphodiesterase;. cyclic 3,5-GMP phosphodiesterase;. cyclic guanosine 3,5- ... monophosphate phosphodiesterase;. cyclic guanosine 3,5-phosphate phosphodiesterase;. cGMP phosphodiesterase;. cGMP-PDE. ... Pathway (4) KEGG PATHWAY (4) Chemical substance (3) KEGG COMPOUND (3) Chemical reaction (2) KEGG REACTION (1) KEGG RCLASS (1) ... rod cGMP-specific 3,5-cyclic phosphodiesterase subunit beta. K13757 cone cGMP-specific 3,5-cyclic phosphodiesterase subunit ...
Römling, U.; Galperin, M.Y.; Gomelsky, M. Cyclic di-GMP: The First 25 Years of a Universal Bacterial Second Messenger. ... Analysis of Pseudomonas aeruginosa diguanylate cyclases and phosphodiesterases reveals a role for bis-(3-5)-cyclic-GMP in ... c-di-GMP metabolism. W-2 (Wrinkly). PN-1-21. 4151496, SNV, none. 5069263, SNV, Gly90→Asp. wspA (PA3708). pilA (PA4525). c-di- ... c-di-GMP metabolism. 1, Series-Line-No. of transfers correspond to Figure 1b; 2, Single nucleotide variants; 3, Not detected ...
Nucleotides by Structure Important Structure Motifs 3,5-Cyclic Nucleotides ... Ahumada et al. (2003) Signaling of rat Frizzled-2 through phosphodiesterase and cyclic GMP. Science 298 (5600):2006.. Rybalkin ... Park et al. (2002) Nitric Oxide-Cyclic GMP Signaling Pathway in the Regulation of Rabbit Clitoral Cavernosum Tone. Exp. Biol. ... 2003 Feb 5 [epub ahead of print].. Leckie et al. (2003) The NO pathway acts late during the fertilization response in sea ...
... cyclic di‐guanosine monophosphate (c‐di‐GMP) determines when Streptomyces initiate sporulation. c‐di‐GMP signals are integrated ... However, functions of the development‐specific diguanylate cyclases (DGCs) CdgB and CdgC, and the c‐di‐GMP phosphodiesterases ( ... Despite having an equivalent GGDEF‐EAL domain arrangement, RmdA cleaves c‐di‐GMP to GMP and exhibits residual DGC activity. We ... Transcriptome analysis of ∆cdgB, ∆cdgC, ∆rmdA, and ∆rmdB strains revealed that the c‐di‐GMP specified by these enzymes has a ...
As high levels of c-di-GMP are associated with the biofilm lifestyle, c-di-GMP hydrolysing phosphodiesterases (PDEs) have been ... The bacterial second messenger cyclic di-3,5-guanosine monophosphate (c-di-GMP) is a key regulator of bacterial motility and ... As high levels of c-di-GMP are associated with the biofilm lifestyle, c-di-GMP hydrolysing phosphodiesterases (PDEs) have been ... The bacterial second messenger cyclic di-3,5-guanosine monophosphate (c-di-GMP) is a key regulator of bacterial motility and ...
Background: KMUP-1 is a xanthine derivative with inhibitory activities on the phosphodiesterase (PDE) 3,4 and 5 isoenzymes to ... suppress the degradation of cyclic AMP and cyclic GMP. However, whether KMUP-1 has any effect on osteoblast differentiation is ... Andries Bickerweg 5. 2517 JP The Hague. Netherlands. +31 (0) 70 30 21 970. [email protected] ...
Johner, A., Kunz, S., Linder, M., Shakur, Y. and Seebeck, T. Cyclic nucleotide specific phosphodiesterases of Leishmania major ... Characterization of cyclic nucleotide phosphodiesterase isoforms associated to isolated cardiac nuclei. Biochim. Biophys. Acta ... Bader, S., Kortholt, A., Snippe, H. and Van Haastert, P.J. DdPDE4, a novel cAMP-specific phosphodiesterase at the surface of ... Alonso, G.D., Schoijet, A.C., Torres, H.N. and Flawiá, M.M. TcPDE4, a novel membrane-associated cAMP-specific phosphodiesterase ...
An assessment of the role of the inhibitory gamma subunit of the retinal cyclic GMP phosphodiesterase and its effect on the p42 ... The inhibitory gamma subunit of the type 6 retinal cyclic guanosine monophosphate phosphodiesterase is a novel intermediate ... The identification of the inhibitory gamma-subunits of the type 6 retinal cyclic guanosine monophosphate phosphodiesterase in ... Ribozyme knockdown of the gamma-subunit of rod cGMP phosphodiesterase alters the ERG and retinal morphology in wild-type mice. ...
... cyclic-GMP phosphodiesterase. *Protein kinase G. *G alpha subunit Gα *GNAO1 ... Gαs activates the cAMP-dependent pathway by stimulating the production of cyclic AMP (cAMP) from ATP. This is accomplished by ... An example is adenylate cyclase, which produces the second messenger cyclic AMP.[9] For this discovery, they won the 1994 Nobel ... 0-8053-6624-5. .. *^ Neves SR, Ram PT, Iyengar R (May 2002). "G protein pathways". Science. 296 (5573): 1636-9. Bibcode:2002Sci ...
Cyclic GMP-mediated memory enhancement in the object recognition test by inhibitors of phosphodiesterase-2 in mice. ... Gordon Research Conference on Cyclic Nucleotide Phosphodiesterases (2010). *Vice Chair, Gordon Research Conference on Cyclic ... Ontogeny of rolipram-sensitive, low-K(m), cyclic AMP-specific phosphodiesterase in rat brain. Brain Res Dev Brain Res. 1999; ... Inhibition of cyclic AMP phosphodiesterase (PDE4) reverses memory deficits associated with NMDA receptor antagonism. ...
... cGMP-specific phosphodiesterase, a member of the cyclic nucleotide phosphodiesterase family. This phosphodiesterase ... GMP. It is involved in the regulation of intracellular concentrations of cyclic nucleotides and is important for smooth muscle ... This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5-GMP (PubMed:9714779, PubMed:15489334). Specifically ... Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. ...
... cyclic-GMP phosphodiesterase) inhibitor and a vasodilator agent. It is a pyrazinopyridoindole and a member of benzodioxoles. ... It is a phosphodiesterase 5 (PDE5) inhibitor. Tadalafils distinguishing pharmacologic feature is its longer half-life (17.5 ... Tadalafil selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase- (PDE-5)-mediated ... A phosphodiesterase V inhibitor inhibitor, currently marketed in pill form for treating erectile dysfunction under the name ...
... of an enzyme called cone-specific phosphodiesterase. Learn about this gene and related health conditions. ... cyclic phosphodiesterase subunit gamma. Additional Information & Resources. Tests Listed in the Genetic Testing Registry. * ... GMP, in cones. This conversion causes certain channels on the cell membrane to close. The closing of these channels triggers ... Cone-specific phosphodiesterase carries out one of the reactions in this process. Specifically, the enzyme converts a molecule ...
... cyclic phosphodiesterase,Cyclic GMP-stimulated phosphodiesterase,CGS-PDE,cGSPDE. Uniprot: O00408. Background: Cyclic nucleotide ... phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important ...
Cyclic nucleotide turnover/signalling in the IUPHAR/BPS Guide to PHARMACOLOGY. ... 2013) Phosphodiesterases: Regulators of cyclic nucleotide signals and novel molecular target for movement disorders. Eur J ... Cyclic GMP-AMP synthase. *Exchange protein activated by cyclic AMP (EPACs) C ... 2011) Mammalian cyclic nucleotide phosphodiesterases: molecular mechanisms and physiological functions. Physiol Rev, 91 (2): ...
Phosphodiesterases from porcine coronary arteries: inhibition of separated forms by xanthines, papaverine, and cyclic ... Radioimmunoassay for cyclic nucleotides. I. Preparation of antibodies and iodinated cyclic nucleotides. ... cyclic GMP from induction of ornithine decarboxylase by the tumor promoter 12-O-tetradecanoyl phorbol-13-acetate in mouse ... cyclic GMP from induction of ornithine decarboxylase by the tumor promoter 12-O-tetradecanoyl phorbol-13-acetate in mouse ...
Jenal U, Malone J. Mechanisms of Cyclic-di-GMP Signaling in bacteria. Annu Rev Genet. 2006;40:385-407. ... and phosphodiesterase (PDE) (Additional file 3). In batch cultures of C. saccharolyticus cells contained very low c-di-GMP ... CG optimized and performed the analysis of c-di-GMP and also contributed with writing related to c-di-GMP. EvN was involved in ... cyclic dimeric guanosine monophosphate (c-di-GMP) and biofilm formation.. Conclusions. In co-cultures C. saccharolyticus ...
Keywords: phosophodiesterase-5 inhibitor, retinal function, color vision, electroretinogram, adverse events, placebo-controlled ... a temporary significant increase of Farnsworth-Munsell D100 total error score after 1 and 6 hours as well as in error lines 3 ... Cyclic nucleotide phosphodiesterases: functional implications of multiple isoforms. Physiol Rev. 1995;75(4):725-748. ... Effects of sildenafil on the relaxation of human corpus cavernosum tissue in vitro and on the activities of cyclic nucleotide ...
... cyclic-GMP phosphodiesterase activity : Catalysis of the reaction: guanosine 3,5-cyclic phosphate + H2O = guanosine 5- ... phosphodiesterase 6A Entrez ID 5145 Ensembl ID ENSG00000132915 (more details) KEGG ID hsa:5145 (more details) OMIM ID 180071 ... cyclic-nucleotide phosphodiesterase activity : Catalysis of the reaction: nucleoside 3,5-cyclic phosphate + H2O = nucleoside ... 5 Strand -1 Start 149857953 End 149944793 miRNA Interactions hsa-miR-147a (RPM: 0.0014) / hsa-miR-374a-5p (RPM: 52.6724) / hsa- ...
Cyclic-GMP Phosphodiesterases * Cyclic Nucleotide Phosphodiesterases, Type 6 * Enzyme Activation * GTP Phosphohydrolases ... cGMP phosphodiesterase (PDE gamma), and another yet unidentified membrane-associated protein factor. Here we test the ... being at least 5-fold more potent than GAIP, stimulates the rate of transducin GTPase by 2 orders of magnitude. Neither RGS4 ...
Cyclic-GMP Phosphodiesterases [D12.776.476.009] * Activating Transcription Factor 6 [D12.776.476.011] * Adaptor Proteins, ... Tumor Necrosis Factor alpha-Induced Protein 3 [D12.644.360.950] * Tumor Protein, Translationally-Controlled 1 [D12.644.360.963] ... Tumor Necrosis Factor alpha-Induced Protein 3 [D12.776.476.938] * Tumor Protein, Translationally-Controlled 1 [D12.776.476.941] ...
... cyclic-GMP phosphodiesterase Current Synonym true false 43518014 3,5-Cyclic-GMP phosphodiesterase Current Synonym true false ... cyclic-guanosine monophosphate phosphodiesterase Current Synonym true false 3721238014 3,5- ... cyclic-guanosine monophosphate phosphodiesterase (substance). Code System Preferred Concept Name. 3,5-cyclic-guanosine ...
Cyclic GMP / metabolism * Cyclic Nucleotide Phosphodiesterases, Type 6 / metabolism * G-Protein-Coupled Receptor Kinase 2 / ... Gautam Sikka 1 , G Patrick Hussmann 2 , Deepesh Pandey 1 , Suyi Cao 1 , Daijiro Hori 3 , Jong Taek Park 1 , Jochen Steppan 1 , ... Signaling is both soluble guanylyl cyclase- and phosphodiesterase 6-dependent but protein kinase G-independent. β-Adrenergic ... Jae Hyung Kim 1 , Viachaslau Barodka 1 , Allen C Myers 4 , Lakshmi Santhanam 5 , Daniel Nyhan 1 , Marc K Halushka 6 , Raymond C ...
cyclic nucleotide phosphodiesterase, putative 0.0058. 0.0155. 1. Echinococcus granulosus. dual 35 cyclic AMP and GMP ... camp-specific 35-cyclic phosphodiesterase 0.0058. 0.0155. 0.0556. Toxoplasma gondii. 35-cyclic nucleotide phosphodiesterase ... cyclic phosphodiesterase R153.1, putative 0.0418. 0.2052. 1. Trichomonas vaginalis. cyclic nucleotide phosphodiesterase, ... cAMP-specific phosphodiesterase, putative 0.0058. 0.0155. 0.3921. Loa Loa (eye worm). cyclic AMP specific phosphodiesterase ...
Activator of cGMP-dependent protein kinases I α, I β & type II and cGMP-gated ion channels (cyclic GMP agonist). Increased ... "The Binding of Cyclic Nucleotide Analogs to a Purified Cyclic GMP- Stimulated Phosphodiesterase from Bovine Adrenal Tissue" ... Chem., 274, 8391 - 8404 (1999), "Cyclic AMP- and Cyclic GMP-Dependent Protein Kinases Differ in Their Regulation of Cyclic AMP ... Chem., 274, 34301 - 34309 (1999), "Activation of Mitogen-Activated Protein Kinase Pathways by Cyclic GMP and Cyclic GMP- ...
Cyclic-GMP Phosphodiesterases. *Activating Transcription Factor 6. *Adaptor Proteins, Signal Transducing ...
Zn2+ and Cd2+ increase the cyclic GMP level in PC 12 cells by inhibition of the cyclic nucleotide phosphodiesterase. Toxicology ... von Bülow V, Rink L, Haase H (2005) Zinc-mediated inhibition of cyclic nucleotide phosphodiesterase activity and expression ... PLoS One 12(5): e0176069. doi:10.1371/journal.pone.0176069. Bulut A, Wörle M, Zorlu Y, Kirpi E, Kurt H, Zubieta J, Grabowsky S ... 87(5), 833-844 Kaltenberg J, Plum LM, Ober-Blöbaum JL, Hönscheid A, Rink L, Haase H (2010) Zinc Signals Promote IL-2-Dependent ...
Specifically amplifies 49, cyclic gmp phosphodiesterase inhibitor. In men over 30 years) undergoing bilateral nerve-sparing ... Or neutral words printed in various animal species.5,23 in animal research, in 491 m e n as helpful in reduc- buccal patches. ... Urology 1998; 35: 700 3. 5. Walsh pc. Even when the oxytocin cells in the postmenopausal range, the eggs also declines with age ...
"Cyclic GMP-mediated memory enhancement in the object recognition test by inhibitors of phosphodiesterase-2 in mice." ... Technikova-Dobrova, Z., A. M. Sardanelli, F. Speranza, S. Scacco, A. Signorile, V. Lorusso and S. Papa (2001). "Cyclic ... Soares, L. M., E. Meyer, H. Milani, H. W. Steinbusch, J. Prickaerts and R. M. de Oliveira (2017). "The phosphodiesterase type 2 ... Acin-Perez, R., E. Salazar, M. Kamenetsky, J. Buck, L. R. Levin and G. Manfredi (2009). "Cyclic AMP produced inside ...
  • The second messenger bis‐3,5‐cyclic di‐guanosine monophosphate (c‐di‐GMP) determines when Streptomyces initiate sporulation. (hu-berlin.de)
  • The bacterial second messenger cyclic di-3',5'-guanosine monophosphate (c-di-GMP) is a key regulator of bacterial motility and virulence. (rcsb.org)
  • 40 μM) intracellular levels of the secondary messenger bis-(3′-5′)-cyclic dimeric guanosine monophosphate (c-di-GMP) and biofilm formation. (biomedcentral.com)
  • however, they enhance the effect of nitric oxide (NO) by inhibiting PDE-5, which is responsible for degradation of cyclic guanosine monophosphate in the corpus cavernosum. (dovepress.com)
  • An enzyme next converts guanosine triphosphate (GTP) into cyclic guanosine monophosphate (cGMP). (rolpapost.com)
  • Pxiv and the Copenhagen Consensus says that' Cyclic guanosine monophosphate GMP is a chemical in your body that relaxes the order cialis low cost muscles in the penis and increases blood flow into the penis. (tamielle.com)
  • The continuous influx of sodium ions results from binding of cyclic guanosine monophosphate (cGMP) to the sodium gates, which keeps the gated channels open while maintaining neurotransmitter release onto the bipolar cell, hyperpolarizing it (ie, the bipolar cells are inhibited). (medscape.com)
  • The activated G-protein activates cGMP phosphodiesterase, which catalyzes the conversion of cGMP to guanosine monophosphate (GMP). (medscape.com)
  • Its mechanism of action shows it selectively targets and inhibits cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), thereby inhibiting the PDE5-mediated degradation of cGMP found in smooth muscle in animal subjects. (blogarama.com)
  • Kamagra inhibits the function of phosphodiesterase type 5 inhibitors in degrading cyclic guanosine monophosphate (cGMP), which is important for directing blood flow to the penis via smooth muscle relaxation and mediates the erectile response in patients. (safehealths.com)
  • Sildenafil is a selective phosphodiesterase type 5 (PDE5) inhibitor that produces arterial smooth muscle relaxation causing vasodilation in the penis and the lungs of animal test subjects by blocking the breakdown of cyclic guanosine monophosphate (cGMP) which results in prolongation of the action of mediators of vasodilation including nitric oxide (NO). It produces mild decreases in systolic and diastolic blood pressure. (lotilabs.com)
  • Cyclic guanosine monophosphate (cGMP) is produced in the penis during sexual stimulation causing the corpora cavernosa to relax, producing an erection. (lotilabs.com)
  • It improves erectile dysfunction by inhibiting phosphodiesterase-5, preventing the breakdown of cyclic guanosine monophosphate. (lotilabs.com)
  • As a cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5) selective inhibitor, penile smooth muscle relaxation allows rapid erection. (medical-steroids.com)
  • The initiation and maintenance of penile erection is related to the relaxation of cavernosal smooth muscle cells, and cyclic guanosine monophosphate (cGMP) is a mediator of the relaxation of cavernosal smooth muscle cells. (xahnb.com)
  • Armani A, Marzolla V, Rosano GM, Fabbri A, Caprio M. (2011) Phosphodiesterase type 5 (PDE5) in the adipocyte: a novel player in fat metabolism? (guidetoimmunopharmacology.org)
  • Alternatively, PKG activation and phosphodiesterase (PDE5/6) inhibition significantly reduce the time to the onset of anoxic coma. (biologists.com)
  • cGMP is then hydrolysed on the lazy GMP by phosphodiesteras kinds 5 (PDE5). (rolpapost.com)
  • Pde5 enzyme called phosphodiesterase inhibitors. (poochdecor.com)
  • Sildenafil is a selective and competitive inhibitor of type 5 phosphodiesterases (PDE5) on Smooth Muscle cells in the penis and pulmonary vessels. (blogarama.com)
  • Sildenafil is a selective phosphodiesterase type 5 (PDE5) inhibitor that is more potent than other phosphodiesterases. (blogarama.com)
  • Kamagra is classed as a PDE5 (phosphodiesterase type 5) inhibitor, which inhibits the enzyme PDE5 that is responsible for an individual's failure to get or keep an erection. (safehealths.com)
  • This drug is a phosphodiesterase type 5 (PDE5) inhibitor. (xahnb.com)
  • Adenosine 3',5' cyclic monophosphate assay at 10-15 mole level. (wikidata.org)
  • A simple and sensitive saturation assay method for the measurement of adenosine 3':5'-cyclic monophosphate. (wikidata.org)
  • Guanosine 3',5'-cyclic monophosphate (cGMP), as a second messenger, plays potential roles in ovarian functions. (geneticsmr.com)
  • cAMP (cyclic adenosine monophosphate) is a second messenger used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway. (glpbio.cn)
  • Guanosine 3',5'-cyclic monophosphate (cyclic GMP or cGMP) is a second messenger that is biosynthesized from GTP by guanylate cyclases. (glpbio.cn)
  • Formation of the cyclic pyrimidine nucleotide cyclic cytidine 3',5'-monophosphate (cCMP) by cytidylyl cyclases is debated. (biomedcentral.com)
  • Ervens J, Seifert R: Differential modulation by N4, 2'-O-dibutyryl cytidine 3':5'-cyclic monophosphate of neutrophil activation. (biomedcentral.com)
  • AbstractEvidence is presented here confirming the identification of guanosine 3′: 5′-monophosphate (c GMP) in the tissue of higher plants. (copernicus.ltd)
  • Ligand binding to MC4R activates adenylyl cyclase, resulting in increased levels of intracellular cyclic adenosine monophosphate (cAMP), a secondary messenger that regulates several cellular processes. (bvsalud.org)
  • Cyclic adenosine monophosphate responsive element-binding protein-1-regulated transcription coactivator-1 (CRTC1) is a cytoplasmic coactivator that translocates to the nucleus in response to cAMP and is reportedly involved in obesity. (bvsalud.org)
  • Second messengers, cyclic adenosine 3'-5'-monophosphate (cAMP) and cyclic guanosine 3'-5'-monophosphate (cGMP) are playing important roles in many animal cells by regulating intracellular signaling pathways and modulating cell physiology. (preprints.org)
  • Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. (nih.gov)
  • It is involved in the regulation of intracellular concentrations of cyclic nucleotides and is important for smooth muscle relaxation in the cardiovascular system. (nih.gov)
  • Cyclic nucleotides are second messengers generated by cyclase enzymes from precursor triphosphates and hydrolysed by phosphodiesterases. (guidetoimmunopharmacology.org)
  • The cellular actions of these cyclic nucleotides are mediated through activation of protein kinases ( cAMP - and cGMP -dependent protein kinases), ion channels ( cyclic nucleotide-gated, CNG , and hyperpolarization and cyclic nucleotide-gated, HCN ) and guanine nucleotide exchange factors (GEFs, Epac ). (guidetoimmunopharmacology.org)
  • The positive control of cell proliferation by the interplay of calcium ions and cyclic nucleotides. (wikidata.org)
  • Control of ornithine decarboxylase activity by cyclic nucleotides in the phytohemagglutinin induced lymphocyte transformation. (wikidata.org)
  • Radioimmunoassay for cyclic nucleotides. (wikidata.org)
  • I. Preparation of antibodies and iodinated cyclic nucleotides. (wikidata.org)
  • These purine cyclic nucleotides activate PKA and PKG, respectively. (biomedcentral.com)
  • So far, there was no evidence of further cyclic nucleotides acting as second messengers. (biomedcentral.com)
  • Enzymes that catalyze the hydrolysis of the 2'- or 3'- phosphate bonds of 2',3'-cyclic nucleotides. (nih.gov)
  • Keravis T, Lugnier C. (2012) Cyclic nucleotide phosphodiesterase (PDE) isozymes as targets of the intracellular signalling network: benefits of PDE inhibitors in various diseases and perspectives for future therapeutic developments. (guidetoimmunopharmacology.org)
  • The effect of the phosphodiesterase (PDE) isozyme selective inhibitors siguazodan (PDE III-selective), rolipram (PDE IV-selective), denbufylline (PDE IV-selective) and zaprinast (PDE V-selective) was examined on the relaxant responses to field stimulation and on relaxations elicited by the nitric oxide donor 3-morpholinosydnonimine-N-ethylcarbamide (SIN-1). (unboundmedicine.com)
  • The response to field stimulation in the presence of alpha-chymotrypsin (the putative nitric oxide component), at all the frequencies tested, was potentiated significantly by the PDE IV inhibitors rolipram (1 and 10 microM) and denbufylline (3 and 10 microM) as were responses to SIN-1. (unboundmedicine.com)
  • Missing at the time the definitive test, but it Isto inhibitors of phosphodiesterase type 5 (sildenafil, tadalafil,It was also given a stoneâAdult Attachment Interview brata, restricted/disinvestita and not integrated/ambivalent. (brekkieattiffanys.com)
  • Phosphodiesterase type 5 inhibitors in the treatment of pulmonary arterial iiron-dragon.com. (cwtvsource.com)
  • From a naturopathic perspective psoriasis is caused a toxic allergen, protein maldigestion, increased intestinal permeability, bowel toxicity, excess inflammation, leading to excess polyamines in the gut causing an imbalance of cAMP : cGMP and excess phosphodiesterase inhibitors (the enzyme involved in breaking down cGMP). (carahealth.com)
  • Including Cialis, cialis belongs to a group of medications called phosphodiesterase type 5 inhibitors. (nexus-people.com)
  • to inhibitors of phosphodiesterase type 5 (sildenafil, tadalafil, viagra online purchase central nervous system level. (theadventuresofgoldenass.com)
  • Diuretics water pills - household name drugs are also called phosphodiesterase pde inhibitors. (poochdecor.com)
  • Because no phosphodiesterase type 5 inhibitors limit the activity of cGMP in the patients, sufficient amounts of cGMP are maintained to trigger an erectile response. (safehealths.com)
  • Do not use nitroglycerin sublingual tablets in patients who are taking PDE-5 Inhibitors, such as avanafil, sildenafil, tadalafil, vardenafil hydrochloride. (nih.gov)
  • The enzyme 3′,5′-cyclic-GMP phosphodiesterase (EC 3.1.4.35) catalyzes the reaction guanosine 3′,5′-cyclic phosphate + H2O ⇌ {\displaystyle \rightleftharpoons } guanosine 5′-phosphate This enzyme belongs to the family of hydrolases, specifically those acting on phosphoric diester bonds. (wikipedia.org)
  • The third metal is positioned to stabilise the negative charge of the 5'-phosphate, and thus three metals could be required for catalysis in analogy to other nucleases. (rcsb.org)
  • 3',5'-cyclic-nucleotide phosphodiesterase activity : Catalysis of the reaction: nucleoside 3',5'-cyclic phosphate + H2O = nucleoside 5'-phosphate. (behrc.ir)
  • A major contribution in the endogenous production of H 2 S is offered by two pyridoxal-5′-phosphate- (PLP-) dependent enzymes, namely, CSE and CBS. (hindawi.com)
  • Nucleoside-2',3'-cyclic phosphate nucleotidohydrolase. (nih.gov)
  • Zolpidem, s And amount circled, warburton 3 points, registration predicted for 2022 see also Light. (tamielle.com)
  • However, functions of the development‐specific diguanylate cyclases (DGCs) CdgB and CdgC, and the c‐di‐GMP phosphodiesterases (PDEs) RmdA and RmdB, are poorly understood. (hu-berlin.de)
  • Caffeine is a potent albeit nonselective inhibitor of phosphodiesterase (PDEs), but how the health-related effects of caffeine are linked to PDEs is unknown. (biorxiv.org)
  • Spread of cAMP and cGMP is further shaped by cyclic nucleotide phosphodiesterases (PDEs) for orchestration of intracellular microdomain signaling. (preprints.org)
  • Recently discovered rhodopsin phosphodiesterase gene from protists established new and direct biological connection between light and PDEs. (preprints.org)
  • Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. (nih.gov)
  • In particular, it Has been seen that an increase of 1 mg/dl of serum uric acid levelsOverview of Module 5 of the dossier: clinical aspects The core clinical program, consisting of 31 Phase II/III clinical studies (4 main and other supportive) was aimed at evaluating the efficacy and safety of sildenafil for the treatment of erectile dysfunction (ED) in a broad-spectrum population. (theadventuresofgoldenass.com)
  • By inhibiting this enzyme, Sildenafil Citrate improves the amount of cyclic GMP and thus improves erection. (beemedz.com)
  • Sildenafil, a type-5 cGMP phosphodiesterase inhibitor, specifically amplifies endogenous cGMP-dependent relaxation in rabbit corpus cavernosum smooth muscle in vitro. (blogarama.com)
  • Sildenafil works by blocking the phosphodiesterase enzyme, breaking down cGMP, restoring erectile function. (lotilabs.com)
  • Sildenafil inhibits the PDE type-5 which is accountable for degradation of cyclic-GMP in the penis. (rxonpharm.com)
  • [3] Signaling molecules bind to a domain of the GPCR located outside the cell, and an intracellular GPCR domain then in turn activates a particular G protein. (wikipedia.org)
  • Cyclic di-GMP transduces extracellular stimuli into intracellular responses to modulate important biological processes. (nature.com)
  • Identification of YedQ as a bile receptor in enteric pathogens including S . Typhimurium and enterohemorrhagic Escherichia coli (EHEC) suggests bile salts will induce a rise in intracellular c-di-GMP levels when these pathogens enter the host gut. (nature.com)
  • Tadalafil is usually consumed in the form of tablets having 2.5, 5, 10, and 20 mg strengths. (weefselpharma.com)
  • Tadalafil inhibits the enzyme phosphodiesterase, which normally breaks down a substance called cyclic GMP (cGMP). (tadasiva.com)
  • Nevertheless, men who have never used erection pills before are recommended to start taking 5 mg of Tadalafil. (greatquotes.in)
  • Taking Viagra when its patent expiration generic cialis daily is to use Cialis, comprar viagra contrareembolso en españa you take tadalafil tablets should be immunized. (khio.no)
  • The in vivo mechanism of action is not entirely clear, but an inhibition of the enzyme phosphodiesterase causing elevation of cyclic AMP and cyclic GMP [ clarification needed ] levels is significant. (cloudfront.net)
  • The enzyme phosphodiesterase type 5 inactivates cyclic GMP. (beemedz.com)
  • EC 3.1.4.17 , 3,5-cyclic-nucleotide phosphodiesterase and EC 3.1.4.35 , 3,5-cyclic-GMP phosphodiesterase). (enzyme-database.org)
  • Reduce toxic levels of cyclic GMP in the RPE. (medscape.com)
  • As a phosphodiesterase type-5 inhibitor, it improves the levels of cyclic GMP, which is involved in producing a smooth muscle relaxation in the penis cavernous body in the course of protein interactions. (greatquotes.in)
  • The drug boosts levels of a substance called cyclic gmp, which is responsible for widening the blood vessels of the penis. (tinytalent.ca)
  • Activator of cGMP-dependent protein kinases I α, I β & type II and cGMP-gated ion channels (cyclic GMP agonist). (biolog.de)
  • Quorum sensing is a type of bacterial communication that occurs via the secretion of autoinducer molecules (5). (kenyon.edu)
  • Painless notes exactly how viagra jobs: Viagra Inhibits a protein also known as phosphodiesterase type 5 (PDE-5), making muscle tissue from inside the phallus prone to sit back and permitting blood stream to circulate in, leading to a hardon. (rolpapost.com)
  • Moreover, this chemical acts as a phosphodiesterase type-5-inhibitor. (arrowmeds.com)
  • Pharmacovigilance of the Ministry of levitra vs viagra vs cialis type 5 in human corpus cavernosum smooth muscle cells. (theadventuresofgoldenass.com)
  • These receptors trigger several cascades of signal transduction pathways, ultimately activating the critical transcription factors nuclear factor B (NF-B) and interferon regulatory factor 3 (IRF3), inducing the robust expression of type I interferons (IFNs), other cytokines, and chemokines (3). (icce2013bali.org)
  • Sildigra is a Phosphodiesterase type-5 inhibitor used for the treatment of erectile dysfunction in adult men available in the tablet form. (rxonpharm.com)
  • It is a type of medicine that is denoted as a phosphodiesterase type-5 inhibitor, which is an enzyme that lessens and causes breakdown of cyclic GMP, an another enzyme. (greatquotes.in)
  • 2002) Nitric Oxide-Cyclic GMP Signaling Pathway in the Regulation of Rabbit Clitoral Cavernosum Tone. (jenabioscience.com)
  • These results suggest that the nitric oxide component of the nonadrenergic, noncholinergic relaxant response is mediated primarily via cyclic AMP whose action is inactivated by a PDE IV isozyme and also by cyclic GMP which is inactivated by a PDE V isozyme. (unboundmedicine.com)
  • The most important interaction with ET is nitric oxide (NO). NO gets released after the utilization of L-arginine by the endothelial nitric oxide synthase (eNOS) to, therefore, increase cyclic GMP. (statpearls.com)
  • After releasing the nitric oxide activity, the enzyme guanylate cyclase leads to the synthesis of cyclic GMP or cGMP. (beemedz.com)
  • Its generation from NO synthase (NOS) and its action as a vasodilator were discovered a few years later in 1987 [ 3 ]. (hindawi.com)
  • Virus nucleic acids are predominantly recognized by Toll-like receptors (TLR3 for double-stranded RNA [dsRNA], TLR7 for single-stranded RNA [ssRNA], and TLR9 for CpG DNA) in the endosome and by retinoic acid-inducible gene I (RIG-I), melanoma differentiation-associated gene 50 (MDA5), cyclic GMP-AMP synthase DNA (cGAS), and other receptors in the cytosol (1, 2). (icce2013bali.org)
  • 1 When sexual stimulation causes local release of NO, inhibition of PDE-5 by vardenafil causes smooth muscle relaxation and inflow of blood to the corpus cavernosum. (dovepress.com)
  • 9 - 14 this may depend on the selectivity of PDE-5 inhibition. (dovepress.com)
  • Therefore, this study was designed to especially investigate the possible influence of vardenafil-induced PDE-5 inhibition on ocular side effects and the function of the retina. (dovepress.com)
  • This was most recently demonstrated by Lee et al who showed differences in protein kinase G (PKG) induced phosphoproteomic signatures depending on the upstream activating cascade.1 Here we identified unique sets of PKG-mediated phosphorylation targets, stimulated by phosphodiesterase (PDE) 5A or 9A inhibition. (researchsquare.com)
  • This enzyme is specific for 3′,5′-cAMP and does not hydrolyse other nucleoside 3′,5′-cyclic phosphates such as cGMP ( cf . (enzyme-database.org)
  • Background: KMUP-1 is a xanthine derivative with inhibitory activities on the phosphodiesterase (PDE) 3,4 and 5 isoenzymes to suppress the degradation of cyclic AMP and cyclic GMP. (fip.org)
  • Bayer AG, Leverkusen, Germany) has been developed as an inhibitor of phosphodiesterase 5 (PDE-5) for the treatment of erectile dysfunction. (dovepress.com)
  • Vardenafil has been shown to be effective and safe when administered to patients with erectile dysfunction in placebo-controlled studies over a dose range of 5-20 mg once daily and up to 40 mg twice daily in multiple-dose Phase I and II studies. (dovepress.com)
  • It improves erectile dysfunction by inhibiting phosphodiesterase-5. (blogarama.com)
  • Further benefits for your sex life and erectile function is in kind thanks to vitamin B6s ability to reduce your levels of the bad LDL Cholesterol and your total cholesterol levels [3]. (curemyerectiledysfunction.com)
  • Transcriptome analysis of ∆cdgB, ∆cdgC, ∆rmdA, and ∆rmdB strains revealed that the c‐di‐GMP specified by these enzymes has a global regulatory role, with about 20% of all S. venezuelae genes being differentially expressed in the cdgC mutant. (hu-berlin.de)
  • Our data suggest that the major c‐di‐GMP‐controlled targets determining the timing and mode of sporulation are genes involved in cell division and the production of the hydrophobic sheath that covers Streptomyces aerial hyphae and spores. (hu-berlin.de)
  • The products of the genes expressed at high GA 3 also conferred the deterrence of BIPOL colonization at SD = OD 0.6 . (biorxiv.org)
  • These genes include those encoding phototransduction-related proteins, such as rhodopsin, subunits of cyclic nucleotide phosphodiesterase (PDE), and cyclic nucleotide-gated (CNG) channel subunits, as well as genes encoding photoreceptor outer segment structural proteins, such as peripherin/ rds . (arvojournals.org)
  • Diurnal fluctuation and -adrenergic elevation of cyclic AMP in mouse epidermis in vivo. (wikidata.org)
  • 2003) Signaling of rat Frizzled-2 through phosphodiesterase and cyclic GMP. (jenabioscience.com)
  • Signaling is both soluble guanylyl cyclase- and phosphodiesterase 6-dependent but protein kinase G-independent. (nih.gov)
  • Impaired phosphodiesterase (PDE) function and mitochondrial Ca 2+ - [Ca 2+ ]m signaling leads to cardiac failure, ischemic damage and dysfunctional learning and memory. (biorxiv.org)
  • To elucidate the role of phosphodiesterase (PDE) in cGMP signaling during ovarian follicular development, the present study was conducted to investigate ovarian cGMP level and cGMP-PDE activity by radioimmunoassay (RIA) in postnatal rats, immature rats during gonadotropin-primed follicular development, ovulation and luteinization, adult rats during normal estrous cycle, and aged rats that spontaneously developed persistent estrus (PE). (geneticsmr.com)
  • Since the discovery of c-di-GMP almost three decades ago, cyclic dinucleotides (CDNs) have emerged as widely used signaling molecules in most kingdoms of life. (nature.com)
  • Seminal work on the discovery of c-di-GMP as an allosteric regulator of bacterial cellulose synthesis that laid the foundation of CDN signaling research. (nature.com)
  • 4. Nebigil, C.G., Pharm D., Maroteaux L. Functional consequence of serotonin 5-HT2B receptor signaling in heart. (rjptonline.org)
  • T3SS-1 has been shown to be regulated by c-di-GMP signaling, with decreased secretion of T3SS-1 effectors and reduced invasion caused by elevated c-di-GMP levels 1 , 6 . (nature.com)
  • The last question is how c-di-GMP signaling control the T3SS-1. (nature.com)
  • Guellich A, Mehel H, Fischmeister R. (2014) Cyclic AMP synthesis and hydrolysis in the normal and failing heart. (guidetoimmunopharmacology.org)
  • Regulation of cellulose synthesis in Acetobacter xylinum by cyclic diguanylic acid. (nature.com)
  • c-di-GMP-binding protein, a new factor regulating cellulose synthesis in Acetobacter xylinum . (nature.com)
  • Here, the authors show that AI-2 and bile salts induce cyclic-di-GMP synthesis via YeaJ and YedQ, respectively, to repress the T3SS via a cyclic-di-GMP-responsive T3SS chaperone. (nature.com)
  • Our study reveals that the quorum sensing signal autoinducer-2 (AI-2) and bile salts induce c-di-GMP synthesis via directly targeting a GAPES1 domain-containing diguanylate cyclase (DGC) YeaJ and the transmembrane DGC YedQ, respectively. (nature.com)
  • As AI-2 induces c-di-GMP synthesis, it is not surprising that AI-2 also represses T3SS-1 gene expression. (nature.com)
  • Here, we provide biochemical evidence that the GGDEF‐EAL domain protein RmdB from S. venezuelae is a monofunctional PDE that hydrolyzes c‐di‐GMP to 5′pGpG. (hu-berlin.de)
  • This phosphodiesterase specifically hydrolyzes cGMP to 5'-GMP. (nih.gov)
  • This gene encodes a cGMP-binding, cGMP-specific phosphodiesterase, a member of the cyclic nucleotide phosphodiesterase family. (nih.gov)
  • The PDE6H gene provides instructions for making one part (called the inhibitory gamma subunit) of an enzyme called cone-specific phosphodiesterase. (medlineplus.gov)
  • 5. Cote, F. Disruption of the nonneuronal tph 1 gene demonstrates the importance of peripheral serotonin in cardiac function/ F. Cote, E. Thevenot, C. Fligny. (rjptonline.org)
  • However, it took four more decades to elucidate the genetic defect underlying photoreceptor degeneration in the rd mouse: a nonsense mutation in the rod photoreceptor cGMP phosphodiesterase β subunit gene. (bmj.com)
  • Protein phosphorylation plays a role in a variety of cellular processes such as gene expression, metabolism, signal transduction, apoptosis, and cellular growth, division, and differentiation3-5. (researchsquare.com)
  • In 1984, Bowman and Drummond reported that a selective cyclic GMP phosphodiesterase inhibitor M&B22948 (zaprinast) increased cyclic GMP in the tissue and relaxed the bovine retractor penis muscle (Cyclic GMP mediates neurogenic relaxation in the bovine retractor penis muscle, Br. (justia.com)
  • Papaverine has also been demonstrated to be a selective phosphodiesterase inhibitor for the PDE 10A subtype found mainly in the striatum of the brain. (cloudfront.net)
  • This change prevents the production of any functional inhibitory gamma subunit, which interferes with the normal function of cone-specific phosphodiesterase. (medlineplus.gov)
  • provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-memberred amine ring substituted with a hydroxyl group is excluded. (justia.com)
  • [5] [6] Papaverine, when injected in penile tissue, causes direct smooth muscle relaxation and consequent filling of the corpus cavernosum with blood resulting in erection . (cloudfront.net)
  • S . Typhimurium encodes 17 predicted c-di-GMP-metabolizing enzymes, among which 9 contain a putative periplasmic sensory domain flanked by two transmembrane helices 4 . (nature.com)
  • While H 2 S is biosynthesized by three constitutively expressed enzymes (CBS, CSE, and 3-MST) from L-cysteine and homocysteine, NO is generated endogenously from L-arginine by the action of various isoforms of NOS. (hindawi.com)
  • However, it remains unclear if and how the activity of other 8 c-di-GMP-metabolizing enzymes with periplasmic sensory domains is modulated by extracellular signals. (nature.com)
  • Using cells with mutations in RNA repair and decay enzymes, we show that phosphorylation of two different HAC1 splicing intermediates is required for their degradation by the 5′→3′ exonuclease Xrn1 to enact opposing effects on the UPR. (elifesciences.org)
  • This has involved the study of noradrenergic mechanisms in the actions of antidepressant drugs and of cyclic nucleotide phosphodiesterases as potential targets for novel antidepressant, anxiolytic, and memory-enhancing drugs. (buffalo.edu)
  • García-Osta A, Cuadrado-Tejedor M, García-Barroso C, Oyarzábal J, Franco R. (2012) Phosphodiesterases as therapeutic targets for Alzheimer's disease. (guidetoimmunopharmacology.org)
  • This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, PubMed:15489334). (nih.gov)
  • On June 5, 2018, Eisai and Biogen announced positive elenbecestat topline results of Study 202 at 18 months which demonstrated acceptable safety and tolerability (primary endpoint), as well as a statistically significant effect on brain amyloid levels in the brain as measured by amyloid PET (exploratory endpoint). (picante.today)
  • To investigate rod function and survival after cone dysfunction and degeneration in a mouse model of cone cyclic nucleotide-gated (CNG) channel deficiency. (arvojournals.org)
  • Jenkins AL, Jenkins DJ, Zdravkovic U, Würsch P, Vuksan V.raltro always in the ag- buy viagra online 5. (bidgamlestaden.se)
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  • GC44920 Sp-8-bromo-Cyclic AMPS (sodium salt) Sp-8-bromo-cyclic AMPS (Sp-8-bromo-cAMPS) is a cell-permeable, cAMP analog that combines an exocyclic sulfur substitution in the axial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP. (glpbio.cn)
  • GC43339 Cyclic di-AMP (sodium salt) Cyclic di-AMP (c-di-AMP) is a second messenger produced by bacteria but not by mammals. (glpbio.cn)
  • The conversion of cGMP to GMP closes sodium channels. (medscape.com)
  • We confirmed that cCMP activates the purified cyclic nucleotide-dependent protein kinases cAK and cGK. (biomedcentral.com)
  • Then we investigated the effect of cCMP on purified cyclic nucleotide-dependent protein kinases and on intact tissues of wildtype (WT) and cGKI-knockout (KO) mice, namely jejunum, lung and brain. (biomedcentral.com)
  • cCMP stimulated cyclic GMP-dependent protein kinases in WT tissue lysates, however there was no stimulation of phosphorylation in KO tissue lysates. (biomedcentral.com)
  • Subsequently, other workers have reported one after another the relaxation of the penis cavernosum by increasing cyclic GMP in the tissue (Int. J. Impotence Res. (justia.com)
  • The improve in cyclic GMP causes rest of easy muscular tissues and arteries, leading to extra blood flowing into the penis. (dogacicek.com)
  • which is commonly known as cyclic GMP or cGMP, in the smooth muscle cells of the corpus cavernosum penis. (weefselpharma.com)
  • c‐di‐GMP signals are integrated into the genetic differentiation network by the regulator BldD and the sigma factor σWhiG. (hu-berlin.de)
  • Group 5: Pulmonary hypertension caused by other diseases or conditions, including sarcoidosis, polycythemia vera (which can lead to increased blood viscosity and, subsequently, pulmonary hypertension), vasculitis, and other disorders. (medscape.com)
  • 3. Avdeev S.N. Pulmonary hypertension.GEOTAR- Media. (rjptonline.org)
  • GC42622 8-bromo-Cyclic AMP 8-bromo-Cyclic AMP is a brominated derivative of cAMP that remains long-acting due to its resistance to degradation by cAMP phosphodiesterase. (glpbio.cn)
  • GC18751 Reticulol Reticulol is an isocoumarin derivative produced by certain species of Streptomyces that inhibits cAMP phosphodiesterase (IC50 = 41 uM). (glpbio.cn)
  • Isoprenaline (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-K m cAMP phosphodiesterase (cAMP-PDE) activity by about 100% in intact rat fat cells [1] . (medchemexpress.com)
  • million men aged 40 and above (5) .development âthe present day and of the metabolic syndrome, the market CHO) and the replacement of 15g of sucrose with 15 g ofalmost 50% after 70 years.lutointerested. (icte.at)
  • 2P236 Directional reversal of electrotactic movements in cyclic GMP metabolic mutants(39. (tsukuba.ac.jp)
  • 3 4 In 1993, 70 years after Keeler's original observations on the r mouse, Pittler and co-workers demonstrated by polymerase chain reaction (PCR) analysis of r DNA isolated from old histological sections that the defects in the r mouse and the rd mouse were identical. (bmj.com)
  • Try a chemical cyclic gmp in risky sexual stimulation. (poochdecor.com)
  • Isoprenaline (5 nM and 10 μM) increases cyclic AMP levels and this effect is potentiated by cilostamide (10 mM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO) [3] . (medchemexpress.com)
  • Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells [5] . (medchemexpress.com)
  • TDT patients had substantial mean increases in fetal hemoglobin (HbF) and corresponding increases in mean total hemoglobin (Hb), while all severe SCD were free of VOCs and mean HbF of approximately 40% by month 3 and 4 respectively. (ithanet.eu)
  • IMR-687 was developed to selectively block phosphodiesterase 9 (PDE9) in red blood cells, which in turn increases cyclic GMP levels, as a means to reactivate the production of foetal haemoglobin (HbF), a well-established modifier of disease severity. (ithanet.eu)
  • The amount of c GMP present increases 90-fold during fruit ripening. (copernicus.ltd)
  • It has been reported that the DGC YedQ increases c-di-GMP concentrations through sensing of L-arginine and other nutrient-related signals by its periplasmic sensory domain 4 . (nature.com)
  • A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. (drugbank.com)
  • Little is known about how extracellular signals modulate c-di-GMP metabolism to control T3SSs. (nature.com)
  • However, extracellular signals that modulate c-di-GMP metabolism to control bacterial secretion systems and c-di-GMP effectors that relay environmental stimuli to changes in activity of the secretion systems remain largely obscure. (nature.com)
  • Our work provides new insights into how environmental stimuli modulate bacterial c-di-GMP metabolism, as well as the molecular mechanism underlying c-di-GMP-mediated control of bacterial T3SSs. (nature.com)
  • In another study, the improvement of the copyrighted - insulin- dietary factors, which are so important to reduce theports, special-the end of phosphodiesterases in the vascular smooth muscle, with1 cc of solution = 1 U. I. to insulin of at least 60 mg/dl compared to the previous value, the patient20 years (mean 4.8 years). (mediasiegel.at)
  • Compared to placebo, administration of vardenafil hydrochloride lead to a temporary significant increase of Farnsworth-Munsell D100 total error score after 1 and 6 hours as well as in error lines 3 and 4 after 1 hour. (dovepress.com)
  • In co-cultures C. saccharolyticus fortified the trade of biofilm formation by C. owensensis , which was mediated by elevated levels of c-di-GMP in C. owensensis . (biomedcentral.com)
  • Hickman, J.W., Tifrea, D.F. & Harwood, C.S. A chemosensory system that regulates biofilm formation through modulation of cyclic diguanylate levels. (nature.com)