• As in somatic cells, sperm intracellular cAMP concentration is regulated by the opposite action of two enzymes: the adenylyl cyclases (AC), which synthesize cAMP from ATP, and the phosphodiesterases (PDE), which break the phosphodiester bond of cAMP to form 5'-adenosine monophosphate (AMP). (plos.org)
  • Bronchiolar obstruction, which causes airway obstruction in hyperresponsive airways, often results from the contraction of the airway's smooth muscles, increased viscid mucous secretions, and mucosal oedema consequent upon a reduced cyclic 3,5-adenosine monophosphate (c-AMP). (biomedcentral.com)
  • 3'-5'-Cyclic adenosine monophosphate/protein kinase A (cAMP/PKA) signalling is activated by different extracellular stimuli and mediates many diverse processes within the same cell. (ox.ac.uk)
  • Cyclic adenosine monophosphate ( cAMP , cyclic AMP , or 3',5'-cyclic adenosine monophosphate ) is a second messenger , or cellular signal occurring within cells, that is important in many biological processes. (wikipedia.org)
  • Earl Sutherland of Vanderbilt University won a Nobel Prize in Physiology or Medicine in 1971 "for his discoveries concerning the mechanisms of the action of hormones", especially epinephrine, via second messengers (such as cyclic adenosine monophosphate, cyclic AMP). (wikipedia.org)
  • Adenyl Cyclase - A membrane-bound enzyme that converts adenosine monophosphate to cyclic adenosine monophosphate (cAMP), an intracellular second messenger. (poisonfluoride.com)
  • Thus, our discovery of the role of functional interaction between intracellular signaling pathways mediated by calcium ions (Ca 2+) and cyclic adenosine monophosphate (cAMP) (Ca 2+ /cAMP signaling interaction) in these cellular responses, opened a great avenue for the development of new antitumor therapeutic strategies. (researchgate.net)
  • Fertel and Weiss, 1976) therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s). (biomedjournal.com)
  • Bronchoconstriction, a state of bronchial smooth muscle tone is modulated by the interactions of the beta-adrenergic receptors and the metabolism of the intracellular cyclic nucleotides. (biomedcentral.com)
  • Cyclic nucleotides, including cyclic AMP (cAMP), cyclic GMP (cGMP) and cyclic ADP-ribose, have been extensively studied as second messengers of intracellular events initiated by activation of GPCRs. (sigmaaldrich.com)
  • Cyclic nucleotides, like other nucleotides, are composed of three functional groups: a ribose sugar, a nitrogenous base, and a single phosphate group. (pancreapedia.org)
  • A cyclic nucleotide, unlike other nucleotides, has a cyclic bond arrangement between the ribose sugar and the phosphate group. (pancreapedia.org)
  • There are two main groups of cyclic nucleotides: the canonical or well-established and the non-canonical or unknown-function cyclic nucleotides. (pancreapedia.org)
  • The two well-established cyclic nucleotides are adenosine-3',5'-cyclic monophosphate (cyclic AMP) and guanine-3',5'-cyclic monophosphate (cyclic GMP). (pancreapedia.org)
  • The non-canonical cyclic nucleotides include the purines inosine-3',5'-cyclic monophosphate (cyclic IMP), xanthosine-3',5'-cyclic monophosphate (cyclic XMP) and the pyrimidines cytidine-3',5'-cyclic monophosphate (cyclic cCMP), uridine-3',5'-cyclic monophosphate (cyclic UMP), and thymidine-3',5'-cyclic monophosphate (cTMP) (145). (pancreapedia.org)
  • An overview of the non-canonical cyclic nucleotides is provided in Section V. (pancreapedia.org)
  • Cyclic nucleotides form when the phosphate group of the molecule of nucleotide triphosphate (ATP or GTP) is attacked by the 3' hydroxyl group of the ribose, forming a cyclic 3',5'-phosphate ester with release of pyrophosphate. (pancreapedia.org)
  • This cyclic conformation allows cyclic nucleotides to bind to proteins to which other nucleotides cannot. (pancreapedia.org)
  • In addition, cAMP binds to and regulates the function of ion channels such as the HCN channels and a few other cyclic nucleotide-binding proteins such as Epac1 and RAPGEF2 . (wikipedia.org)
  • Cyclic AMP binds to specific locations on the regulatory units of the protein kinase, and causes dissociation between the regulatory and catalytic subunits, thus enabling those catalytic units to phosphorylate substrate proteins. (wikipedia.org)
  • Intracellular Signaling Peptides and Proteins" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (jefferson.edu)
  • Intracellular signaling peptide and proteins may be part of an enzymatic signaling cascade or act through binding to and modifying the action of other signaling factors. (jefferson.edu)
  • This graph shows the total number of publications written about "Intracellular Signaling Peptides and Proteins" by people in this website by year, and whether "Intracellular Signaling Peptides and Proteins" was a major or minor topic of these publications. (jefferson.edu)
  • Below are the most recent publications written about "Intracellular Signaling Peptides and Proteins" by people in Profiles. (jefferson.edu)
  • Hormones mobilize intracellular second messengers and initiate signalling cascades involving protein kinases and phosphatases, which are often spatially compartmentalized by anchoring proteins to increase signalling specificity 1 . (nature.com)
  • Goupil S, Maréchal L, El Hajj H, Tremblay M-È, Richard FJ, Leclerc P (2016) Identification and Localization of the Cyclic Nucleotide Phosphodiesterase 10A in Bovine Testis and Mature Spermatozoa. (plos.org)
  • Zhang L, Zhang Z, Zhang RL, Cui Y, LaPointe MC, Silver B, Chopp M. Tadalafil, a long-acting type 5 phosphodiesterase isoenzyme inhibitor, improves neurological functional recovery in a rat model of embolic stroke. (umassmed.edu)
  • Phosphodiesterase inhibitor-mediated potentiation of adenovirus delivery to myocardium. (umassmed.edu)
  • While most candidates stated that milrinone was an inodilator details on its mechanism of action as a selective phosphodiesterase type III inhibitor were on the whole vague. (derangedphysiology.com)
  • Preincubation of CF-T43 cells with CFTR anti-sense oligonucleotides prevented an increase in 36Cl- efflux in response to beta-agonist and phosphodiesterase inhibitor. (nih.gov)
  • A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE) selectively in the brain. (biomedjournal.com)
  • Retinal 3′,5′-cGMP phosphodiesterase (PDE) is located in photoreceptor outer segments and is an important enzyme in phototransduction. (wikipedia.org)
  • Both rod and cone PDEs catalyze the hydrolysis of cAMP or cGMP to their 5′ monophosphate form. (wikipedia.org)
  • cGMP) are important intracellular regulators downstream from GPCRs. (enzolifesciences.com)
  • Enzo Life Sciences offers the most sensitive and complete colorimetric ELISA kits for quantification of intracellular or extracellular cAMP or cGMP in a variety of sample types. (enzolifesciences.com)
  • Most sensitive (0.025 pmol/ml) colorimetric kit for intracellular cGMP quantification. (enzolifesciences.com)
  • The homeostatic role of phosphodiesterases (PDEs) as related to the intracellular levels of cAMP and cGMP was first described by Sutherland (Sutherland, Rall, 1958) who, due to this, was awarded the Nobel Prize for Physiology and Medicine in 1971. (biomedjournal.com)
  • Phosphodiesterases (PDEs) hydrolyze the phosphodiester bond of cAMP and cGMP to form the inactive 5′-AMP and 5′-GMP. (biomedjournal.com)
  • In optimization of the intracellular levels of cAMP and cGMP, breakdown is predominant over synthesis. (biomedjournal.com)
  • Phosphodiesterase-10A (PDE10A) hydrolyse the secondary messengers cGMP and cAMP , two molecules taking part in vital roles in neurodevelopment and mind capabilities. (aabioetica.org)
  • In eukaryotes, cyclic AMP works by activating protein kinase A (PKA, or cAMP-dependent protein kinase ). (wikipedia.org)
  • The increase in 36Cl- permeability is diminished by protein kinase A inhibitors and is not mediated by an increase in intracellular calcium concentrations. (nih.gov)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • The principal process by which intracellular cAMP levels are reduced is via hydrolysis by the phosphodiesterase enzymes. (biomedcentral.com)
  • Enzymes that catalyze the hydrolysis of cyclic GMP to yield guanosine-5'-phosphate. (umassmed.edu)
  • 2001). The substrate specificities include the enzymes which are specific for cAMP hydrolysis, those for cyclic GMP hydrolysis (Mehats et al. (biomedjournal.com)
  • Within the cytoplasm of the cardiac myocyte milrinone inhibits the enzyme PDE 3 which results in the inhibition of the breakdown of cyclic AMP which in turn results in elevated cellular levels of cAMP. (derangedphysiology.com)
  • Since intracellular calcium plays a key role in cardiac automaticity, conductivity and contractility, intoxication from these drugs leads to an inhibition of sinus and atrio-ventricular (AV) node depolarization and to a depression of myocardial cell contractility5. (doczz.net)
  • Elevated levels of AMP lead to an inhibition of PP2C activity, which allows AMPK to remain stable in the active Thr 172 -phosphorylated state [ 27 ] [ 28 ] . (encyclopedia.pub)
  • We have found that, 36Cl- efflux can be stimulated 19-61% above baseline by beta-adrenoreceptor agonists and cGI-phosphodiesterase inhibitors in transformed nasal polyp (CF-T43) cells homozygous for the deltaF508 mutation. (nih.gov)
  • A cell-based high-throughput screen (HTS) was developed to detect phosphodiesterase 8 (PDE8) and PDE4/8 combination inhibitors. (sigmaaldrich.com)
  • Phosphodiesterase inhibitors (PDIs) have important vascular and myocardial protective effects and thus have shown therapeutic usefulness in the clinical settings for treatment of patients with heart failure, pulmonary hypertension, and coronary artery disease. (biomedjournal.com)
  • The potential activity for selective phosphodiesterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait (Weiss and Hait, 1977). (biomedjournal.com)
  • In the present paper, we focus on ADCY10 localization and a kinetic analysis of intracellular cAMP accumulation in response to human LH in the absence or presence of four different ADCY10 inhibitors (KH7, LRE1, 2-CE and 4-CE) in MTLC-1 cells. (bvsalud.org)
  • Intracellular signaling protein kinases that play a signaling role in the regulation of cellular energy metabolism. (rush.edu)
  • AMP-activated protein kinases modify enzymes involved in LIPID METABOLISM, which in turn provide substrates needed to convert AMP into ATP. (rush.edu)
  • cAMP is a derivative of adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway . (wikipedia.org)
  • cAMP is a second messenger , used for intracellular signal transduction, such as transferring into cells the effects of hormones like glucagon and adrenaline , which cannot pass through the plasma membrane. (wikipedia.org)
  • Considerably higher resistance against cyclic nucleotide phosphodiesterases compared to dibutyryl- or 8-Br-cAMP (Cat. (biolog.de)
  • It is most well recognized as a key signaling trigger in the relaxation of smooth muscle cells (resulting in vasodilation) in response to nitric oxide, and as a sodium ion channel regulator (via its degradation by phosphodiesterases) critical to phototransduction. (enzolifesciences.com)
  • synthesized by GGDEF domain-containing diguanylate cyclases and degraded by HD-GYP domain-containing phosphodiesterases (PDEs) to 2 GMP or by EAL domain-containing PDE-As to 5′-phosphoguanylyl-(3′,5′)-guanosine (pGpG). (knoblauchpublishing.com)
  • Generally, these enzymes hydrolyze a nucleoside 3′,5′-cyclic phosphate to a nucleoside 5′-phosphate: nucleoside 3′,5′-cyclic phosphate + H2O = nucleoside 5′-phosphate They thus control the cellular levels of the cyclic second messengers and the rates of their degradation. (wikipedia.org)
  • Nitrate represses production of an important biofilm component, curli, and activates flagella via the modulation of intracellular cyclic-di-GMP levels. (knoblauchpublishing.com)
  • Their activity largely depends upon the concentration of cellular AMP which is increased under conditions of low energy or metabolic stress. (rush.edu)
  • Using RT-PCR, 5'- and 3'-RACE approaches we clearly show that PDE10A transcript variants X3 and X5 are expressed in bovine testis as well as in primary spermatocytes and spermatids. (plos.org)
  • This step is necessary for the nucleophilic catalysis on the 5' α-phosphate by the newly formed oxyanion. (pancreapedia.org)
  • Glyceraldehyde 3-phosphate dehydrogenase [Interproscan]. (ntu.edu.sg)
  • With regard to the intracellular cyclic AMP level in normal PEC, it was significantly enhanced by a high concentration of TBX (10(-3) g/ml). (unboundmedicine.com)
  • Finally, we propose that PggH could modulate the activities of PDE-As and the intracellular concentration of c-di-GMP, resulting in phenotypic changes including in biofilm formation. (knoblauchpublishing.com)
  • The main interests of single-chain gonadotropins are that 1/only one single plasmid is required to produce an active recombinant hormone, 2/the two subunits' domains are constantly present in equal amounts and 3/they remain in close proximity even at low concentration for forming the hormone bioactive 3D structure. (bvsalud.org)
  • The aim of this study was to determine the off-target effects of the anti-depressant drug FLX, on the human ovarian granulosa tumor COV434 cells stimulated by forskolin (FSK), by measuring the real-time kinetics of intracellular cyclic AMP (cAMP), ATP level, cytoplasmic calcium ([Ca2+]cyt) and survival of COV434 cells. (bvsalud.org)
  • In fact, CCB interfere with calcium cell influx blocking "L" type voltage dependent channels3, whereas BB lower intracellular cyclic AMP and thereby reduce intracellular calcium contents4 (Figure 1). (doczz.net)
  • CCB determine vasodilation by lowering smooth muscle intracellular calcium content6, whereas most BB cause vasoconstriction diverting catecholamines on constricting alfa adrenoceptors. (doczz.net)
  • They generally contain several modular domains, each of which having its own binding activity, and act by forming complexes with other intracellular-signaling molecules. (childrensmercy.org)
  • Despite an improved understanding of how c-di-GMP signaling regulates S. Typhimurium biofilms, the processes that affect the intracellular c-di-GMP levels and the formation of multicellular communities in vivo during infections remain unknown. (knoblauchpublishing.com)
  • Evidences suggest that Ca 2+ channels TRP and Orai participate in the intracellular Ca 2+ signaling involved the physiological angiogenesis processes [17]. (researchgate.net)
  • New antitumor strategies using drugs targeted to intracellular signaling involved in cell proliferation and survival, angiogenesis, and metastasis have become promising in recent years. (researchgate.net)
  • Cyclic nucleotide signaling can be initiated by two general mechanisms. (pancreapedia.org)
  • In addition to its PRKA-dependent effects, different studies have clearly demonstrated that cAMP also activates EPAC ( E xchange P roteins directly A ctivated by c AMP) during capacitation and acrosome exocytosis [ 15 - 17 ]. (plos.org)
  • Elks, M. L. & Manganiello, V. C. Antilipolytic action of insulin: role of cAMP phosphodiesterase activation. (nature.com)
  • By using blockers of PKA and CaMKII and a Caveolin-3-knockout mouse model, we conclude that the β2AR-LTCC regulation requires the presence of caveolin-3 and the activation of the CaMKII pathway. (imperial.ac.uk)
  • Risk factors for depression initiate an infection-like inflammation in the brain that involves activation microglial Toll-like receptors and glycogen synthase kinase-3β (GSK3β). (mdpi.com)
  • Cyclic AMP is synthesized from ATP by adenylate cyclase located on the inner side of the plasma membrane and anchored at various locations in the interior of the cell. (wikipedia.org)
  • Thus, there remains considerable interest in the measurement of intracellular cAMP concentrations in tissues and cell culture. (enzolifesciences.com)
  • Therefore, highly sensitive in vitro bioassays for various hormones and other GPCR ligands can be set up in mLTC to measure circulating concentrations in only 3-10 µL of blood or other body fluids. (bvsalud.org)
  • The signal source can be either extracellular, such as nitric oxide (NO) (114), or intracellular, such as bicarbonate (189). (pancreapedia.org)
  • It plays a key role during sperm capacitation [ 3 - 6 ] and the acrosomal exocytosis [ 7 - 10 ], where it affects different intracellular signalling pathways. (plos.org)
  • Predentin and odontoblastic processes were stained for IGF-I and IGFBP-3. (shengsci.com)
  • Sperm intracellular cAMP levels depend on the activity of adenylyl cyclases, mostly SACY, though transmembrane-containing adenylyl cyclases are also present, and on the activity of cyclic nucleotide phosphodiesterases (PDE) whose role is to degrade cAMP into 5'-AMP. (plos.org)
  • MATERIALS AND METHODS: The human microvascular endothelial tissues microarray datasets (GSE11341) of lung and cardiac expose to hypoxia (1% O2) for 3, 24 and 48 h were retrieved from the public repository. (bvsalud.org)