• PDE10A2 was phosphorylated by cAMP-dependent protein kinase (PKA) at Thr 16 . (johnshopkins.edu)
  • Egan, J. J., Greenberg, A. S., Chang, M. K. & Londos, C. Control of endogenous phosphorylation of the major cAMP-dependent protein kinase substrate in adipocytes by insulin and beta-adrenergic stimulation. (nature.com)
  • cAMP activates the cAMP-dependent protein kinase (PKA). (nih.gov)
  • cAMP modifies cell function in all eukaryotic cells, principally through the activation of cAMP-dependent protein kinase (PKA), but also through cAMP-gated ion channels and guanine nucleotide exchange factors directly activated by cAMP. (sigmaaldrich.com)
  • We show that this dual phenotype results from elevated cAMP levels and hyperactivation of the cAMP-dependent protein kinase (PKA). (crick.ac.uk)
  • The inhibitory effect of cAMP could not be reversed by inhibition of cAMP-dependent protein kinase (PKA) but was blocked by depletion of the alternative intracellular cAMP sensor exchange protein activated by cAMP 1 (Epac1), which is also required to observe SOCS-3 accumulation in response to cAMP. (gla.ac.uk)
  • cGMP via PKG activates 26S proteasomes and enhances degradation of proteins, including ones that cause neurodegenerative diseases. (harvard.edu)
  • Herpes simplex virus protein kinase US3 activates and functionally overlaps protein kinase A to block apoptosis. (uchicago.edu)
  • Activates phosphorylase kinase and cyclic nucleotide-independent protein kinase. (lookformedical.com)
  • Phosphodiesterase (PDE) enzymes are known to control cyclic GMP (cGMP) levels in the parasite, but the mechanisms by which cyclic AMP (cAMP) is regulated remain enigmatic. (crick.ac.uk)
  • melting point = 240°C), also known as 4',5-dihydroxy-7- methoxyisoflavone and 5-hydroxy-3-(4-hydroxyphenyl)-7-methoxy-4H-1- benzopyran-4-one, inhibits alcohol dehydrogenase, aldehyde dehydrogenase, 3',5'-cyclic-nucleotide phosphodiesterase, phosphodiesterase 4, and protein-tyrosine kinase. (chemicalbook.com)
  • Phosphodiesterases (PDEs) regulate the local concentration of 3',5' cyclic adenosine monophosphate (cAMP) within cells. (nih.gov)
  • Considerably higher resistance against cyclic nucleotide phosphodiesterases compared to dibutyryl- or 8-Br-cAMP (Cat. (biolog.de)
  • Dr. Beavo is being recognized for his research on the identification, regulation and functions of cyclic nucleotide phosphodiesterases, work on cyclic nucleotides, and for his strong commitment to mentoring. (aspet.org)
  • In 1977, Dr. Beavo joined the department of pharmacology at the University of Washington, where his research revealed 11 diverse families of cyclic-nucleotide phosphodiesterases with different substrate specificity and regulation. (aspet.org)
  • As can be seen in the cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) images, the 'cyclic' portion consists of two bonds between the phosphate group and the 3' and 5' hydroxyl groups of the sugar, very often a ribose. (wikipedia.org)
  • Evgeny Fesenko, Stanislav Kolesnikov, and Arkady Lyubarsky discovered in 1985 that cyclic guanosine monophosphate (cGMP) can initiate the photoresponse in rods. (wikipedia.org)
  • cAMP is 3'5'-cyclic adenosine monophosphate, cGMP is 3'5'-cyclic guanosine monophosphate, cCMP is cytidine 3',5'-monophosphate, and cUMP is uridine 3',5'-cyclic phosphate. (wikipedia.org)
  • The critical physiological roles of soluble guanylate cyclase (sGC)-cyclic guanosine monophosphate (cGMP) pathway have been well characterized in vasodilation and the corresponding therapies and pathway agonists have shown clinical benefits in treating hypertension. (scientificarchives.com)
  • PDE1 inhibition facilitates proteasomal degradation of misfolded proteins and protects against cardiac proteinopathy. (harvard.edu)
  • Vascular smooth muscle cell contractile protein expression is increased through protein kinase G-dependent and -independent pathways by glucose-6-phosphate dehydrogenase inhibition and deficiency. (harvard.edu)
  • Woolson, H. D. , Thomson, V. S. , Rutherford, C. , Yarwood, S. J. and Palmer, T. M. (2009) Selective inhibition of cytokine-activated extracellular signal-regulated kinase by cyclic amp via Epac1-dependent induction of suppressor of cytokine signalling-3. (gla.ac.uk)
  • Protein-protein interaction inhibition (2P2I): fewer and fewer undruggable targets. (leibniz-fli.de)
  • PTP, protein tyrosine phosphatase. (silverchair.com)
  • Since PKB activation is PI′-3-kinase dependent, the persistent activation of certain protein tyrosine kinases, such as IGF−1 receptor, EGF receptor, PDGF receptor, pp60c-Src, and the like, leads to the persistent activation of PKB which is indeed encountered in many tumors. (justia.com)
  • 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)
  • Although the importance of kinases in this process has long been recognized, an appreciation for the complex and fundamental role of phosphatases is more recent. (rupress.org)
  • Through extensive biochemical and genetic analysis, we now know that pathways are not simply switched on with kinases and off with phosphatases. (rupress.org)
  • Furthermore, kinases and phosphatases may work together to modulate the strength of a signal. (rupress.org)
  • Adding further complexity to this picture is the fact that both kinases and phosphatases can function in signaling networks where multiple kinases and phosphatases contribute to the outcome of a pathway. (rupress.org)
  • A variety of approaches, including biochemical purification, gene isolation by homology, and genetic screens, have been successfully used for the identification of putative protein kinases and phosphatases. (rupress.org)
  • these effects were blocked by U73122, an antagonist of phospholipase C. U73122 also abolished the effects of Wnta1-mediated upregulation of protein kinase C (PKC) β and γ expression, and the PKC antagonist Go 6983 eliminated Wnta1-induced secretion of ANP. (kjpp.net)
  • The present invention provides inhibitors of protein kinases comprising a molecule having at least a first moiety competent for penetration of the molecule into cells, and a second moiety for having a protein kinase inhibiting effect within the cells. (justia.com)
  • The present invention relates to cell permeable, stable conjugates comprising a cell-permeability enhancement moiety and a peptide or peptidomimetic, as selective inhibitors of protein kinases, to pharmaceutical compositions containing them, as well as to processes for the preparation and use of such complex molecules. (justia.com)
  • Contents: Symposium S3 : Protein structure and assembly / editor E. Hofmann - Symposium S4 : Structure and function of enzymes / editor W. Pfeil - Colloquium C5 : Technical enzymology / editor H. Aurich. (kobv.de)
  • A family of enzymes that catalyze the conversion of ATP and a protein to ADP and a phosphoprotein. (lookformedical.com)
  • Interestingly, recombinant protein of wild-type PDE10A2, but not PDE10A2 mutant with an Ala replacement at Thr 16 , was distributed to cytosolic fractions by co-transfection with a plasmid encoding the catalytic subunit of PKA. (johnshopkins.edu)
  • Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition. (rush.edu)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • Here we demonstrate that elevation of cyclic AMP (cAMP) levels in human umbilical vein endothelial cells (HUVECs) specifically attenuates ERK1,2 activation in response to either leptin or a soluble interleukin IL-6 receptor-α/IL-6 (sIL-6R-α/IL-6) trans-signalling complex but not protein kinase C activator phorbol 12-myristate 13-acetate. (gla.ac.uk)
  • Nickel, a specific cyclic nucleotide-gated (CNG) channel activator, decreases PGE 2 binding and so do the CNG channel activators Rp-8-Br-PET-cGMPS and Sp-8-Br-PET-cGMPS. (bgu.ac.il)
  • Nickel, a specific cyclic nucleotide-gated (CNG) channel activator, decreases PGE2 binding and so do the CNG channel activators Rp-8-Br-PET-cGMPS and Sp-8-Br-PET-cGMPS. (bgu.ac.il)
  • Removal of permeable cyclic nucleotides from the cell medium results in a fast and complete restoration of PGE 2 binding to the cells, suggesting that both cyclic nucleotides reduce PGE 2 binding by a reversible interaction with the prostaglandin-binding site, without the involvement of second messenger-activated protein kinases. (bgu.ac.il)
  • The understanding of the concept of second messengers, and in particular the role of cyclic nucleotides and their ability to relay physiological signals to a cell, has its origins in the research of glycogen metabolism by Carl and Gerty Cori, for which they were awarded a Nobel Prize in Physiology or Medicine in 1947. (wikipedia.org)
  • Protein kinases are involved in signal transduction pathways linking growth factors, hormones and other cell regulation molecules to cell growth, survival and metabolism under both normal and pathological conditions. (justia.com)
  • In cytoplasm, zinc mostly binds zinc-chelating proteins called metallothioneins (MTs). (frontiersin.org)
  • The Drosophila system not only allows us to determine whether a specific CRE-binding protein binds to a particular gene, but also allows us to ablate individual CRE-binding proteins and measure the effects of these manipulations on expression of specific target genes. (grantome.com)
  • The protein structural motif that binds cAMP is highly conserved with the exception of loops 3 and 4, whose structure and length are variable. (utmb.edu)
  • Richie-Jannetta, R., Francis, S.H. and Corbin, J.D. Dimerization of cGMP-dependent protein kinase Iβ is mediated by an extensive amino-terminal leucine zipper motif, and dimerization modulates enzyme function. (enzyme-database.org)
  • Cyclic GMP-Dependent Protein Kinases" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • Mitogen-activated protein kinase kinase kinases (MAPKKKs) are serine-threonine protein kinases that initiate protein kinase signaling cascades. (bvsalud.org)
  • During growth, genes associated with protein ubiquitination/deubiquitination, cell cycle progression, and proteasomal degradation were affected, while genes linked to protein and carbohydrate catabolism were affected during early development. (frontiersin.org)
  • Immediate activation of chemosensory neuron gene expression by bacterial metabolites is selectively induced by distinct cyclic GMP-dependent pathways in Caenorhabditis elegans. (harvard.edu)
  • Dr. Martemyanov is being recognized for his research on how G protein signaling pathways are organized and regulated in the retina, heart and brain. (aspet.org)
  • An author of over 100 publications, his lab has made key contributions in elucidation of structure/functional organization of RGS protein complexes, their role in controlling ion channels and second messenger pathways and implications for physiology of the nervous and cardiovascular systems. (aspet.org)
  • Fault tolerance in protein interaction networks: stable bipartite subgraphs and redundant pathways. (leibniz-fli.de)
  • Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction. (leibniz-fli.de)
  • In 1992 Lawrence Haynes and King-Wai Yau uncovered cNMP's role in the light-dependent cyclic-nucleotide-gated channel of cone photoreceptors. (wikipedia.org)
  • This graph shows the total number of publications written about "Cyclic GMP-Dependent Protein Kinases" by people in Harvard Catalyst Profiles by year, and whether "Cyclic GMP-Dependent Protein Kinases" was a major or minor topic of these publication. (harvard.edu)
  • Below are the most recent publications written about "Cyclic GMP-Dependent Protein Kinases" by people in Profiles. (harvard.edu)
  • A cyclic AMP-dependent protein kinase subtype primarily found in particulate subcellular fractions. (uchicago.edu)
  • Overall, this study reveals the impact of cln5 -deficiency on gene expression in D. discoideum , provides insight on the genes and proteins that play a role in regulating Cln5-dependent processes, and sheds light on the molecular mechanisms underlying CLN5 disease. (frontiersin.org)
  • As a postdoctoral fellow and research faculty member, he made major contributions to understanding cyclic AMP-dependent protein kinases and contributed significantly to work that later led to the Nobel Prize for Dr. Krebs. (aspet.org)
  • The sensitivity of PGE 2 binding to selective CNG channel modifying agents, as well as the rapid and reversible interaction with cyclic nucleotides, may suggest that the common low-affinity prostanoid-binding site on bovine aortic endothelial cells is associated with a molecular entity, which possess several properties of a CNG channel. (bgu.ac.il)
  • Discovery of cyclic nucleotides has contributed greatly to the understanding of kinase and phosphatase mechanisms, as well as protein regulation in general. (wikipedia.org)
  • In exocrine acinar cells regulation of intracellular calcium plays a pivotal role in controlling fluid and protein secretion. (rochester.edu)
  • The current proposal takes a fresh look at trying to understand how a single DNA element, the cyclic AMP-regulated enhancer (CRE), participates in the diverse regulation element in the somatostatin and PEPCK genes, the CRE has been found to contribute to the regulation of dozens of cellular, viral, and even plant genes. (grantome.com)
  • STP, serine/threonine protein phosphatase. (rupress.org)
  • Its virulence is determined by the presence of a type 3 secretion system (T3SS) (8, 14), which represents a needle complex that is used to intoxicate host cells with bacterial effector proteins. (healthyconnectionsinc.com)
  • A giant elastic protein of molecular mass ranging from 2,993 kDa (cardiac), 3,300 kDa (psoas), to 3,700 kDa (soleus) having a kinase domain. (lookformedical.com)
  • Deciphering soluble and membrane protein function using yeast systems. (leibniz-fli.de)
  • Mechanisms That Activate 26S Proteasomes and Enhance Protein Degradation. (harvard.edu)
  • Previously, we have shown in a mouse model that exposure to hog dust extract (HDE) collected from a CAFO results in the activation of protein kinase C (PKC), elevated lavage fluid cytokines/chemokines including interleukin-6 (IL-6), and the development of significant lung pathology. (cdc.gov)
  • The complex molecules are preferably peptide conjugates having improved cell-permeability, serum stability and kinase selectivity compared to known protein kinase inhibitors. (justia.com)
  • The potential to use genetics to dissect the components of complex regulatory systems led us to search for CRE-binding proteins in Drosophila. (grantome.com)
  • Based on the sequence differences between CRP and cyclic nucleotide gated channel, three mutants of CRP were constructed: deletion (residues 54-56 in loop 3 were deleted), insertion (loop 4 was lengthened by 5 residues between Glu-78 and Gly-79) and double mutants. (utmb.edu)
  • They have been identified as secondary messengers in both hormone and ion-channel signalling in eukaryotic cells, as well as allosteric effector compounds of DNA binding proteins in prokaryotic cells. (wikipedia.org)
  • The enzyme also has two allosteric cGMP-binding sites (sites A and B). Binding of cGMP causes a conformational change that is associated with activation of the kinase [4]. (enzyme-database.org)
  • abstract = "Cyclic AMP is a ubiquitous secondary message that regulates a large variety of functions. (utmb.edu)
  • The role of cyclic uridine monophosphate (cUMP) is even less well known. (wikipedia.org)
  • This study involves precisely defining by molecular techniques the individual signaling proteins expressed in the acinar cell and then subsequently assessing if individual agonists utilize discrete and different elements of the PI-signaling pathway. (rochester.edu)
  • Molecular structure and characterization of bovine heart protein kinase. (elsevierpure.com)
  • These molecular properties of PKB and its central role in tumorigenesis, implies that this protein kinase may be an attractive target for novel anti-cancer agents. (justia.com)
  • Dr. Martemyanov will deliver the John J. Abel Award in Pharmacology Lecture titled "Molecular Control of G protein Signaling" on Sunday, April 22, 2018 from 8:30 am - 9:15 am. (aspet.org)
  • Four such effector proteins are known, including exoenzymes S (ExoS), T (ExoT), U (ExoU), and Y (ExoY) (9). (healthyconnectionsinc.com)
  • Whereas these effector proteins do not appear to control bacterial invasion, they seem to fulfill critical roles in bacterial dissemination and survival, in part by thwarting the attack of immune cells (32). (healthyconnectionsinc.com)
  • The cAMP receptor protein of Escherichia coli, CRP, was employed as a model system to elucidate the functional roles of these loops. (utmb.edu)
  • Thus, the roles played by loop 3 in CRP may represent a more common mechanism employed by cyclic nucleotide binding domain in modulating ligand binding affinity and intramolecular communication. (utmb.edu)
  • Chen, R & Lee, JC 2003, ' Functional roles of loops 3 and 4 in the cyclic nucleotide binding domain of cyclic AMP receptor protein from Escherichia coli ', Journal of Biological Chemistry , vol. 278, no. 15, pp. 13235-13243. (utmb.edu)
  • Functionally active targeting domain of the beta-adrenergic receptor kinase: an inhibitor of G beta gamma-mediated stimulation of type II adenylyl cyclase. (musc.edu)
  • Bacterial proteases and elastases Lanabecestat degrade matrix proteins and contribute to alveolar edema and hemorrhage. (healthyconnectionsinc.com)
  • More recently investigators have found that these bacterial cyclases simultaneously synthesize more than one cyclic nucleotide. (healthyconnectionsinc.com)