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| phorbol estersSummarySummary: Tumor-promoting compounds obtained from CROTON OIL (Croton tiglium). Some of these are used in cell biological experiments as activators of protein kinase C. Top Publications
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Molecular cloning and characterization of protein kinase D: a target for diacylglycerol and phorbol esters with a distinctive catalytic domainA M Valverde
Imperial Cancer Research Fund, London, United Kingdom
Proc Natl Acad Sci U S A 91:8572-6. 1994A serine/threonine protein kinase that binds phorbol esters and diacylglycerol (named protein kinase D, PKD) has been identified...
Modulation of the transient receptor potential vanilloid channel TRPV4 by 4alpha-phorbol esters: a structure-activity studyThomas Kjaer Klausen
KU Leuven, Department of Molecular Cell Biology, Laboratory Ion Channel Research, Campus Gasthuisberg, Herestraat 49, Bus 802, Leuven, Belgium
J Med Chem 52:2933-9. 2009The mechanism of activation of the transient receptor potential vanilloid 4 (TRPV4) channel by 4alpha-phorbol esters was investigated by combining information from chemical modification of 4alpha-phorbol-didecanoate (4alpha-PDD, 2a), site-..
Prostratin induces HIV activation and downregulates HIV receptors in peripheral blood lymphocytesJoaquín Rullas
AIDS Immunopathogenesis Unit, Centro Nacional de Microbiologia, Instituto de Salud Carlos III, Madrid, Spain
Antivir Ther 9:545-54. 2004..These data support the potential use of prostratin to activate HIV from latency and purge viral reservoirs...- The structural requirements for phorbol esters to enhance serotonin and acetylcholine release from rat brain cortexL Iannazzo
Prince Henry s Institute of Medical Research, Victoria, Australia
Br J Pharmacol 127:1177-89. 1999..Another group of phorbol esters containing a common 13-ester substituent (phorbol 12,13-diacetate, PDA; phorbol 12-myristate 13-acetate, PMA; .. - Phorbol esters induce intracellular accumulation of the anti-apoptotic protein PED/PEA-15 by preventing ubiquitinylation and proteasomal degradationAnna Perfetti
Dipartimento di Biologia e Patologia cellulare e Molecolare DBPCM, Federico II University of Naples, Via Pansini 5, 80131 Naples, Italy
J Biol Chem 282:8648-57. 2007..Exposure of untransfected C5N keratinocytes and transfected HEK293 cells to phorbol esters (12-O-tetradecanoylphorbol-13-acetate (TPA)) increased PED/PEA-15 cellular content and enhanced its .. - Antimycobacterial activity of phorbol esters from the fruits of Sapium indicumParinuch Chumkaew
Department of Chemistry, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand
J Nat Prod 66:540-3. 2003Three new phorbol esters, 12-(2-N-methylaminobenzoyl)-4beta,5,20-trideoxyphorbol-13-acetate (1), 12-(2-N-methylaminobenzoyl)-4alpha,5,20-trideoxyphorbol-13-acetate (2), and 12-(2-N-methylaminobenzoyl)-4alpha, 20-dideoxy-5-hydroxyphorbol-.. - Phorbol esters and neurotransmitter release: more than just protein kinase C?Eugene M Silinsky
Department of Molecular Pharmacology and Biological Chemistry, Northwestern University Medical School, 303 East Chicago Avenue, Chicago, IL 60611, U S A
Br J Pharmacol 138:1191-201. 2003This review focuses on the effects of phorbol esters and the role of phorbol ester receptors in the secretion of neurotransmitter substances... - Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/betaSung Hee Choi
Laboratory of Cancer Biology and Genetics, Center for Cancer Research, NCI, National Institutes of Health, Bethesda, Maryland 20892, USA
J Biol Chem 283:10543-9. 2008C1 domains mediate the recognition and subsequent signaling response to diacylglycerol and phorbol esters by protein kinase C (PKC) and by several other families of signal-transducing proteins such as the chimerins or RasGRP... - Cell swelling, heat, and chemical agonists use distinct pathways for the activation of the cation channel TRPV4J Vriens
Department of Physiology, Campus Gasthuisberg, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
Proc Natl Acad Sci U S A 101:396-401. 2004..b>Phorbol esters and heat operate by means of a distinct, PLA(2)- and cytochrome p450 epoxygenase-independent pathway, which .. - Phorbol esters and adenosine affect the readily releasable neurotransmitter pool by different mechanisms at amphibian motor nerve endingsT J Searl
Department of Molecular Pharmacology and Biological Chemistry, Northwestern University Medical School, 303 East Chicago Avenue, Chicago, IL 60611, USA
J Physiol 553:445-56. 2003b>Phorbol esters and adenosine have been proposed to interact at common sites downstream of calcium entry at amphibian motor nerve endings... - Molecular characterization, reactivation, and depletion of latent HIVDavid G Brooks
Department of Microbiology, Immunology and Molecular Genetics, University of California, Los Angeles, Los Angeles, CA 90095, USA
Immunity 19:413-23. 2003..We demonstrate that activation of latent virus is required for targeting by antiviral agents and provide the basis for future therapeutic strategies to eradicate the latent reservoir... - Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entryMyriam Witvrouw
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
Antivir Chem Chemother 14:321-8. 2003..We concluded that prostratin inhibits the entry step of the replication cycle of HIV by interacting with a cellular target necessary for viral entry... - Regulated internalization and phosphorylation of the native norepinephrine transporter in response to phorbol esters. Evidence for localization in lipid rafts and lipid raft-mediated internalizationLankupalle D Jayanthi
Department of Physiology and Neuroscience, Medical University of South Carolina, Charleston, South Carolina 29425, USA
J Biol Chem 279:19315-26. 2004.... - A vascular gene trap screen defines RasGRP3 as an angiogenesis-regulated gene required for the endothelial response to phorbol estersDavid M Roberts
Curriculum in Genetics and Molecular Biology, Department of Biology, CB 3280, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Mol Cell Biol 24:10515-28. 2004..b>Phorbol esters mimic the second messenger diacylglycerol (DAG) in activating both protein kinase C (PKC) and non-PKC phorbol .. - Prostratin antagonizes HIV latency by activating NF-kappaBSamuel A Williams
Gladstone Institute of Virology and Immunology, University of California, San Francisco, San Francisco, California 94141, USA
J Biol Chem 279:42008-17. 2004..These findings provide new insights into the molecular pathway through which prostratin antagonizes HIV latency highlighting a central role for the action of NF-kappaB... - Inhibition of bovine immunodeficiency virus by anti-HIV-1 compounds in a cell culture-based assayG J Tobin
Laboratory of Cell and Molecular Structure, SAIC Frederick, MD, USA
Antiviral Res 33:21-31. 1996.... - Swelling-activated Ca2+ entry via TRPV4 channel is defective in cystic fibrosis airway epitheliaMaite Arniges
Laboratori de Fisiologia Molecular, Unitat de Senyalització Cellular, Universitat Pompeu Fabra, C Dr Aiguader 80, Barcelona 08003, Spain
J Biol Chem 279:54062-8. 2004..Together, these results suggest that defective RVD in CF airway epithelia might be caused by the absence of a TRPV4-mediated Ca(2+) signal and the subsequent activation of Ca(2+)-dependent K(+) channels... - Expression of latent HAART-persistent HIV type 1 induced by novel cellular activating agentsJoseph Kulkosky
Center for Human Virology and Biodefense, Division of Infectious Diseases and Environmental Medicine, Department of Medicine, Jefferson Medical College, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
AIDS Res Hum Retroviruses 20:497-505. 2004.... - Dual role of prostratin in inhibition of infection and reactivation of human immunodeficiency virus from latency in primary blood lymphocytes and lymphoid tissueAngelique Biancotto
Unité de Pathogénie des Infections à Lentivirus, Parc Scientifique et Technologique de Luminy, INSERM U372, Marseille, France
J Virol 78:10507-15. 2004.... - Mechanisms of HIV receptor and co-receptor down-regulation by prostratin: role of conventional and novel PKC isoformsMarjan Hezareh
AIDS Research Alliance, West Hollywood, Calif, USA
Antivir Chem Chemother 15:207-22. 2004..Altogether these results showed that prostratin, through the activation of conventional and/or novel PKC isoforms, rapidly reduces cell surface expression of CD4 and CXCR4, but not CCR5, by inducing their internalization and degradation... - Human immunodeficiency virus reactivation by phorbol esters or T-cell receptor ligation requires both PKCalpha and PKCthetaSergey A Trushin
Division of Infectious Diseases and Progam in Translational Immunology and Biodefense, Mayo Clinic College of Medicine, Rochester, MN 55905, USA
J Virol 79:9821-30. 2005..Antigens, T-cell receptor (TCR) ligation, and phorbol esters can reactivate HIV from latency in a protein kinase C (PKC)-dependent manner; however, it is unknown which .. - Activation of latent HIV-1 expression by the potent anti-tumor promoter 12-deoxyphorbol 13-phenylacetateSven Bocklandt
National Cancer Institute, NIH, 9000 Rockville Pike, Bethesda, MD 20892, USA
Antiviral Res 59:89-98. 2003..The combination of high potency and anti-tumor promoting activity make DPP an attractive candidate for the adjunctive therapy of persistent HIV-1 infection... - Substitution on the A-ring confers to bryopyran analogues the unique biological activity characteristic of bryostatins and distinct from that of the phorbol estersGary E Keck
Department of Chemistry, University of Utah, 315 South 1400 East, RM 2020, Salt Lake City, Utah 84112, USA
Org Lett 11:593-6. 2009..Biological assays reveal a crucial role for substitution in the bryostatin 1 A-ring in conferring those responses which are characteristic of bryostatin 1 and distinct from those observed with PMA... - Variability in content of the anti-AIDS drug candidate prostratin in Samoan populations of Homalanthus nutansHOLLY E JOHNSON
Institute for Ethnomedicine, Box 3464, Jackson, Wyoming 83001, USA
J Nat Prod 71:2041-4. 2008..The reversed-phase HPLC assay will allow plants to be selected for agricultural development and genetic analysis by identifying those individuals above and below a 95% confidence interval for the median concentration... - Phorbol esters modulate spontaneous and Ca2+-evoked transmitter release via acting on both Munc13 and protein kinase CXuelin Lou
Department of Membrane Biophysics, AG Synaptic Dynamics and Modulation, Max Planck Institute for Biophysical Chemistry, D 37077 Gottingen, Germany
J Neurosci 28:8257-67. 2008Diacylglycerol (DAG) and phorbol esters strongly potentiate transmitter release at synapses by activating protein kinase C (PKC) and members of the Munc13 family of presynaptic vesicle priming proteins... - Practical synthesis of prostratin, DPP, and their analogs, adjuvant leads against latent HIVPaul A Wender
Department of Chemistry, Stanford University, 337 Campus Drive, Stanford, CA 94305, USA
Science 320:649-52. 2008..This synthesis reliably supplies gram quantities of the therapeutically promising natural products, hitherto available only in low and variable amounts from natural sources, and opens access to a variety of new analogs... - Prostratin: activation of latent HIV-1 expression suggests a potential inductive adjuvant therapy for HAARTJ Kulkosky
Dorrance H Hamilton Laboratories, Center for Human Virology, Division of Infectious Diseases, Department of Medicine, Jefferson Medical College, Thomas Jefferson University, Philadelphia, PA 19107, USA
Blood 98:3006-15. 2001..This novel observation suggests the agent may be an excellent candidate to augment HAART by inducing expression of latent HIV-1 with the ultimate goal of eliminating persistent viral reservoirs in certain individuals infected with HIV-1... - Factor recruitment and TIF2/GRIP1 corepressor activity at a collagenase-3 response element that mediates regulation by phorbol esters and hormonesI Rogatsky
Department of Cellular and Molecular Pharmacology, University of California, 513 Parnassus Avenue, HSW1201, San Francisco, CA 94143 0450, USA
EMBO J 20:6071-83. 2001..col3A, associated with the collagenase-3 gene in human U2OS osteosarcoma cells; col3A confers activation by phorbol esters, and repression by glucocorticoid and thyroid hormones... - Protein kinase C and other diacylglycerol effectors in cancerErin M Griner
Department of Pharmacology and Institute for Translational Medicine and Therapeutics ITMAT, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
Nat Rev Cancer 7:281-94. 2007.... - A novel functional target for tumor-promoting phorbol esters and lysophosphatidic acid. The p21rac-GTPase activating protein n-chimaerinS Ahmed
Institute of Molecular and Cell Biology, National University of Singapore
J Biol Chem 268:10709-12. 1993b>Phorbol esters are potent tumor promoters widely used for investigating mechanisms of cell transformation with protein kinase C (PKC) generally considered as being their only protein target... - Prostratin as a new therapeutic agent targeting HIV viral reservoirsMarjan Hezareh
AIDS Research Alliance, West Hollywood, California, USA
Drug News Perspect 18:496-500. 2005..Prostratin represents a distinct subclass of protein kinase C activators, since unlike other phorbol esters it does not induce tumor formation... - High-frequency epigenetic repression and silencing of retroviruses can be antagonized by histone deacetylase inhibitors and transcriptional activators, but uniform reactivation in cell clones is restricted by additional mechanismsRichard A Katz
Institute for Cancer Research, Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA 19111, USA
J Virol 81:2592-604. 2007..We conclude that HDACs can act rapidly to initiate and maintain promoter-independent retroviral epigenetic repression and silencing but that reactivation can be restricted by additional mechanisms... - Effects of prostratin on T-cell activation and human immunodeficiency virus latencyYael D Korin
Department of Medicine, UCLA School of Medicine, and UCLA AIDS Institute, 90095-1678, USA
J Virol 76:8118-23. 2002.... - Effects of prostratin on Cyclin T1/P-TEFb function and the gene expression profile in primary resting CD4+ T cellsTzu Ling Sung
Department of Molecular Virology and Microbiology, Baylor College of Medicine, Houston, Texas 77030, USA
Retrovirology 3:66. 2006..We also examined effects of prostratin on Cyclin T2a, an alternative regulatory subunit for CDK9, and 7SK snRNA and the HEXIM1 protein, two factors that associate with P-TEFb and repress its kinase activity... - Distinct protein kinase C isoforms mediate regulation of vascular endothelial growth factor expression by A2A adenosine receptor activation and phorbol esters in pheochromocytoma PC12 cellsAlicia M Gardner
Department of Pharmacology and Cell Biophysics, College of Medicine, University of Cincinnati, Cincinnati, Ohio 45267 0575, USA
J Biol Chem 278:15421-8. 2003..Together, the findings suggest that phorbol ester-induced down-regulation of VEGF mRNA occurs as a result of a reduction of PKCepsilon activity, whereas that mediated by the A(2A)AR occurs following deactivation of PKCzeta... - Move over protein kinase C, you've got company: alternative cellular effectors of diacylglycerol and phorbol estersNils Brose
Abteilung Molekulare Neurobiologie, Max Planck Institut fur experimentelle Medizin, D 37075 Gottingen, Germany
J Cell Sci 115:4399-411. 2002..The most prominent intracellular targets of diacylglycerol and of the functionally analogous phorbol esters belong to the protein kinase C (PKC) family... - Phorbol esters and related analogs regulate the subcellular localization of beta 2-chimaerin, a non-protein kinase C phorbol ester receptorM J Caloca
Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
J Biol Chem 276:18303-12. 2001..We have previously shown that, like PKCs, beta2-chimaerin binds phorbol esters with high affinity in a phospholipid-dependent manner (Caloca, M. J., Fernandez, M. N., Lewin, N. E., Ching, D... - Phorbol esters affect skeletal muscle glucose transport in a fiber type-specific mannerDavid C Wright
Department of Medicine, Washington University School of Medicine, St. Louis, Missouri 63110, USA
Am J Physiol Endocrinol Metab 287:E305-9. 2004..However, earlier studies demonstrated that phorbol esters increase glucose transport in skeletal muscle... - Tyrosine phosphorylation of p130(cas) by bombesin, lysophosphatidic acid, phorbol esters, and platelet-derived growth factor. Signaling pathways and formation of a p130(cas)-Crk complexA Casamassima
Imperial Cancer Research Fund, P O Box 123, 44 Lincoln s Inn Fields, London WC2A 3PX, United Kingdom
J Biol Chem 272:9363-70. 1997..Thus, our results identified distinct signal transduction pathways that lead to tyrosine phosphorylation of p130(cas) in the same cells and suggest that p130(cas) could play a role in mitogen-mediated signal transduction... - Protein kinase C-dependent and -independent inhibition of Ca(2+) influx by phorbol ester in rat pancreatic beta-cellsJ Nakamura
Department of Physiology, Hirosaki University School of Medicine, 5 Zaifu-cho, 036-8562, Hirosaki, Japan
Cell Signal 13:199-205. 2001b>Phorbol esters were used to investigate the action of protein kinase C (PKC) on insulin secretion from pancreatic beta-cells... - Opposing effects of calcium entry and phorbol esters on fusion of chick muscle cellsM Rapuano
Cellular and Developmental Biology Program, State University of New York, Stony Brook 11794
Dev Biol 134:271-8. 1989..We have investigated the effects of Ca2+ channel modulators and phorbol esters on fusion of embryonic chick myoblasts in culture... - Phorbol esters: structure, biological activity, and toxicity in animalsGunjan Goel
Institute for Animal Production in the Tropics and Subtropics, University of Hohenheim, Stuttgart, Germany
Int J Toxicol 26:279-88. 2007b>Phorbol esters are the tetracyclic diterpenoids generally known for their tumor promoting activity... - Different pathways of calcium sensitization activated by receptor agonists and phorbol esters in vascular smooth muscleM Hori
Department of Veterinary Pharmacology, Faculty of Agriculture, University of Tokyo, Japan
Br J Pharmacol 110:1527-31. 19931. It has been shown that receptor agonists and activators of protein kinase C, phorbol esters, increase Ca2+ sensitivity of contractile elements in vascular smooth muscle... - Selective binding of phorbol esters and diacylglycerol by individual C1 domains of the PKD familyJun Chen
Department of Pharmacology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA
Biochem J 411:333-42. 2008..The twin C1 domains of PKD, designated C1a and C1b, have been shown to bind DAG or phorbol esters. However, their ligand-binding activities and selectivities have not been fully characterized... - A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1K R Gustafson
Laboratory of Drug Discovery Research and Development, National Cancer Institute NCI, Frederick Cancer Research and Development Center FCRDC, Maryland 21702 1201
J Med Chem 35:1978-86. 1992..to and activated protein kinase C in vitro in CEM-SS cells and elicited other biochemical effects typical of phorbol esters in C3H10T1/2 cells; however, the compound does not appear to be a tumor promoter... - Adapter molecule DOC-2 is differentially expressed in pressure and volume overload hypertrophy and inhibits collagen synthesis in cardiac fibroblastsDeepa H Kumbar
The Heart Institute for Children, Advocate Hope Children s Hospital, Oak Lawn, IL, USA
J Appl Physiol 102:2024-32. 2007..Results suggest a role of DOC-2 in cardiac remodeling involving collagen expression during chronic hemodynamic overload... - Calcium-dependent interactions of the human norepinephrine transporter with syntaxin 1AUhna Sung
Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
Mol Cell Neurosci 34:251-60. 2007..Furthermore, PMA enhanced Ca2+-dependent modulation of NE transport in synaptosomes. Our data reveal roles for SYN1A in the Ca2+-dependent regulation of NET, likely reliant on regulation by PKC signaling, but independent of CaMK... - Hyperoxia alters phorbol ester-induced phospholipase D activation in bovine lung microvascular endothelial cellsShukla Roy
Department of Pulmonary and Critical Care Medicine, Department of Medicine, Johns Hopkins University, Baltimore, MD 21224, USA
Antioxid Redox Signal 5:217-28. 2003..As protein tyrosine phosphorylation and PLD play important roles in inflammatory responses, this could provide a mechanism for the regulation of endothelial barrier function during hyperoxic lung injury... - Integration of DAG signaling systems mediated by PKC-dependent phosphorylation of RasGRP3Christine Teixeira
Department of Biochemistry, University of Alberta, Edmonton, Canada
Blood 102:1414-20. 2003..of Ras activators have C1 domains that bind diacylglycerol (DAG) and DAG analogs such as the tumor-promoting phorbol esters. RasGRP members could be responsible for some of the DAG signaling processes that have previously been .. - Effect of protein kinase C activation and inhibition on rat hepatic stellate cell activationGrant A Ramm
Division of Gastroenterology and Hepatology, Department of Internal Medicine, Saint Louis University School of Medicine, St. Louis, Missouri 63110-0250, USA
Dig Dis Sci 48:790-6. 2003..The demonstration that hepatic stellate cell activation can be suppressed by PKC inhibitors suggests a role for PKC in the regulation of hepatic stellate cell activation... - Tumor necrosis factor-alpha converting enzyme is processed by proprotein-convertases to its mature form which is degraded upon phorbol ester stimulationKristina Endres
Institute of Biochemistry, Johannes Gutenberg University, Mainz, Germany
Eur J Biochem 270:2386-93. 2003.... - Requirement of AMPA receptor GluR2 phosphorylation for cerebellar long-term depressionHee Jung Chung
Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205 USA
Science 300:1751-5. 2003..In contrast, transfection with a point mutant that mimicked phosphorylation at Ser880 occluded subsequent LTD. Thus, PKC phosphorylation of GluR2 Ser880 is a critical event in the induction of cerebellar LTD... - Regulation of HERG potassium channel activation by protein kinase C independent of direct phosphorylation of the channel proteinDierk Thomas
Department of Cardiology, Medical University Hospital Heidelberg, Bergheimerstrasse 58, D 69115 Heidelberg, Germany
Cardiovasc Res 59:14-26. 2003..The aim of the present study was to elucidate the biochemical pathways of the protein kinase C (PKC)-dependent regulation of HERG currents... - Inhibition of the renal betaine transporter by calcium ionsStephen A Kempson
Department of Cellular and Integrative Physiology, Indiana University School of Medicine, Indianapolis, Indiana, USA
Am J Physiol Renal Physiol 291:F305-13. 2006..Amino acid transport system A, assayed as a control, was not inhibited. Brief treatment with phorbol esters reproduced the specific inhibition of Na(+)-GABA cotransport, and the inhibition was blocked by staurosporine... - Phorbol ester induces CYP2E1 in astrocytes, through a protein kinase C- and tyrosine kinase-dependent mechanismNiclas Tindberg
Division of Molecular Toxicology, Institute of Environmental Medicine, Karolinska Institutet, Stockholm, Sweden
J Neurochem 86:888-95. 2003..g. cerebral injury, cytokines or phorbol ester, and mediated in part through protein kinase C... - The cytosolic II-III loop of Cav2.3 provides an essential determinant for the phorbol ester-mediated stimulation of E-type Ca2+ channel activityUdo Klockner
Institute of Vegetative Physiology, University of Cologne, Germany
Eur J Neurosci 19:2659-68. 2004..3 was eliminated. Receptor independent stimulation of PKC and its interaction with Ca(v)2.3 channels therefore represents an important positive feedback mechanism to decode electrical signals into a variety of cellular functions... - Dramatic switching of protein kinase C agonist/antagonist activity by modifying the 12-ester side chain of phorbol estersReiko Wada
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo 113-0033, Japan
J Am Chem Soc 124:10658-9. 2002..The approach of controlling the agonist/antagonist activity of phorbol esters by the nature (i.e., hydrophilicity, charge, and rigidity, etc... - Zinc release from protein kinase C as the common event during activation by lipid second messenger or reactive oxygenIrina Korichneva
Program in Immunology, Memorial Sloan Kettering Cancer Center, New York, New York 10021, USA
J Biol Chem 277:44327-31. 2002..kinase C (PKC) activation involving either the lipid second messengers (diacylglycerol and its mimetics, the phorbol esters) or reactive oxygen converge at the zinc finger of the regulatory domain... - The impact of phorbol ester on the regulation of amiloride-sensitive epithelial sodium channel in alveolar type ii epithelial cellsToshiyuki Yamagata
Third Department of Internal Medicine, Wakayama Medical University, Wakayama City, Wakayama, Japan
Exp Lung Res 28:543-62. 2002..These results suggest that an activation of PKC may play an important role in the regulation of ENaC mRNA expression and function... - Neurokinin 2 receptor-mediated activation of protein kinase C modulates capsaicin responses in DRG neurons from adult ratsAdrian Sculptoreanu
Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA, USA
Eur J Neurosci 27:3171-81. 2008..Thus, activation of NK2 autoreceptors by NKs released from the peripheral afferent terminals or by mast cells during inflammatory responses may be a mechanism that sensitizes TRPV1 channels and enhances afferent excitability... - Chlorpromazine inhibits the glucocorticoid receptor-mediated gene transcription in a calcium-dependent mannerA Basta-Kaim
Department of Endocrinology, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31 343 Krakow, Poland
Neuropharmacology 43:1035-43. 2002..The inhibitory effect of chlorpromazine on the corticosterone-induced gene transcription seems to depend on the inhibition of Ca(2+) influx and/or the inhibition of some calcium-dependent enzymes, e.g. phospholipase beta(1)... - Role of specific protein kinase C isozymes in mediating epidermal growth factor, thyrotropin-releasing hormone, and phorbol ester regulation of the rat prolactin promoter in GH4/GH4C1 pituitary cellsCheryl A Pickett
Department of Medicine, Division of Metabolism, Endocrinology and Nutrition, University of Washington School of Medicine, 1959 NE Pacific Street, Seattle, WA 98195 6426, USA
Mol Endocrinol 16:2840-52. 2002..Inhibitor data suggest that the EGF response may also involve Ca(2+)-dependent isozymes, whereas the TRH response appears to be more dependent on diacylglycerol... - Cholecystokinin stimulates extracellular signal-regulated kinase through activation of the epidermal growth factor receptor, Yes, and protein kinase C. Signal amplification at the level of Raf by activation of protein kinase CepsilonAlbrecht Piiper
Department of Internal Medicine II, University of the Saarland, D 66421 Homburg Saar, Germany
J Biol Chem 278:7065-72. 2003.... - The chaperone protein 14-3-3 interacts with 3BP2/SH3BP2 and regulates its adapter functionIsabelle Foucault
INSERM U343 and Laboratoire d Immunologie, hôpital de l Archet I, Nice 06202, France
J Biol Chem 278:7146-53. 2003..Indeed, a 3BP2 mutant protein incapable of binding 14-3-3 showed increased capacity to stimulate NFAT transcriptional activities, suggesting that 14-3-3 binding to 3BP2 negatively regulates 3BP2 adapter function in lymphocytes... - Opposing effects of phorbol-12-myristate-13-acetate, an activator of protein kinase C, on the signaling of structurally related human dopamine D1 and D5 receptorsAdele Jackson
Ottawa Health Research Institute, Ottawa Hospital (Civic Campus, and Department of Medicine/Cellular and Molecular Medicine/Psychiatry, University of Ottawa, Ottawa, Ontario, Canada
J Neurochem 95:1387-400. 2005.... - The role of protein phosphorylation in alpha2,6(N)-sialyltransferase activityKieran C Breen
Department of Psychiatry, University of Dundee Medical School, Ninewells Hospital, UK
Biochem Biophys Res Commun 309:32-5. 2003..These results provide further evidence for the role of second messenger-associated kinase enzymes in the modulation of the cell glycosylation potential... - PKC activates BKCa channels in rat pulmonary arterial smooth muscle via cGMP-dependent protein kinaseScott A Barman
Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta, GA 30912, USA
Am J Physiol Lung Cell Mol Physiol 286:L1275-81. 2004.... - Repression of 5-aminolevulinate synthase gene by the potent tumor promoter, TPA, involves multiple signal transduction pathwaysAlejandra S Guberman
Departamento de Quimica Biologica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellon II Piso 4, Ciudad Universitaria, 1428 Buenos Aires, Argentina
Arch Biochem Biophys 436:285-96. 2005..Finally, by overexpression of a constitutively active p90RSK and the coactivator, cAMP-response element protein (CREB)-binding protein (CBP), we reinforced our previous model, that implies competition between AP-1 and CREB for CBP... - Phosphorylation of histone deacetylase 7 by protein kinase D mediates T cell receptor-induced Nur77 expression and apoptosisFranck Dequiedt
Cellular and Molecular Biology Unit, Faculty of Agronomy, B 5030 Gembloux, Belgium
J Exp Med 201:793-804. 2005..These findings indicate that PKD is likely to play a key role in the signaling pathways controlling negative selection... - A role for ERK1/2 in EGF- and ATP-dependent regulation of amiloride-sensitive sodium absorptionRebecca Falin
Case Western Reserve Univ, 2109 Adelbert Rd, Cleveland, OH 44106-4948, USA
Am J Physiol Cell Physiol 288:C1003-11. 2005.... - Differential regulation of GLAST immunoreactivity and activity by protein kinase C: evidence for modification of amino and carboxyl terminiBala T S Susarla
Department of Pediatrics, University of Pennsylvania and Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, USA
J Neurochem 91:1151-63. 2004.... - Protein kinase C-mediated phosphorylation of the leukemia-associated HOXA9 protein impairs its DNA binding ability and induces myeloid differentiationUlka Vijapurkar
Department of Medicine, University of California VA Medical Center, San Francisco, California 94121, USA
Mol Cell Biol 24:3827-37. 2004..These data suggest that phorbol ester-induced myeloid differentiation is in part due to PKC-mediated phosphorylation of HOXA9, which decreases the DNA binding of the homeoprotein... - Phorbol ester-induced differentiation of L6 myogenic cells involves phospholipase D activationHiba Komati
Laboratoire de Physiopathologie des Lipides et Membranes, , , 69621 Villeurbanne, France
FEBS Lett 577:409-14. 2004..TPA-induced differentiation was inhibited by 1-butanol, confirming the involvement of PLD in this effect. These data suggest that prolonged elevation of PLD activity is required for myogenic differentiation... - Activation of arylalkylamine N-acetyltransferase by phorbol esters in bovine pinealocytes suggests a novel regulatory pathway in melatonin synthesisC Schomerus
Dr Senckenbergische Anatomie, Institut für Anatomie II, Johann Wolfgang Goethe Universitat Frankfurt, Frankfurt, Germany
J Neuroendocrinol 16:741-9. 2004..Other compounds which are known to influence the melatonin-generating system are phorbol esters. The effect of phorbol esters on regulation of melatonin synthesis has been mainly investigated in rat .. - Receptor activator of nuclear factor-kappaB is induced by a rottlerin-sensitive and p38 MAP kinase-dependent pathway during monocyte differentiationHong Soon Kang
Skeletal Diseases Genome Research Center, Kyungpook National University Hospital, Kyungpook National University, Daegu 700 412, Korea
Mol Cells 17:438-45. 2004..Together, these results demonstrate that expression of RANK is dependent upon a rottlerin-sensitive and p38MAPK-dependent pathway during monocyte differentiation... - Combined action of extracellular signal-regulated kinase and p38 kinase rescues Molt4 T cells from nitric oxide-induced apoptotic and necrotic cell deathHyun Mee Oh
Department of Microbiology and Immunology, Wonkwang University School of Medicine, Iksan, Chonbuk 570 749, South Korea
Free Radic Biol Med 37:463-79. 2004..Together, these findings suggest that the PMA-induced activations of ERK and p38 kinase are parallel events that are both required for inhibition of NO-induced death of Molt4 cells... - Evidence that protein kinase Cdelta is not required for palmitate-induced cytotoxicity in BRIN-BD11 beta-cellsH J Welters
Institute of Biomedical and Clinical Science, Peninsula Medical School, Plymouth, Devon, PL6 8BX, UK
J Mol Endocrinol 32:227-35. 2004..However, it is clear that PKCdelta is not required for this response... - Studies on regulation of IGF (insulin-like growth factor)-binding protein (IGFBP) 4 proteolysis by pregnancy-associated plasma protein-A (PAPP-A) in cells treated with phorbol esterArun S Sivanandam
Musculoskeletal Disease Center, J L Pettis Memorial Veterans Medical Center, 11201 Benton Street, Loma Linda, CA 92357, USA
Biochem J 379:57-64. 2004..These data suggest that a novel mechanism, namely conversion of PAPP-A470 to the less-active PAPP-A400, could account for the TPA-induced suppression of PAPP-A activity... - Phorbol ester-dependent activation of peroxiredoxin I gene expression via a protein kinase C, Ras, p38 mitogen-activated protein kinase signaling pathwayAlexander Hess
Institut fur Klinische Chemie und Pathobiochemie, Justus Liebig Universitat Giessen, Giessen D 35392, Germany
J Biol Chem 278:45419-34. 2003..The data indicate that a protein kinase C, Ras, MEKK1, p38 MAPK signaling pathway plays a major role for the transcriptional up-regulation of Prx I gene expression... - Shp2 is required for protein kinase C-dependent phosphorylation of serine 307 in insulin receptor substrate-1Karsten Müssig
Division of Endocrinology, Metabolism, and Pathobiochemistry, Department of Internal Medicine, University Hospital of Tubingen, Tubingen 72076, Germany
J Biol Chem 280:32693-9. 2005..Because the activation of these kinases does not depend on Shp2, it is concluded that the function of Shp2 is to direct these activated kinases to IRS-1... - Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4Feng Xu
Department of Pharmacology, Akita University School of Medicine, 1-1-1 Hondoh, Akita 010-8543, Japan
Br J Pharmacol 140:413-21. 2003..7 nm. Exposure to a hypotonic solution (HTS) after PMA further increased [Ca2+]i. Two other PKC-activating phorbol esters, phorbol 12,13-didecanoate (PDD) and phorbol 12,13-dibutyrate, also caused [Ca2+]i to increase. 3... - Cytotoxic action of phorbol esters on human pancreatic cancer cellsJane A Bond
Department of Pathology, School of Medicine, Cardiff University, Cardiff CF14 4XN, United Kingdom
Int J Cancer 121:1445-54. 2007We previously showed that phorbol esters are cytotoxic to human thyroid epithelial cells expressing a mutant RAS oncogene... - Desensitization of nicotine acetylcholine receptors: modulation by kinase activation and phosphatase inhibitionWilliam Marszalec
Department of Molecular Pharmacology and Biological Chemistry, Northwestern University Medical School, 303 E. Chicago Avenue, Chicago, IL 60611-3008, USA
Eur J Pharmacol 514:83-90. 2005..Protein kinase C activation or phosphatase 2B inhibition may favor the D1 receptor state over that of D2 to promote faster overall rates of desensitization recovery... - Direct, rapid effects of 25-hydroxyvitamin D3 on isolated intestinal cellsRuta Phadnis
Department of Nutrition and Food Sciences and the Biotechnology Center, Utah State University, Logan, Utah 84322-8700, USA
J Cell Biochem 90:287-93. 2003..We conclude that 25(OH)D(3) has a direct effect on calcium handling in enterocytes of young animals that may in part be mediated by the protein kinase A signal transduction pathway... - IL-4-dependent CD86 expression requires JAK/STAT6 activation and is negatively regulated by PKCdeltaEric L Deszo
Department of Animal Sciences, College of Agriculture, Consumer and Environmental Sciences, 1207 West Gregory Dr, University of Illinois at Urbana Champaign, Urbana, IL 61801, USA
Cell Signal 16:271-80. 2004..We conclude from these data that IL-4-dependent CD11b expression relies predominantly on enhanced activation of ERK1/2, while IL-4-dependent CD86 expression utilizes the JAK/STAT6 pathway... - Ca2+-dependent protein kinase C isoforms induce cholestasis in rat liverRalf Kubitz
Department of Gastroenterology, Hepatology, and Infectiology, Heinrich Heine University, D 40225 Dusseldorf, Germany
J Biol Chem 279:10323-30. 2004..The data identify Ca(2+)-dependent PKC isoforms as inducers of cholestasis. This is mainly due to inhibition of taurocholate excretion involving transporter retrieval from the canalicular membrane... - Bidirectional regulation of renal cortical Na+,K+-ATPase by protein kinase CJerzy Bełtowski
Department of Pathophysiology, Medical University, Lublin, Poland
Acta Biochim Pol 51:757-72. 2004..The inhibitory effect is mediated by cytochrome P450-dependent arachidonate metabolites and PI3K, and is caused by redistribution of the sodium pump from the plasma membrane to the inactive intracellular pool... - Inhibition of human p53 basal transcription by down-regulation of protein kinase CdeltaTarek Abbas
Institute for Biomolecular Structure and Function and Department of Biological Sciences, Hunter College and Graduate School, City University of New York, New York 10021, USA
J Biol Chem 279:9970-7. 2004..kinase C (PKC) delta has been implicated as a tumor suppressor that is down-regulated by tumor-promoting phorbol esters in both mouse skin and cell culture models... - Depolarization of skeletal muscle cells induces phosphorylation of cAMP response element binding protein via calcium and protein kinase CalphaCesar Cardenas
Centro de Estudios Moleculares de la Célula, Instituto de Ciencias Biomedicas, Facultad de Medicina, Universidad de Chile, Independencia 1027, Santiago 7, Chile
J Biol Chem 279:39122-31. 2004..These results strongly implicate nuclear PKCalpha translocation in CREB phosphorylation induced by skeletal muscle membrane depolarization... - Activation of Ras, Raf-1 and protein kinase C in differentiating human neuroblastoma cells after treatment with phorbolester and NGFH Söderholm
Tumour Biology, Department of Genetics and Pathology, The Rudbeck Laboratory, Uppsala University, SE 751 85, Uppsala, Sweden
Cell Signal 13:95-104. 2001..The results identify Raf-1 as a target for both TPA- and NGF-induced signals in differentiating SH-SY5Y/TrkA cells and demonstrate that signalling to Raf-1 was mediated via distinct mechanisms... - Interdependence of PKC-dependent and PKC-independent pathways for presynaptic plasticityKeimpe D B Wierda
Department of Functional Genomics, Center for Neurogenomics and Cognitive Research, Vrije Universiteit Amsterdam, The Netherlands
Neuron 54:275-90. 2007..Munc18-1 is an essential downstream target in the PKC pathway. This pathway is of general importance for presynaptic plasticity... - Diacylglycerol generated by exogenous phospholipase C activates the mitogen-activated protein kinase pathway independent of Ras- and phorbol ester-sensitive protein kinase C: dependence on protein kinase C-zetaM van Dijk
Division of Cellular Biochemistry, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
Biochem J 323:693-9. 1997..The results suggest that DG generated by PC-PLC can activate the MAPK pathway independent of Ras and phorbol-ester-sensitive PKC but, instead, via PKC-zeta... - Phorbol esters modulate the Ras exchange factor RasGRP3P S Lorenzo
Laboratory of Cellular Carcinogenesis and Tumor Promotion, National Cancer Institute, Bethesda, Maryland 20892 4255, USA
Cancer Res 61:943-9. 2001..We show here that RasGRP3 bound phorbol esters with high affinity... - Subtype-specific translocation of the delta subtype of protein kinase C and its activation by tyrosine phosphorylation induced by ceramide in HeLa cellsT Kajimoto
Laboratory of Molecular Pharmacology, Biosignal Research Center, Kobe University, Nada-ku, Kobe 657-8501, Japan
Mol Cell Biol 21:1769-83. 2001.... - Chromaffin cell F-actin disassembly and potentiation of catecholamine release in response to protein kinase C activation by phorbol esters is mediated through myristoylated alanine-rich C kinase substrate phosphorylationS D Rose
Secretory Process Research Program, Department of Cellular and Molecular Medicine, Faculty of Medicine, University of Ottawa, Ottawa, Ontario K1H 8M5, Canada
J Biol Chem 276:36757-63. 2001..These results provide the first evidence for MARCKS involvement in chromaffin cell secretion and suggest that regulation of cortical F-actin cross-linking might be involved in this process... - Involvement of multiple protein kinase C isozymes in the ACTH secretory pathway of AtT-20 cellsB W McFerran
Molecular Endocrinology Unit, School of Biological and Medical Sciences, University of St Andrews
Br J Pharmacol 115:307-15. 1995..The beta isozyme of PKC may act ata stage early in the secretory pathway to regulate the cytosolic calcium concentration... - Stimulatory effect of a phorbol ester on expression of insulin-like growth factor (IGF) binding protein-2 and level of IGF-I receptors in mouse osteoblastic MC3T3-E1 cellsY Hakeda
Department of Oral Anatomy, Meikai University School of Dentistry, Saitama, Japan
J Cell Physiol 158:444-50. 1994..These results indicate that the production of IGF-I and the expression of IGF-I receptors and IGFBP-2 are up-regulated by the activation of adenylate cyclase and protein kinase C, respectively, in osteoblastic MC3T3-E1 cells... - Proteasome implication in phorbol ester- and GnRH-induced selective down-regulation of PKC (alpha, epsilon, zeta) in alpha T(3)-1 and L beta T(2) gonadotrope cell linesBrice Junoy
Centre National de la Recherche Scientifique UMR 6544, , , 13916 Marseille, France
Endocrinology 143:1386-403. 2002..Thus, the proteasome system by adjusting PKC cellular levels, may represent a regulatory proteolytic pathway implicated in the adaptive mechanisms of the time dependent cell responses... - Mesangial cell filamentous actin disassembly and hypocontractility in high glucose are mediated by PKC-zetaJohn A Dlugosz
Institute of Medical Science and Department of Medicine, University of Toronto, Toronto, Ontario, Canada
Am J Physiol Renal Physiol 282:F151-63. 2002..In HG, altered F-actin and contractile functions in MCs are mediated by PKC-zeta... - LPA is a novel lipid regulator of mesangial cell hexokinase activity and HKII isoform expressionPlatina E Coy
Section of Nephrology, Department of Medicine, University of Illinois at Chicago College of Medicine, Chicago, Illinois 60612-7315, USA
Am J Physiol Renal Physiol 283:F271-9. 2002..They also suggest a novel mechanism whereby metabolism may be coupled to cellular injury via extracellular lipid mediators... - P2X7 receptors activate protein kinase D and p42/p44 mitogen-activated protein kinase (MAPK) downstream of protein kinase CMichelle D Bradford
Division of Signal Transduction, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Institutes of Medicine, MA 02215, USA
Biochem J 366:745-55. 2002....
Research Grants
- ARACHIDONATE METABOLISM IN BLOOD AND VASCULAR CELLSKenneth Wu; Fiscal Year: 2002..promoter which is switched to a more powerful distal promoter when cells are stimulated by cytokines and phorbol esters, (2) Aspirin suppresses the distal promoter activity of PGHS-1 gene...
- Activation of HTLV1 Gene Expression and OncogenesisArnold Rabson; Fiscal Year: 2006..infected cell lines by treatment with immune activation related stimuli, such as phytohemagglutinin (PHA) and phorbol esters (PMA)...
- Regulation of Ovarian Cancer Multidrug Resistance by MAP KinasesScott T Eblen; Fiscal Year: 2010..phosphorylation in human ascites and in cell lines in response to chemotherapeutic drugs, oxidative stress, phorbol esters and UV irradiation...
- PKC/PKA Regulation in Prostate Cancer by SSeCKS/Gravin/AKAP12Irwin H Gelman; Fiscal Year: 2010Activation of protein kinase (PK) C has been considered cancer-promoting based on early data showing that phorbol esters could induce oncogenes is through the activation of so called classic and novel PKC isozymes...
- MECHANISMS OF MAMMALIAN FERTILIZATION/POLYSPERMY BLOCKGREGORY KOPF; Fiscal Year: 1990..eggs retain their sperm receptor activity, but have lost the ability to induce a complete acrosome reaction; phorbol esters activate protein kinase C...
- CELLULAR MECHANISMS IN THE INDUCTION OF AROMATASECAROLE MENDELSON; Fiscal Year: 1993..there are distinct tissue- specific differences in the actions of several other regulatory factors, including phorbol esters, and a number of growth factors and cytokines...
- Prostate carcinogenesis and PKC signalingMARCELO GABRIEL KAZANIETZ; Fiscal Year: 2010The phorbol esters are natural compounds with tumor promoter activity that have been instrumental to define the stages of mutagen-initiated multistage carcinogenesis...
- MOLECULAR BIOLOGY OF BILE ACID SYNTHESISJOHN CHIANG; Fiscal Year: 2001..and an activator region in the promoter have been mapped to contain elements responsive to bile acid, phorbol esters and retinoic acid. Yeast one-hybrid system will be used to isolate DNA-binding proteins isolated...
- PROTEIN KINASE C AND PHOTORECEPTORSALEXANDRA NEWTON; Fiscal Year: 2002..of retinas with dopamine alters the phosphorylation of rhodopsin in a similar manner as treatment with phorbol esters, potent protein kinase C activators...
- CELLULAR MECHANISMS IN THE INDUCTION OF AROMATASECAROLE MENDELSON; Fiscal Year: 1991..b>Phorbol esters potentiate the cyclic AMP induction of aromatase activity in human adipose stromal cells...