phorbol esters

Summary

Summary: 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

  1. ncbi Prostratin induces HIV activation and downregulates HIV receptors in peripheral blood lymphocytes
    Joaquín Rullas
    AIDS Immunopathogenesis Unit, Centro Nacional de Microbiologia, Instituto de Salud Carlos III, Madrid, Spain
    Antivir Ther 9:545-54. 2004
  2. ncbi Prostratin: activation of latent HIV-1 expression suggests a potential inductive adjuvant therapy for HAART
    J 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
  3. ncbi Prostratin antagonizes HIV latency by activating NF-kappaB
    Samuel 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
  4. ncbi Regulated internalization and phosphorylation of the native norepinephrine transporter in response to phorbol esters. Evidence for localization in lipid rafts and lipid raft-mediated internalization
    Lankupalle D Jayanthi
    Department of Physiology and Neuroscience, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Biol Chem 279:19315-26. 2004
  5. ncbi Phorbol esters: structure, biological activity, and toxicity in animals
    Gunjan Goel
    Institute for Animal Production in the Tropics and Subtropics, University of Hohenheim, Stuttgart, Germany
    Int J Toxicol 26:279-88. 2007
  6. ncbi Phorbol esters from Jatropha meal triggered apoptosis, activated PKC-δ, caspase-3 proteins and down-regulated the proto-oncogenes in MCF-7 and HeLa cancer cell lines
    Ehsan Oskoueian
    Department of Microbiology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia
    Molecules 17:10816-30. 2012
  7. ncbi HIV type 1 inhibition by protein kinase C modulatory compounds
    David Warrilow
    Division of Immunology and Infectious Disease, Queensland Institute of Medical Research, Brisbane, Queensland 4006, Australia
    AIDS Res Hum Retroviruses 22:854-64. 2006
  8. pmc Dual role of prostratin in inhibition of infection and reactivation of human immunodeficiency virus from latency in primary blood lymphocytes and lymphoid tissue
    Angelique Biancotto
    Unité de Pathogénie des Infections à Lentivirus, Parc Scientifique et Technologique de Luminy, INSERM U372, Marseille, France
    J Virol 78:10507-15. 2004
  9. ncbi Protein kinase C and other diacylglycerol effectors in cancer
    Erin 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
  10. pmc Factor recruitment and TIF2/GRIP1 corepressor activity at a collagenase-3 response element that mediates regulation by phorbol esters and hormones
    I 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

Research Grants

Detail Information

Publications210 found, 100 shown here

  1. ncbi Prostratin induces HIV activation and downregulates HIV receptors in peripheral blood lymphocytes
    Joaquín 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...
  2. ncbi Prostratin: activation of latent HIV-1 expression suggests a potential inductive adjuvant therapy for HAART
    J 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...
  3. ncbi Prostratin antagonizes HIV latency by activating NF-kappaB
    Samuel 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...
  4. ncbi Regulated internalization and phosphorylation of the native norepinephrine transporter in response to phorbol esters. Evidence for localization in lipid rafts and lipid raft-mediated internalization
    Lankupalle D Jayanthi
    Department of Physiology and Neuroscience, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Biol Chem 279:19315-26. 2004
    ....
  5. ncbi Phorbol esters: structure, biological activity, and toxicity in animals
    Gunjan Goel
    Institute for Animal Production in the Tropics and Subtropics, University of Hohenheim, Stuttgart, Germany
    Int J Toxicol 26:279-88. 2007
    b>Phorbol esters are the tetracyclic diterpenoids generally known for their tumor promoting activity...
  6. ncbi Phorbol esters from Jatropha meal triggered apoptosis, activated PKC-δ, caspase-3 proteins and down-regulated the proto-oncogenes in MCF-7 and HeLa cancer cell lines
    Ehsan Oskoueian
    Department of Microbiology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia
    Molecules 17:10816-30. 2012
    Jatropha meal produced from the kernel of Jatropha curcas Linn. grown in Malaysia contains phorbol esters (PEs). The potential benefits of PEs present in the meal as anticancer agent are still not well understood...
  7. ncbi HIV type 1 inhibition by protein kinase C modulatory compounds
    David Warrilow
    Division of Immunology and Infectious Disease, Queensland Institute of Medical Research, Brisbane, Queensland 4006, Australia
    AIDS Res Hum Retroviruses 22:854-64. 2006
    ..This result hints at the possibility of inhibition by a PKC modulatory compound of an early pathway of viral entry in PBMC...
  8. pmc Dual role of prostratin in inhibition of infection and reactivation of human immunodeficiency virus from latency in primary blood lymphocytes and lymphoid tissue
    Angelique Biancotto
    Unité de Pathogénie des Infections à Lentivirus, Parc Scientifique et Technologique de Luminy, INSERM U372, Marseille, France
    J Virol 78:10507-15. 2004
    ....
  9. ncbi Protein kinase C and other diacylglycerol effectors in cancer
    Erin 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
    ....
  10. pmc Factor recruitment and TIF2/GRIP1 corepressor activity at a collagenase-3 response element that mediates regulation by phorbol esters and hormones
    I 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...
  11. ncbi Phorbol esters modulate the Ras exchange factor RasGRP3
    P 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...
  12. pmc Effects of prostratin on T-cell activation and human immunodeficiency virus latency
    Yael D Korin
    Department of Medicine, UCLA School of Medicine, and UCLA AIDS Institute, 90095 1678, USA
    J Virol 76:8118-23. 2002
    ....
  13. ncbi Activation of arylalkylamine N-acetyltransferase by phorbol esters in bovine pinealocytes suggests a novel regulatory pathway in melatonin synthesis
    C 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 ..
  14. pmc Some phorbol esters might partially resemble bryostatin 1 in their actions on LNCaP prostate cancer cells and U937 leukemia cells
    Noemi Kedei
    Laboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892 4255, USA
    Chembiochem 12:1242-51. 2011
    ..Since phorbol ester lipophilicity influences PKCδ localization, we have examined in LNCaP cells a series of phorbol esters and related derivatives spanning some eight logs in lipophilicity (logP) to see if any behave like bryostatin ..
  15. ncbi Synthesis and phorbol ester binding of the cysteine-rich domains of diacylglycerol kinase (DGK) isozymes. DGKgamma and DGKbeta are new targets of tumor-promoting phorbol esters
    Mayumi Shindo
    Applied Biosystems Japan Ltd, 4 5 4 Hacchobori, Chuo Ku, Tokyo 104 0032, Japan
    J Biol Chem 278:18448-54. 2003
    ..Although most PKC C1 domains strongly bind phorbol esters, there has been no direct evidence that DGK C1 domains bind phorbol esters...
  16. ncbi Degradation of phorbol esters by Pseudomonas aeruginosa PseA during solid-state fermentation of deoiled Jatropha curcas seed cake
    Chetna Joshi
    Enzyme and Microbial Biochemistry Lab, Department of Chemistry, Indian Institute of Technology, Hauz Khas, New Delhi 110016, India
    Bioresour Technol 102:4815-9. 2011
    ..Presence of toxic phorbol esters restricts its utilization as livestock feed...
  17. ncbi Counteracting vasopressin-mediated water reabsorption by ATP, dopamine, and phorbol esters: mechanisms of action
    Michelle Boone
    Department of General and Environmental Physiology, University of Bari, Bari, Italy
    Am J Physiol Renal Physiol 300:F761-71. 2011
    ..Interestingly, phorbol esters only reduced AQP2 through the first pathway...
  18. ncbi A novel functional target for tumor-promoting phorbol esters and lysophosphatidic acid. The p21rac-GTPase activating protein n-chimaerin
    S Ahmed
    Institute of Molecular and Cell Biology, National University of Singapore
    J Biol Chem 268:10709-12. 1993
    b>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...
  19. ncbi Cytotoxic phorbol esters of Croton tiglium
    Xiao Long Zhang
    Key Laboratory of Mountain Ecological Restoration and Bioresource Utilization and Ecological Restoration Biodiversity Conservation, Key Laboratory of Sichuan Province, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, People s Republic of China
    J Nat Prod 76:858-64. 2013
    ..The cytotoxic activities of the phorbol diesters were evaluated against the SNU387 hepatic tumor cell line, and compound 3 exhibited the most potent activity (IC50 1.2 μM)...
  20. ncbi Are Jatropha curcas phorbol esters degraded by rumen microbes?
    Harinder P S Makkar
    Institute for Animal Production in the Tropics and Subtropics 480b, University of Hohenheim, Stuttgart, Germany
    J Sci Food Agric 90:1562-5. 2010
    ..However, the presence of highly toxic phorbol esters limits its use. Degradation of J...
  21. ncbi Phorbol esters inhibit the Hedgehog signalling pathway downstream of Suppressor of Fused, but upstream of Gli
    M Lauth
    Department of Biosciences and Nutrition, Karolinska Institutet, Novum Research Park, Huddinge, Sweden
    Oncogene 26:5163-8. 2007
    ....
  22. ncbi Toxicity of Jatropha curcas phorbol esters in mice
    Cai Yan Li
    College of Animal Science, Zhejiang University, 310029 Hangzhou, PR China
    Food Chem Toxicol 48:620-5. 2010
    b>Phorbol esters are the main toxins in Jatropha curcas seed and oil. The aim of this study was to assess the acute toxicity of phorbol esters given by intragastric administration and to determine the LD50 for Swiss Hauschka mice...
  23. ncbi PKA and PKC enhance excitatory synaptic transmission in human dentate gyrus
    Huan Xin Chen
    Department of Neurological Surgery and Evelyn F and William L McKnight Brain Institute, Gainesville, Florida 32610, USA
    J Neurophysiol 89:2482-8. 2003
    ..In addition, the occlusion experiments suggest that the two kinases may share a common signal pathway...
  24. ncbi Move over protein kinase C, you've got company: alternative cellular effectors of diacylglycerol and phorbol esters
    Nils 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...
  25. ncbi Isolation, stability and bioactivity of Jatropha curcas phorbol esters
    Joy S Roach
    Institute for Animal Production in the Tropics and Subtropics, 480b, University of Hohenheim, Stuttgart 70599, Germany
    Fitoterapia 83:586-92. 2012
    ..curcas seed oil, which can be utilized for biodiesel production upon transesterification, is also rich in phorbol esters (PEs). In this study, PEs from J...
  26. ncbi Swelling-activated Ca2+ entry via TRPV4 channel is defective in cystic fibrosis airway epithelia
    Maite 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...
  27. ncbi Defining the human targets of phorbol ester and diacylglycerol
    Markus Geiger
    Institute of Medical Chemistry and Biochemistry, University of Innsbruck, Fritz Pregistr 3, A 6020 Innsbruck, Austria
    Curr Opin Mol Ther 5:631-41. 2003
    b>Phorbol esters (PEs) and their derivatives are potent tumor-promoting agents...
  28. ncbi Molecular characterization, reactivation, and depletion of latent HIV
    David 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...
  29. ncbi Selective binding of phorbol esters and diacylglycerol by individual C1 domains of the PKD family
    Jun 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...
  30. pmc The structural requirements for phorbol esters to enhance serotonin and acetylcholine release from rat brain cortex
    L 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; ..
  31. ncbi Prostratin and bortezomib are novel inducers of latent Kaposi's sarcoma-associated herpesvirus
    Helen J Brown
    Department of Microbiology, Immunology and Molecular Genetics, UCLA, Los Angeles, CA, USA
    Antivir Ther 10:745-51. 2005
    ....
  32. pmc Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta
    Sung 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. 2008
    C1 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...
  33. ncbi Modulation of the transient receptor potential vanilloid channel TRPV4 by 4alpha-phorbol esters: a structure-activity study
    Thomas 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. 2009
    The 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-..
  34. ncbi Phorbol esters induce intracellular accumulation of the anti-apoptotic protein PED/PEA-15 by preventing ubiquitinylation and proteasomal degradation
    Anna 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 ..
  35. pmc Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone
    Elizabeth R Sharlow
    Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, Pennsylvania 15261, USA
    J Biol Chem 283:33516-26. 2008
    ..In summary, our findings indicate that CID755673 is a potent and selective PKD1 inhibitor with valuable pharmacological and cell biological potential...
  36. pmc Molecular cloning and characterization of protein kinase D: a target for diacylglycerol and phorbol esters with a distinctive catalytic domain
    A M Valverde
    Imperial Cancer Research Fund, London, United Kingdom
    Proc Natl Acad Sci U S A 91:8572-6. 1994
    A serine/threonine protein kinase that binds phorbol esters and diacylglycerol (named protein kinase D, PKD) has been identified...
  37. ncbi Antimycobacterial activity of phorbol esters from the fruits of Sapium indicum
    Parinuch Chumkaew
    Department of Chemistry, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand
    J Nat Prod 66:540-3. 2003
    Three 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-..
  38. pmc 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. 2003
    This review focuses on the effects of phorbol esters and the role of phorbol ester receptors in the secretion of neurotransmitter substances...
  39. pmc Phorbol esters and adenosine affect the readily releasable neurotransmitter pool by different mechanisms at amphibian motor nerve endings
    T 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. 2003
    b>Phorbol esters and adenosine have been proposed to interact at common sites downstream of calcium entry at amphibian motor nerve endings...
  40. ncbi Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entry
    Myriam 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...
  41. ncbi Activation of latent HIV-1 expression by the potent anti-tumor promoter 12-deoxyphorbol 13-phenylacetate
    Sven 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...
  42. ncbi Mechanisms of HIV receptor and co-receptor down-regulation by prostratin: role of conventional and novel PKC isoforms
    Marjan 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...
  43. pmc Variability in content of the anti-AIDS drug candidate prostratin in Samoan populations of Homalanthus nutans
    HOLLY 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...
  44. pmc A vascular gene trap screen defines RasGRP3 as an angiogenesis-regulated gene required for the endothelial response to phorbol esters
    David 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 ..
  45. pmc Effects of prostratin on Cyclin T1/P-TEFb function and the gene expression profile in primary resting CD4+ T cells
    Tzu 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...
  46. ncbi Phorbol esters modulate spontaneous and Ca2+-evoked transmitter release via acting on both Munc13 and protein kinase C
    Xuelin 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. 2008
    Diacylglycerol (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...
  47. pmc Human immunodeficiency virus reactivation by phorbol esters or T-cell receptor ligation requires both PKCalpha and PKCtheta
    Sergey 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 ..
  48. pmc Role of the regulatory domain of protein kinase D2 in phorbol ester binding, catalytic activity, and nucleocytoplasmic shuttling
    Alexandra Auer
    Department of Internal Medicine l, Medical University of Ulm, Ulm 89081, Germany
    Mol Biol Cell 16:4375-85. 2005
    Protein kinase D2 (PKD2) belongs to the PKD family of serine/threonine kinases that is activated by phorbol esters and G protein-coupled receptors (GPCRs)...
  49. ncbi Differential effects of phorbol-13-monoesters on human immunodeficiency virus reactivation
    Nieves Marquez
    Departamento de Biologia Celular, Fisiologia e Inmunologia, Facultad de Medicina, Avda de Menendez Pidal s n, 14004 Universidad de Córdoba, Spain
    Biochem Pharmacol 75:1370-80. 2008
    ..Nevertheless, this compound induces a translocation pattern of the PKC isotypes alpha and delta to cellular compartments distinctly different from that elicited by prostratin and PMA...
  50. ncbi Dramatic switching of protein kinase C agonist/antagonist activity by modifying the 12-ester side chain of phorbol esters
    Reiko 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...
  51. ncbi 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 phosphorylation
    S 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...
  52. ncbi Cytotoxic action of phorbol esters on human pancreatic cancer cells
    Jane A Bond
    Department of Pathology, School of Medicine, Cardiff University, Cardiff CF14 4XN, United Kingdom
    Int J Cancer 121:1445-54. 2007
    We previously showed that phorbol esters are cytotoxic to human thyroid epithelial cells expressing a mutant RAS oncogene...
  53. pmc Cell swelling, heat, and chemical agonists use distinct pathways for the activation of the cation channel TRPV4
    J 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 ..
  54. ncbi Distinct protein kinase C isoforms mediate regulation of vascular endothelial growth factor expression by A2A adenosine receptor activation and phorbol esters in pheochromocytoma PC12 cells
    Alicia 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...
  55. pmc 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 mechanisms
    Richard 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...
  56. ncbi Inhibition of bovine immunodeficiency virus by anti-HIV-1 compounds in a cell culture-based assay
    G J Tobin
    Laboratory of Cell and Molecular Structure, SAIC Frederick, MD, USA
    Antiviral Res 33:21-31. 1996
    ....
  57. pmc Substitution on the A-ring confers to bryopyran analogues the unique biological activity characteristic of bryostatins and distinct from that of the phorbol esters
    Gary 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...
  58. ncbi A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1
    K 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...
  59. ncbi Biodegradation of Jatropha curcas phorbol esters in soil
    Rakshit K Devappa
    Institute for Animal Production in the Tropics and Subtropics 480b, University of Hohenheim, 70593 Stuttgart, Germany
    J Sci Food Agric 90:2090-7. 2010
    Jatropha curcas seed cake is generated as a by-product during biodiesel production. Seed cake containing toxic phorbol esters (PEs) is currently used as a fertiliser and thus it is of eco-toxicological concern...
  60. ncbi Prostratin as a new therapeutic agent targeting HIV viral reservoirs
    Marjan 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...
  61. pmc Practical synthesis of prostratin, DPP, and their analogs, adjuvant leads against latent HIV
    Paul 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...
  62. ncbi Expression of latent HAART-persistent HIV type 1 induced by novel cellular activating agents
    Joseph 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
    ....
  63. ncbi Phorbol esters and related analogs regulate the subcellular localization of beta 2-chimaerin, a non-protein kinase C phorbol ester receptor
    M 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...
  64. ncbi Protein kinase C-dependent and -independent inhibition of Ca(2+) influx by phorbol ester in rat pancreatic beta-cells
    J Nakamura
    Department of Physiology, Hirosaki University School of Medicine, 5 Zaifu-cho, 036-8562, Hirosaki, Japan
    Cell Signal 13:199-205. 2001
    b>Phorbol esters were used to investigate the action of protein kinase C (PKC) on insulin secretion from pancreatic beta-cells...
  65. ncbi 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 complex
    A 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...
  66. ncbi Phorbol esters affect skeletal muscle glucose transport in a fiber type-specific manner
    David 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...
  67. ncbi Opposing effects of calcium entry and phorbol esters on fusion of chick muscle cells
    M 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...
  68. pmc Different pathways of calcium sensitization activated by receptor agonists and phorbol esters in vascular smooth muscle
    M Hori
    Department of Veterinary Pharmacology, Faculty of Agriculture, University of Tokyo, Japan
    Br J Pharmacol 110:1527-31. 1993
    1. 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...
  69. ncbi Phorbol ester-dependent activation of peroxiredoxin I gene expression via a protein kinase C, Ras, p38 mitogen-activated protein kinase signaling pathway
    Alexander 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...
  70. ncbi Direct, rapid effects of 25-hydroxyvitamin D3 on isolated intestinal cells
    Ruta 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...
  71. pmc Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4
    Feng 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...
  72. ncbi Interdependence of PKC-dependent and PKC-independent pathways for presynaptic plasticity
    Keimpe 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...
  73. ncbi The role of protein phosphorylation in alpha2,6(N)-sialyltransferase activity
    Kieran 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...
  74. ncbi Phorbol ester induces CYP2E1 in astrocytes, through a protein kinase C- and tyrosine kinase-dependent mechanism
    Niclas 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...
  75. ncbi Regulation of HERG potassium channel activation by protein kinase C independent of direct phosphorylation of the channel protein
    Dierk 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...
  76. ncbi Requirement of AMPA receptor GluR2 phosphorylation for cerebellar long-term depression
    Hee 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...
  77. ncbi Tumor necrosis factor-alpha converting enzyme is processed by proprotein-convertases to its mature form which is degraded upon phorbol ester stimulation
    Kristina Endres
    Institute of Biochemistry, Johannes Gutenberg University, Mainz, Germany
    Eur J Biochem 270:2386-93. 2003
    ....
  78. pmc Neurokinin 2 receptor-mediated activation of protein kinase C modulates capsaicin responses in DRG neurons from adult rats
    Adrian 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...
  79. ncbi Integration of DAG signaling systems mediated by PKC-dependent phosphorylation of RasGRP3
    Christine 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 ..
  80. ncbi Ca2+-dependent protein kinase C isoforms induce cholestasis in rat liver
    Ralf 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...
  81. ncbi IL-4-dependent CD86 expression requires JAK/STAT6 activation and is negatively regulated by PKCdelta
    Eric 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...
  82. ncbi Effect of protein kinase C activation and inhibition on rat hepatic stellate cell activation
    Grant 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...
  83. ncbi Receptor activator of nuclear factor-kappaB is induced by a rottlerin-sensitive and p38 MAP kinase-dependent pathway during monocyte differentiation
    Hong 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...
  84. ncbi Combined action of extracellular signal-regulated kinase and p38 kinase rescues Molt4 T cells from nitric oxide-induced apoptotic and necrotic cell death
    Hyun 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...
  85. ncbi Depolarization of skeletal muscle cells induces phosphorylation of cAMP response element binding protein via calcium and protein kinase Calpha
    Cesar 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...
  86. ncbi 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 receptors
    Adele 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
    ....
  87. ncbi Bidirectional regulation of renal cortical Na+,K+-ATPase by protein kinase C
    Jerzy 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...
  88. ncbi Shp2 is required for protein kinase C-dependent phosphorylation of serine 307 in insulin receptor substrate-1
    Karsten 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...
  89. ncbi Phorbol ester-induced differentiation of L6 myogenic cells involves phospholipase D activation
    Hiba Komati
    Laboratoire de Physiopathologie des Lipides et Membranes, Institut National de la Santé et de la Recherche Médicale Unité 585, Institut National des Sciences Appliquees de Lyon, 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...
  90. ncbi Differential regulation of GLAST immunoreactivity and activity by protein kinase C: evidence for modification of amino and carboxyl termini
    Bala T S Susarla
    Department of Pediatrics, University of Pennsylvania and Children s Hospital of Philadelphia, Philadelphia, Pennsylvania, USA
    J Neurochem 91:1151-63. 2004
    ....
  91. ncbi Repression of 5-aminolevulinate synthase gene by the potent tumor promoter, TPA, involves multiple signal transduction pathways
    Alejandra 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...
  92. ncbi Inhibition of the renal betaine transporter by calcium ions
    Stephen 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...
  93. ncbi The cytosolic II-III loop of Cav2.3 provides an essential determinant for the phorbol ester-mediated stimulation of E-type Ca2+ channel activity
    Udo 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...
  94. ncbi Desensitization of nicotine acetylcholine receptors: modulation by kinase activation and phosphatase inhibition
    William 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...
  95. ncbi Adapter molecule DOC-2 is differentially expressed in pressure and volume overload hypertrophy and inhibits collagen synthesis in cardiac fibroblasts
    Deepa H Kumbar
    The Heart Institute for Children, Advocate Hope Children s Hospital, Oak Lawn, IL, USA
    J Appl Physiol (1985) 102:2024-32. 2007
    ..Results suggest a role of DOC-2 in cardiac remodeling involving collagen expression during chronic hemodynamic overload...
  96. ncbi Inhibition of human p53 basal transcription by down-regulation of protein kinase Cdelta
    Tarek 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...
  97. pmc Phosphorylation of histone deacetylase 7 by protein kinase D mediates T cell receptor-induced Nur77 expression and apoptosis
    Franck 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...
  98. pmc 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 ester
    Arun 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...
  99. pmc Calcium-dependent interactions of the human norepinephrine transporter with syntaxin 1A
    Uhna 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...
  100. ncbi Evidence that protein kinase Cdelta is not required for palmitate-induced cytotoxicity in BRIN-BD11 beta-cells
    H 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...
  101. ncbi PKC activates BKCa channels in rat pulmonary arterial smooth muscle via cGMP-dependent protein kinase
    Scott 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
    ....

Research Grants63

  1. Regulation of Ovarian Cancer Multidrug Resistance by MAP Kinases
    Scott T Eblen; Fiscal Year: 2013
    ..phosphorylation in human ascites and in cell lines in response to chemotherapeutic drugs, oxidative stress, phorbol esters and UV irradiation...
  2. PKC/PKA Regulation in Prostate Cancer by SSeCKS/Gravin/AKAP12
    Irwin H Gelman; Fiscal Year: 2013
    ..Activation 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...
  3. C/EBP beta SIGNALS HEPATOCYTE PROLIFERATION AND SURVIVAL
    Mario Chojkier; Fiscal Year: 2012
    ..We have found that transforming growth factor (TGF)-c_ and phorbol esters/protein kinaseC (PKC)-o_ mediate their effects on hepatocyte proliferation, through the activation of ..
  4. ROLE AND REGULATION OF PROTEIN KINASE C ISOENZYMES
    Yusuf Awni Hannun; Fiscal Year: 2013
    ..requires sustained activation of PKC (30-60 min) in response to ligands of G-protein-coupled receptors (and phorbol esters), and it requires continuous activation of PKC as well as PLD (unlike the acute translocation of PKC to the PM)..
  5. Chimaerins-receptors for diacylgly and phorbal esters
    MARCELO GABRIEL KAZANIETZ; Fiscal Year: 2012
    ..protein kinase C (PKC) family, considered until not so long ago the only intracellular receptors for DAG and phorbol esters. 2-chimaerin possesses 3 well-defined regions: a N-terminal SH2 domain of unknown function (present only in a2-..
  6. RNA Dynamics of Transient Macromolecular Complexes in Cancer Cells
    Jack D Keene; Fiscal Year: 2013
    ..following treatment of embryonic carcinoma cells with retinoic acid or leukemia-derived immune T cells with phorbol esters plus mitogens...
  7. Very Late Antigen Integrin Activity on T Cells
    Yoji Shimizu; Fiscal Year: 2010
    ..TCR-mediated integrin activation can be mimicked by phorbol esters such as PMA, implicating effectors downstream of protein kinase C (PKC) in this process...
  8. ADENOSINE AND ANTIOXIDANT ENZYMES
    Vickram Ramkumar; Fiscal Year: 1999
    ..A23187 (a Ca2+ ionophore) and phorbol esters (activators of protein kinase C) both mimicked activation of these enzymes via the A3AR...
  9. DIFFERENTIATING AGENTS IN HEMATOLOGIC MALIGNANCIES
    Donald W Kufe; Fiscal Year: 2012
    ..Our initial studies with phorbol esters and other activators of protein kinase C (PKC) demonstrated the importance of reactive oxygen species (ROS) in ..
  10. Regulation of tumor promotion by RasGRP1
    JOE WILLIAM RAMOS; Fiscal Year: 2013
    ..carcinogenesis model, Ras is activated by mutations induced by a carcinogen, and subsequent treatment with phorbol esters induces tumor promotion...
  11. The Role of Ubiquitin in Sodium Chloride Co-Transporter Regulation
    BENJAMIN S KO; Fiscal Year: 2012
    ..presence of WNK4 (a kinase associated with a form of genetic hypertension called Gordon's Syndrome) and phorbol esters (chemical analogs of diacylglycerol, a common pathway for hormonal stimulation) but the mechanism by which NCC ..
  12. Effects of Acitretin on the activation of latent HIV
    Peilin Li; Fiscal Year: 2013
    ..with HIV (Aim1) and to define thein vitro activity of acitretin alone and in combination with HDACi or phorbol esters for inducing vira transcription and clearance of CD4 T cells carrying HIV from HIV patients on suppressive ..
  13. Enzymatic formation of the hydrocarbon skeletons underlying diterpenoid diversity
    REUBEN JOHN PETERS; Fiscal Year: 2013
    ..g., the protein kinase C activating and tumor promoting phorbol esters, and adenylate cyclase activator forskolin)...
  14. The role of PKD3 in prostate carcinogenesis
    Qiming Jane Wang; Fiscal Year: 2013
    ..kinases is a novel target of the key second messenger diacylglycerol (DAG) and its pharmacological analogs, phorbol esters. DAG and phorbol esters directly bind PKD at its C1 domain and activate PKD through phosphorylation via ..
  15. PHOSPHOLIPID TURNOVER IN EXOCRINE PANCREAS
    Ronald Rubin; Fiscal Year: 1991
    ..We will investigate the relative abilities of phorbol esters and diacylglycerol analogues, which directly activate protein kinase C, to interact synergistically with ..
  16. REGULATION OF BILE ACID SYNTHESIS
    JOHN CHIANG; Fiscal Year: 1999
    ..constructs in HepG2 cells revealed that most cis-acting elements conferring the repression by bile acids, phorbol esters (PMA), cAMP and insulin, and activation by glucocorticoid and retinoic acids are all localized in the region ..
  17. CHIRAL APPROACHES TO NATURAL PRODUCT SYNTHESIS
    Gary E Keck; Fiscal Year: 2013
    ..Protein Kinase C superfamily, bryostatin 1 is unique in being a functional antagonist to the tumor-promoting phorbol esters. The studies proposed are aimed at realizing the therapeutic potential of this agent...
  18. STRUCTURE, FUNCTION AND REGULATION OF PROTEIN KINASE C
    Alexandra C Newton; Fiscal Year: 2013
    ..cellular functions The discovery in the 1980s that they are the receptors for the potent tumor promoting phorbol esters, led to the dogma that activation of protein kinase C by phorbol esters promotes tumorigenesis...
  19. Activation of HTLV1 Gene Expression and Oncogenesis
    Arnold Rabson; Fiscal Year: 2006
    ..infected cell lines by treatment with immune activation related stimuli, such as phytohemagglutinin (PHA) and phorbol esters (PMA)...
  20. EFFECTS OF PHORBOL ESTERS ON LYMPHOCYTE STIMULATION
    Andrea Mastro; Fiscal Year: 1991
    ..The cells will also be tested for suppressor activity...
  21. MECHANISMS OF E HISTOLYTICA ADHERENCE AND CYTOLYSIS
    JONATHAN RAVDIN; Fiscal Year: 1993
    ..Amebic cytolytic activity is stimulated by phorbol esters requires amebic phospholipase A activity, an acid pH in endocytic vesicles- lethal increase in target cell ..
  22. XENOBIOTICS, INFLAMMATION AND CARCINOGENESIS
    James Lewis; Fiscal Year: 1991
    ..The association between chemicals, carcinogenesis and inflammation has long been noted. Phorbol esters have been shown to be both the inflammatory agents and the tumor promoting agents in the vesicant croton oil...
  23. PROTEIN KINASE C AND PHOTORECEPTORS
    ALEXANDRA 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...
  24. MOLECULAR BASIS OF NERVE GROWTH FACTOR
    Jeffrey Milbrandt; Fiscal Year: 1993
    ..Each of these three genes, c-fos, NGFI-A and NGFI-B, are rapidly transcribed in response to NGF, phorbol esters (TPA), and calcium ionophores (A23187), and the induction process does not require de novo protein synthesis...
  25. GENETICS OF SUSCEPTIBILITY TO SKIN TUMOR PROMOTION
    John DiGiovanni; Fiscal Year: 1990
    ..is designed to further investigate the genetic factors controlling susceptibility to skin tumor promotion by phorbol esters and other classes of tumor promoters in inbred mouse strains...
  26. REGULATION OF CALCIUM CHANNELS BY PROTEIN KINASE C
    Robert Messing; Fiscal Year: 1990
    ..The interaction between phorbol esters and Ca2+ channels will be examined in detail by studying K+-stimulated 45Ca2+ uptake and 3H-Ca2+ channel ..
  27. INSULIN REGULATION OF C-FOS EXPRESSION
    Perry Blackshear; Fiscal Year: 1991
    ..region of the c-fos gene which is necessary for induction of the gene by insulin and active tumor- promoting phorbol esters has recently been identified...
  28. STRUCTURAL STUDIES OF PLATELET GPIIB/IIIA ACTIVATION
    JOEL BENNETT; Fiscal Year: 1999
    ..GPIIb-IIIa can be induced to interact specifically with fibrinogen by stimulating the lymphocytes with phorbol esters. Consequently, this expression system permits the use of molecular techniques to study the process of GPIIb-..
  29. REGULATION OF PARATHORMONE SECRETION IN DISPERSED CELLS
    Dolores Shoback; Fiscal Year: 1990
    ..b>Phorbol esters which activate protein kinase C reverse the inhibitory effects of high EC Ca++ and stimulate PTH release...
  30. HORMONE-ACTION AND CYTOKINE REGULATION OF DECIDUA CELLS
    CHARLES CHAFFIN; Fiscal Year: 2003
    ..Our goal is to lower the threshold for apoptosis by ovariectomy (Ovx), administration of anti-progestins and phorbol esters by enhancing PKC activity...
  31. CELL BIOLOGY OF PHOSPHATIDYLCHOLINE
    Susan Jaken; Fiscal Year: 1990
    ..of phosphatidylcholine-derived diacylglycerol (DAG) in cell signal transduction and the mechanism by which phorbol esters stimulate this pathway...
  32. PHARMACOLOGIC AND MOLECULAR CONTROL OF C-JUN IN LEUKEMIA
    MATTHEW SHERMAN; Fiscal Year: 1992
    ..Jun/AP-1 binds to DNA sequences that regulate transcription of genes responsive to phorbol esters and growth factors...
  33. REGULATION OF A C JUN KINASE BY A NOVEL TUMOR PROMOTER
    ELIZABETH WATTENBERG; Fiscal Year: 2001
    ..This novel tumor promoter is as potent as the phorbol esters in the two-stage mouse skin model, but does not activate protein kinase C...
  34. Ras/Rap Signaling and Endothelial Morphogenesis
    Victoria Bautch; Fiscal Year: 2009
    ..messenger diacylglycerol (DAG) promotes vascular permeability and disrupts endothelial barrier function, and phorbol esters mimic DAG activity...
  35. TUMOR PROMOTERS AND PROTEIN KINASE C IN CANCER METASTASI
    Rayudu Gopalakrishna; Fiscal Year: 1992
    Tumor promoter phorbol esters, and cellular regulators which elevate intracellular diacylglycerol, induce protein kinase C association to the plasma membrane and thereby influence various cellular functions including cell adhesion and ..
  36. REGULATION OF ORNITHINE DECARBOXYLASE BY PHORBOL ESTERS
    Andrew Butler; Fiscal Year: 2002
    ..Taken together, these studies should provide new insight into the mechanisms by which tumor promoters and oncogenes influence ODC regulation and corrupt patterns of gene expression during carcinogenesis. ..
  37. MECHANISM OF 1-25-D3 ANTI-PROLIFERATIVE ACTION IN CML
    Jeffrey Clark; Fiscal Year: 1991
    ..Treatment of RWLeu-4 with la,25(OH)2 Vitami D3 (1,25-D3), phorbol esters (PMA), or DMSO causes these cells to cease proliferating and to differentiate into cells with phenotypic, ..
  38. TRANSCRIPTIONAL REGULATION OF CD43 GENE EXPRESSION
    CARL SHELLEY; Fiscal Year: 2001
    ..Consistent with its role in immune function, expression of CD43 is regulated by cytokines, antibodies and phorbol esters which induce cellular activation...
  39. IONIC REGULATION AND TUMOR PROMOTION
    THOMAS O BRIEN; Fiscal Year: 2000
    ..It is likely, but not proven, that the heterogeneity of cellular responses to phorbol esters is due to the diversity of PKC isoforms expressed in various cells, the diversity of protein substrates that ..
  40. Regulation of tumor promotion by RasGRP1
    Patricia Lorenzo; Fiscal Year: 2002
    ..The nature of the interaction between phorbol esters and Ras signaling in tumor promotion has not been defined yet...
  41. ION FLUXES IN VASCULAR SMOOTH MUSCLE PROLIFERATION
    MARTHA O DONNELL; Fiscal Year: 1990
    ..g., platelet-derived growth factor), phorbol esters (e.g., 12-0-tetradecanoyl phorbol-13-acetate), and evalations in cyclic AMP (cAMP)...
  42. Action of Novel Anti-tumor Agents on Cell Communication
    Diane Matesic; Fiscal Year: 2005
    ..of this hypothesis, a wide variety of tumor-promoting chemicals, including organochlorine compounds and phorbol esters, have been shown to suppress gap junction-mediated communication, implicating a role for cell-cell ..
  43. MOLECULAR MECHANISMS OF MULTI-STAGE CARCINOGENESIS
    CURTIS ASHENDEL; Fiscal Year: 1993
    ..are the signal transducing enzyme protein kinase C (PKC), also known to be the receptor for tumor promoting phorbol esters, and proteins encoded by oncogenes that have demonstrated roles in intracellular signal transduction, such as ..
  44. CL TRANSPORT REGULATION IN CULTURED HUMAN COLONOCYTES
    Mrinalini Rao; Fiscal Year: 1999
    ..In contrast tot he colonic cell line, T-84, C1 transport in human colonocytes is activated by phorbol esters and human, but not rabbit, colonocytes have a cGMP-activated C1 transport...
  45. PKC ISOZYMES AND SUBSTRATES IN MAMMARY CARCINOGENESIS
    Susan Jaken; Fiscal Year: 1999
    ..pathway in tumor promotion/progression since PKCs are the major cellular receptors for tumor promoting phorbol esters. The purpose of this proposal is to provide a clear understanding of the role of PKC isozymes and substrates ..
  46. PKC Signaling in cAMP-Induced Pulmonary Vasodilation
    SCOTT BARMAN; Fiscal Year: 2010
    ..Progress of these studies will provide important knowledge towards the development of novel therapeutic agents that will help reduce the morbidity and mortality associated with pulmonary hypertension. ..
  47. Dissection of Ethanol Actions on Cholinergic Nerve Endings
    TIMOTHY SEARL; Fiscal Year: 2008
    ..Our preliminary data with botulinums toxins demonstrate that the synaptic vesicle protein synaptobrevin is an important target for the effects of ethanol. [unreadable] [unreadable] [unreadable] [unreadable]..
  48. Arachidonic Acid Metabolism in Blood and Vascular Cells
    Jun Yang Liou; Fiscal Year: 2006
    ..Information provided by studies from this renewal application will have great impact on understanding the fundamental cytoprotection process and offer an excellent opportunity for developing new therapeutic agents. ..
  49. EICOSANOIDS AND NO IN CEREBROVASCULAR THROMBOSIS
    Kenneth Wu; Fiscal Year: 2003
    ..It is intended that this program will enable several laboratories to work individually and together to achieve the highest degree of innovating and productivity. ..
  50. Molecular Mechanisms That Regulate CD11d Expression
    JOHN NOTI; Fiscal Year: 2004
    ..Transgenic analysis of the CD11d cis elements will be done to complement these studies. These studies will expand our understanding of normal myeloid development and leukemogenesis. ..
  51. Scanning laser Confocal Microscope
    RICHARD BURRY; Fiscal Year: 2003
    ..Acquisition of the Zeiss 510 LSM META will significantly enhance the research programs of the major users and aid other investigators in the university community. ..
  52. Colon Barrier Breakdown in the Elderly
    James Mullin; Fiscal Year: 2005
    ..Changes in membrane composition/fluidity are known to affect paracellular permeability in general, and tight junction proteins specifically. ..
  53. Expression of TRPV1 and variant TRPV1 in the kidney
    David Cohen; Fiscal Year: 2005
    ..In addition, such a reagent might have potential therapeutic utility with respect to this important pathway mediating nociception. ..
  54. IgE Regulation of Mast Cell Growth and Survival
    Toshiaki Kawakami; Fiscal Year: 2006
    ..abstract_text> ..
  55. IQGAP1 in microbial pathogenesis
    David Sacks; Fiscal Year: 2006
    ..Elucidation of the mechanisms of pathogen-host interactions could reveal new targets for diagnosis, therapy and vaccines. ..
  56. Osteoblast Derived Pathogenic Factors in Hyp Mice
    Norimoto Yanagawa; Fiscal Year: 2005
    ..abstract_text> ..
  57. Endocannabinoid Analogs as Anti-inflammatory Agents
    Sumner Burstein; Fiscal Year: 2008
    ..Thus, agents such as NAGly that can regulate in vivo anandamide levels could be effective modulators of many of these health related processes. ..
  58. Tumor Necrosis Factor-Alpha Signaling in Breast Cancer
    Alakananda Basu; Fiscal Year: 2009
    ..The long-term objective is to develop strategies to intervene with these pathways to inhibit progression of breast cancer. ..
  59. IL-2 Suppression by Endocannabinoid Activation of PPARgamma
    NORBERT EDWARD KAMINSKI; Fiscal Year: 2010
    ....
  60. REGULATION OF CD154 EXPRESSION
    WILLIAM FREDERICK CARSON RIGBY; Fiscal Year: 2010
    ..Importantly, the CD153'UTR CA repeats are polymorphic with certain alleles associated with CD154 overexpression and the development of RA and SLE. ..
  61. Cocaine Regulation of Norepinephrine Transporter
    LANKUPALLE JAYANTHI; Fiscal Year: 2005
    ..Results from these studies will provide valuable scientific insights to our understanding of the role of drugs of abuse in regulating NET function and expression. ..
  62. Nitric oxide in bladder neural-epithelial signaling
    Lori Birder; Fiscal Year: 2005
    ..Elucidation of mechanisms impacting on urothelial function may provide insights into the pathology of bladder dysfunction. ..