Abstract
A protein kinase C (PKC) agonist selective for the beta I isozyme, 12-deoxyphorbol 13-phenylacetate 20-acetate (dPPA), induced NF-kappa B-like binding activity and surface expression of E-selectin and VCAM-1 in human umbilical vein endothelial cells (HUVEC), similar to the effects of tumor necrosis factor-alpha (TNF-alpha). Induction of E-selectin and VCAM-1 expression by dPPA was completely inhibited by the PKC inhibitors staurosporine and Ro31-7549. The PKC inhibitors also reduce TNF-alpha-induced VCAM-1 expression. However, neither dPPA nor TNF-alpha translocated PKC from the cytosolic to the plasma or nuclear membrane particulate fractions in HUVEC. These results indicate that activation of the beta I PKC isozyme is sufficient for expression of E-selectin and VCAM-1, and suggest that PKC may mediate the effects of TNF-alpha and dPPA without requiring the translocation normally associated with activation of PKC.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkaloids / pharmacology
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Base Sequence
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Cell Adhesion Molecules / biosynthesis*
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Cell Adhesion Molecules / genetics
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Cell Membrane / drug effects
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Cell Membrane / metabolism
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Cells, Cultured
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Cytosol / enzymology
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E-Selectin
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Endothelium, Vascular / drug effects
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Endothelium, Vascular / metabolism*
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Humans
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Indoles / pharmacology
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Isoenzymes / antagonists & inhibitors
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Isoenzymes / metabolism*
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Kinetics
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Maleimides / pharmacology
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Membrane Glycoproteins / biosynthesis
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Molecular Sequence Data
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NF-kappa B / metabolism
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Oligonucleotide Probes
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Phorbol Esters / pharmacology*
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Promoter Regions, Genetic
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Protein Kinase C / antagonists & inhibitors
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Protein Kinase C / metabolism*
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Staurosporine
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Tetradecanoylphorbol Acetate / pharmacology
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Tumor Necrosis Factor-alpha / pharmacology
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Umbilical Veins
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Vascular Cell Adhesion Molecule-1
Substances
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Alkaloids
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Cell Adhesion Molecules
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E-Selectin
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Indoles
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Isoenzymes
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Maleimides
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Membrane Glycoproteins
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NF-kappa B
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Oligonucleotide Probes
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Phorbol Esters
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Tumor Necrosis Factor-alpha
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Vascular Cell Adhesion Molecule-1
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12-deoxyphorbolphenylacetate
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thymeleatoxin
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Protein Kinase C
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Staurosporine
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Tetradecanoylphorbol Acetate
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Ro 31-7549