Abstract
The active vitamin D metabolite 1,25-dihydroxyvitamin D(3) (1,25(OH)(2)D(3)) inhibits proliferation and promotes differentiation of colon cancer cells through the activation of vitamin D receptor (VDR), a transcription factor of the nuclear receptor superfamily. Additionally, 1,25(OH)(2)D(3) has several nongenomic effects of uncertain relevance. We show that 1,25(OH)(2)D(3) induces a transcription-independent Ca(2+) influx and activation of RhoA-Rho-associated coiled kinase (ROCK). This requires VDR and is followed by activation of the p38 mitogen-activated protein kinase (p38MAPK) and mitogen- and stress-activated kinase 1 (MSK1). As shown by the use of chemical inhibitors, dominant-negative mutants and small interfering RNA, RhoA-ROCK, and p38MAPK-MSK1 activation is necessary for the induction of CDH1/E-cadherin, CYP24, and other genes and of an adhesive phenotype by 1,25(OH)(2)D(3). RhoA-ROCK and MSK1 are also required for the inhibition of Wnt-beta-catenin pathway and cell proliferation. Thus, the action of 1,25(OH)(2)D(3) on colon carcinoma cells depends on the dual action of VDR as a transcription factor and a nongenomic activator of RhoA-ROCK and p38MAPK-MSK1.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antigens, CD
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Caco-2 Cells
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Cadherins / genetics
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Cadherins / metabolism
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Calcitriol / metabolism
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Calcitriol / pharmacology*
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Calcium / metabolism
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Cdh1 Proteins
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Cell Cycle Proteins / genetics
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Cell Cycle Proteins / metabolism
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Cell Proliferation / drug effects
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Colonic Neoplasms / enzymology*
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Colonic Neoplasms / genetics
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Enzyme Activation / drug effects
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Humans
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Mice
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NIH 3T3 Cells
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Receptors, Calcitriol / genetics
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Receptors, Calcitriol / metabolism
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Ribosomal Protein S6 Kinases, 90-kDa / genetics
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Ribosomal Protein S6 Kinases, 90-kDa / metabolism*
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Steroid Hydroxylases / genetics
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Steroid Hydroxylases / metabolism
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Transcription, Genetic / drug effects
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Vitamin D3 24-Hydroxylase
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Vitamins / metabolism*
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Vitamins / pharmacology
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Wnt Proteins / genetics
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Wnt Proteins / metabolism*
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beta Catenin / genetics
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beta Catenin / metabolism
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p38 Mitogen-Activated Protein Kinases / genetics
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p38 Mitogen-Activated Protein Kinases / metabolism*
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rho GTP-Binding Proteins / genetics
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rho GTP-Binding Proteins / metabolism*
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rho-Associated Kinases / genetics
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rho-Associated Kinases / metabolism*
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rhoA GTP-Binding Protein / genetics
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rhoA GTP-Binding Protein / metabolism*
Substances
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Antigens, CD
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CDH1 protein, human
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Cadherins
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Cdh1 Proteins
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Cell Cycle Proteins
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Fzr1 protein, mouse
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Receptors, Calcitriol
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Vitamins
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Wnt Proteins
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beta Catenin
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RHOA protein, human
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Steroid Hydroxylases
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Vitamin D3 24-Hydroxylase
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Ribosomal Protein S6 Kinases, 90-kDa
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mitogen and stress-activated protein kinase 1
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rho-Associated Kinases
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p38 Mitogen-Activated Protein Kinases
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RhoA protein, mouse
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rho GTP-Binding Proteins
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rhoA GTP-Binding Protein
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Calcitriol
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Calcium