Abstract
Histone deacetylase (HDAC) inhibitors induce an intrinsic type of apoptosis in human papillomavirus (HPV)-positive cells by disrupting the mitochondrial transmembrane potential (deltapsim). Loss of deltapsim was only detected in E7, but not in E6 oncogene-expressing cells. HDAC inhibition led to a time-dependent degradation of the pocket proteins pRb, p107 and p130, releasing 'free' E2F-1 following initial G1 arrest. Inhibition of proteasomal proteolysis, but not of caspase activity rescued pRb from degradation and functionally restored its inhibitory effect on the cyclin E gene, known to be suppressed by pRb-E2F-1 in conjunction with HDAC1. Using siRNA targeted against p53, E2F-1 still triggered apoptosis by inducing the E2F-responsive proapoptotic alpha- and beta-isoforms of p73. These data may determine future therapeutic strategies in which HDAC inhibitors can effectively eliminate HPV-positive cells by an apoptotic route that does not rely on the reactivation of the 'classical' p53 pathway through a preceding shut-off of viral gene expression.
Copyright 2004 Nature Publishing Group
MeSH terms
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Apoptosis / drug effects*
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Base Sequence
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Cell Cycle Proteins*
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DNA Primers
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DNA-Binding Proteins / drug effects
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DNA-Binding Proteins / physiology*
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E2F Transcription Factors
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E2F1 Transcription Factor
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Enzyme Inhibitors / pharmacology*
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Genes, Tumor Suppressor
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HeLa Cells
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Histone Deacetylase Inhibitors*
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Humans
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Intracellular Membranes / drug effects
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Membrane Potentials / drug effects
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Membrane Potentials / physiology
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Mitochondria / drug effects
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Mitochondria / physiology
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Nuclear Proteins / drug effects
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Nuclear Proteins / physiology*
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Papillomaviridae / pathogenicity*
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Protein Isoforms / drug effects
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Protein Isoforms / physiology
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RNA, Small Interfering / genetics
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Receptors, Fc / antagonists & inhibitors
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Transcription Factors / drug effects
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Transcription Factors / physiology*
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Tumor Protein p73
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Tumor Suppressor Proteins
Substances
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Cell Cycle Proteins
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DNA Primers
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DNA-Binding Proteins
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E2F Transcription Factors
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E2F1 Transcription Factor
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E2F1 protein, human
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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Nuclear Proteins
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Protein Isoforms
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RNA, Small Interfering
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Receptors, Fc
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TP73 protein, human
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Transcription Factors
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Tumor Protein p73
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Tumor Suppressor Proteins