Abstract
The ATP/ubiquitin-dependent 26S proteasome is a central regulator of cell cycle progression and stress responses. While investigating the application of peptide aldehyde proteasome inhibitors to block signal-induced IkappaBalpha degradation in human LNCaP prostate carcinoma cells, we observed that persistent inhibition of proteasomal activity signals a potent cell death program. Biochemically, this program included substantial upregulation of PAR-4 (prostate apoptosis response-4), a putative pro-apoptotic effector protein and stabilization of c-jun protein, a potent pro-death effector in certain cells. We also observed modest downregulation of bcl-XL, a pro-survival effector protein. However, in contrast to some recent reports stable, high level, expression of functional bcl-2 protein in prostate carcinoma cells failed to signal protection against cell death induction by proteasome inhibitors. Also in disagreement to a recent report, no evidence was found for activation of the JNK stress kinase pathway. A role for p53, a protein regulated by the proteasome pathway, was ruled out, since comparable cell death induction by proteasome inhibitors occurred in PC-3 cells that do not express functional p53 protein. These data signify that the ubiquitin/proteasome pathway represents a potential therapeutic target for prostate cancers irrespective of bcl-2 expression or p53 mutations.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aldehydes / pharmacology
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Aldehydes / therapeutic use
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Apoptosis Regulatory Proteins
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Blotting, Western
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Calcium-Calmodulin-Dependent Protein Kinases / metabolism
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Carrier Proteins / metabolism
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Cell Death / drug effects*
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Cytoskeletal Proteins / metabolism
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DNA-Binding Proteins / metabolism
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Dose-Response Relationship, Drug
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Humans
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I-kappa B Proteins*
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Intracellular Signaling Peptides and Proteins*
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JNK Mitogen-Activated Protein Kinases
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Leucine / analogs & derivatives
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Leucine / pharmacology
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Male
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Mitogen-Activated Protein Kinases*
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NF-KappaB Inhibitor alpha
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NF-kappa B / metabolism
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Peptide Hydrolases / metabolism*
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Peptides / pharmacology
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Peptides / therapeutic use
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Prostatic Neoplasms / drug therapy
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Prostatic Neoplasms / pathology
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Prostatic Neoplasms / physiopathology*
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Proteasome Endopeptidase Complex*
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Proto-Oncogene Proteins c-bcl-2 / metabolism*
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Proto-Oncogene Proteins c-jun / metabolism
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Signal Transduction / drug effects
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Trans-Activators*
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Transcription Factor RelA
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Tumor Cells, Cultured
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Tumor Suppressor Protein p53 / metabolism*
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Ubiquitins / metabolism
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beta Catenin
Substances
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Aldehydes
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Apoptosis Regulatory Proteins
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CTNNB1 protein, human
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Carrier Proteins
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Cytoskeletal Proteins
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DNA-Binding Proteins
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I-kappa B Proteins
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Intracellular Signaling Peptides and Proteins
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NF-kappa B
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NFKBIA protein, human
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Peptides
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Proto-Oncogene Proteins c-bcl-2
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Proto-Oncogene Proteins c-jun
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Trans-Activators
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Transcription Factor RelA
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Tumor Suppressor Protein p53
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Ubiquitins
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acetyl-leucinal-leucinal-normethional
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acetyl-leucinal-nor-leucinal
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beta Catenin
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prostate apoptosis response-4 protein
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NF-KappaB Inhibitor alpha
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Calcium-Calmodulin-Dependent Protein Kinases
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JNK Mitogen-Activated Protein Kinases
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Mitogen-Activated Protein Kinases
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Peptide Hydrolases
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Proteasome Endopeptidase Complex
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ATP dependent 26S protease
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Leucine