Abstract
In this Letter, we present a concise strategy to prepare a conjugate of the tumor homing peptide iRGD and histone deacetylase inhibitor valproic acid, VPA-GFLG-iRGD. The conjugate VPA-GFLG-iRGD and a mixture of VPA and GFLG-iRGD have shown similar cytotoxicity against DU-145 prostate cancer cells. However, the treatment of DU-145 cells with conjugate VPA-GFLG-iRGD resulted in a decreased percentage of cells in the G2 phase, whereas the exposure of a mixture of VPA and GFLG-iRGD led to an increased percentage of cells in the G2 phase. We also found that GFLG-iRGD possessed cytotoxicity at the tested concentrations.
Keywords:
Cell cycle arrest; Cell penetrating peptide; Histone deacetylase inhibitor; Valproic acid.
Copyright © 2014 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Cycle / drug effects
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Cell Line, Tumor
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Flow Cytometry
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Histone Deacetylase Inhibitors / chemical synthesis*
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Histone Deacetylase Inhibitors / chemistry
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Histone Deacetylase Inhibitors / pharmacology*
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Humans
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Male
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Molecular Structure
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Prostatic Neoplasms / drug therapy*
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Valproic Acid / chemical synthesis
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Valproic Acid / chemistry*
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Valproic Acid / pharmacology*
Substances
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Antineoplastic Agents
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Histone Deacetylase Inhibitors
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Oligopeptides
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Valproic Acid
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arginyl-glycyl-aspartic acid