Document Detail


Histone deacetylase inhibitor induces DNA damage, which normal but not transformed cells can repair.
MedLine Citation:
PMID:  20679231     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Histone deacetylase inhibitors (HDACi) developed as anti-cancer agents have a high degree of selectivity for killing cancer cells. HDACi induce acetylation of histones and nonhistone proteins, which affect gene expression, cell cycle progression, cell migration, and cell death. The mechanism of the tumor selective action of HDACi is unclear. Here, we show that the HDACi, vorinostat (Suberoylanilide hydroxamic acid, SAHA), induces DNA double-strand breaks (DSBs) in normal (HFS) and cancer (LNCaP, A549) cells. Normal cells in contrast to cancer cells repair the DSBs despite continued culture with vorinostat. In transformed cells, phosphorylated H2AX (gammaH2AX), a marker of DNA DSBs, levels increased with continued culture with vorinostat, whereas in normal cells, this marker decreased with time. Vorinostat induced the accumulation of acetylated histones within 30 min, which could alter chromatin structure-exposing DNA to damage. After a 24-h culture of cells with vorinostat, and reculture without the HDACi, gammaH2AX was undetectable by 2 h in normal cells, while persisting in transformed cells for the duration of culture. Further, we found that vorinostat suppressed DNA DSB repair proteins, e.g., RAD50, MRE11, in cancer but not normal cells. Thus, the HDACi, vorinostat, induces DNA damage which normal but not cancer cells can repair. This DNA damage is associated with cancer cell death. These findings can explain, in part, the selectivity of vorinostat in causing cancer cell death at concentrations that cause little or no normal cell death.
Authors:
J-H Lee; M L Choy; L Ngo; S S Foster; Paul A Marks
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2010-08-02
Journal Detail:
Title:  Proceedings of the National Academy of Sciences of the United States of America     Volume:  107     ISSN:  1091-6490     ISO Abbreviation:  Proc. Natl. Acad. Sci. U.S.A.     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-08-18     Completed Date:  2010-09-27     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7505876     Medline TA:  Proc Natl Acad Sci U S A     Country:  United States    
Other Details:
Languages:  eng     Pagination:  14639-44     Citation Subset:  IM    
Affiliation:
Cell Biology, Sloan-Kettering Institute, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.
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MeSH Terms
Descriptor/Qualifier:
Acetylation / drug effects
Antineoplastic Agents / pharmacology
Cell Cycle / drug effects
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects,  genetics
Cells, Cultured
DNA Breaks, Double-Stranded / drug effects
DNA Damage*
DNA Repair*
Dose-Response Relationship, Drug
Fibroblasts / cytology,  drug effects,  metabolism
Flow Cytometry
Foreskin / cytology
Histone Deacetylase Inhibitors / pharmacology*
Histones / metabolism
Humans
Hydroxamic Acids / pharmacology*
Immunoblotting
Male
Microscopy, Fluorescence
Grant Support
ID/Acronym/Agency:
P30CA08748-44/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/H2AFX protein, human; 0/Histone Deacetylase Inhibitors; 0/Histones; 0/Hydroxamic Acids; 149647-78-9/vorinostat

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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