Abstract
Recent clinical trials demonstrating the efficacy of poly(ADP-ribose) polymerase (PARP) inhibitors for the treatment of BRCA1-deficient breast cancer have provided support for the 'synthetic lethal' concept of targeted cancer therapeutics. A new study provides further preclinical validation of this concept by demonstrating that BRCA1-deficient mouse mammary tumor cells are selectively sensitive to an inhibitor of the polycomb gene EZH2. The development of polycomb gene inhibitors may provide a novel approach to selectively exploit the molecular alterations in BRCA1-deficient breast tumors.
MeSH terms
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Animals
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BRCA1 Protein / deficiency*
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Breast Neoplasms / drug therapy*
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Breast Neoplasms / enzymology
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Breast Neoplasms / genetics
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DNA-Binding Proteins / antagonists & inhibitors
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Enhancer of Zeste Homolog 2 Protein
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Female
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Histone-Lysine N-Methyltransferase / antagonists & inhibitors
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Humans
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Mammary Neoplasms, Experimental / drug therapy
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Mammary Neoplasms, Experimental / enzymology
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Mammary Neoplasms, Experimental / genetics
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Mice
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Poly(ADP-ribose) Polymerase Inhibitors*
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Polycomb Repressive Complex 2
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Transcription Factors / antagonists & inhibitors
Substances
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BRCA1 Protein
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DNA-Binding Proteins
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Poly(ADP-ribose) Polymerase Inhibitors
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Transcription Factors
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EZH2 protein, human
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Enhancer of Zeste Homolog 2 Protein
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Ezh2 protein, mouse
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Histone-Lysine N-Methyltransferase
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Polycomb Repressive Complex 2