Abstract
Tazemetostat is the first epigenetic therapy to gain FDA approval in a solid tumor. This lysine methyltransferase inhibitor targets EZH2, the enzymatic subunit of the PRC2 transcriptional silencing complex. Tumors with mutations in subunits of the SWI/SNF chromatin remodeling complex, inclusive of most epithelioid sarcomas, are sensitive to EZH2 inhibition.
Copyright © 2020. Published by Elsevier Inc.
MeSH terms
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Benzamides / therapeutic use*
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Biphenyl Compounds
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Cell Line, Tumor
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Chromatin Assembly and Disassembly
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DNA Helicases / metabolism
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Enhancer of Zeste Homolog 2 Protein / drug effects
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Enhancer of Zeste Homolog 2 Protein / genetics
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Enzyme Inhibitors / pharmacology
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Epigenesis, Genetic / genetics*
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Epigenomics
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Genetic Therapy / methods
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Humans
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Morpholines
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Nuclear Proteins / metabolism
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Pyridones / therapeutic use*
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Sarcoma / drug therapy*
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Sarcoma / genetics
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Transcription Factors / metabolism
Substances
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Benzamides
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Biphenyl Compounds
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Enzyme Inhibitors
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Morpholines
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Nuclear Proteins
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Pyridones
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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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DNA Helicases
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tazemetostat