Epigenetic Therapy for Epithelioid Sarcoma

Cell. 2020 Apr 16;181(2):211. doi: 10.1016/j.cell.2020.03.042.

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.

MeSH terms

  • Benzamides / therapeutic use*
  • Cell Line, Tumor
  • Chromatin Assembly and Disassembly
  • DNA Helicases / metabolism
  • Enhancer of Zeste Homolog 2 Protein / drug effects
  • Enhancer of Zeste Homolog 2 Protein / genetics
  • Enzyme Inhibitors / pharmacology
  • Epigenesis, Genetic / genetics*
  • Epigenomics
  • Genetic Therapy / methods
  • Humans
  • Nuclear Proteins / metabolism
  • Pyridones / therapeutic use*
  • Sarcoma / drug therapy*
  • Sarcoma / genetics
  • Transcription Factors / metabolism

Substances

  • Benzamides
  • Enzyme Inhibitors
  • Nuclear Proteins
  • Pyridones
  • Transcription Factors
  • EZH2 protein, human
  • Enhancer of Zeste Homolog 2 Protein
  • DNA Helicases
  • tazemetostat