Epigenetic Therapy for Epithelioid Sarcoma

Scott B Rothbart; Stephen B Baylin

doi:10.1016/j.cell.2020.03.042

Epigenetic Therapy for Epithelioid Sarcoma

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

Authors

Scott B Rothbart¹, Stephen B Baylin²

Affiliations

¹ Center for Epigenetics, Van Andel Institute, Grand Rapids, MI 49503, USA. Electronic address: scott.rothbart@vai.org.
² Center for Epigenetics, Van Andel Institute, Grand Rapids, MI 49503, USA; Department of Oncology, Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins School of Medicine, Baltimore, MD 21287, USA. Electronic address: sbaylin@jhmi.edu.

PMID: 32302562
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*
Biphenyl Compounds
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
Morpholines
Nuclear Proteins / metabolism
Pyridones / therapeutic use*
Sarcoma / drug therapy*
Sarcoma / genetics
Transcription Factors / metabolism

Substances

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