1. Epigenetic Therapy for Epithelioid Sarcoma
- Author
-
Scott B. Rothbart and Stephen B. Baylin
- Subjects
Epigenomics ,Pyridones ,Protein subunit ,Epithelioid sarcoma ,Morpholines ,Lysine ,macromolecular substances ,Biology ,General Biochemistry, Genetics and Molecular Biology ,Chromatin remodeling ,Epigenesis, Genetic ,03 medical and health sciences ,0302 clinical medicine ,Cell Line, Tumor ,medicine ,Gene silencing ,Humans ,Enhancer of Zeste Homolog 2 Protein ,Enzyme Inhibitors ,030304 developmental biology ,0303 health sciences ,EZH2 ,Biphenyl Compounds ,DNA Helicases ,Nuclear Proteins ,Sarcoma ,Genetic Therapy ,medicine.disease ,Chromatin Assembly and Disassembly ,Benzamides ,biology.protein ,Cancer research ,PRC2 ,030217 neurology & neurosurgery ,Epigenetic therapy ,Transcription Factors - 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.
- Published
- 2020