上皮样肉瘤的表观遗传学治疗。
Epigenetic Therapy for Epithelioid Sarcoma.
机构信息
Center for Epigenetics, Van Andel Institute, Grand Rapids, MI 49503, USA.
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.
出版信息
Cell. 2020 Apr 16;181(2):211. doi: 10.1016/j.cell.2020.03.042.
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.
他泽莫司他是首个获得美国食品药品监督管理局批准用于实体瘤的表观遗传学治疗药物。这种赖氨酸甲基转移酶抑制剂的作用靶点是 PRC2 转录沉默复合物的酶亚基 EZH2。包含大多数上皮样肉瘤在内的，SWI/SNF 染色质重塑复合物亚基发生突变的肿瘤对 EZH2 抑制敏感。
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