EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity
Author:
Affiliation:
1. Epizyme, Inc., 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02139, United States
2. Eisai Co., Ltd., Tokodai 5-1-3, Tsukuba, Ibarakai 300-2635, Japan
3. Eisai, Inc., 4 Corporate Drive, Andover, Massachusetts 01810, United States
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry,Drug Discovery,Biochemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.5b00037
Reference16 articles.
1. Histone methyltransferase activity associated with a human multiprotein complex containing the Enhancer of Zeste protein
2. Role of Histone H3 Lysine 27 Methylation in Polycomb-Group Silencing
3. Roles of the EZH2 histone methyltransferase in cancer epigenetics
4. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
5. Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas
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