Discovery of dihydropyridinone derivative as a covalent EZH2 degrader
Author:
Publisher
Elsevier BV
Subject
Organic Chemistry,Drug Discovery,Pharmacology,General Medicine
Reference33 articles.
1. Targeting EZH2 in cancer;Kim;Nat. Med.,2016
2. Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation;Yap;Blood,2011
3. Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas;Sneeringer;Proc. Natl. Acad. Sci. U.S.A.,2010
4. Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27);McCabe;Proc. Natl. Acad. Sci. U. S. A. A.,2012
5. A687V EZH2 is a gain-of-function mutation found in lymphoma patients;Majer;FEBS Lett.,2012
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