Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies
Author:
Affiliation:
1. Epizyme Inc., 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02139, United States
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry,Drug Discovery,Biochemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.1c00272
Reference19 articles.
1. Identification and Characterization of a Novel Human Histone H3 Lysine 36-specific Methyltransferase
2. Dynamic histone H3 methylation during gene induction: HYPB/Setd2 mediates all H3K36 trimethylation
3. Transcriptionally active chromatin recruits homologous recombination at DNA double-strand breaks
4. SETD2 is required for DNA double-strand break repair and activation of the p53-mediated checkpoint
5. Splicing enhances recruitment of methyltransferase HYPB/Setd2 and methylation of histone H3 Lys36
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