The DOI matches its Crossref record; 9 of the 9 references it cites were found in a registry or an index.
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2
Open accessAbstract
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part of a drug discovery program targeting EZH2, we have identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 (3) and GSK343 (6). These compounds are small molecule chemical tools that would be useful to further explore the biology of EZH2.
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Citations
Cites
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The polycomb group protein EZH2 is involved in progression of prostate cancer
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Self-citationEpigenetic regulation in psychiatric disorders
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Cited by
Kim, K. H., & Roberts, C. W. M. (2016) · Nature Medicine · doi:10.1038/nm.4036 · Cited by 1,471
Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials
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EZH2: a novel target for cancer treatment
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Self-citationEZH2 is a potential therapeutic target for H3K27M-mutant pediatric gliomas
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Germinal centres and B cell lymphomagenesis
Basso, K., & Dalla-Favera, R. (2015) · Nature Reviews Immunology · doi:10.1038/nri3814 · Cited by 510
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Poised epigenetic states and acquired drug resistance in cancer
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Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
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Epigenetic mechanisms of tumor resistance to immunotherapy
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Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres: Miniperspective
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Metadata
- Authors
- Verma, S. K., Tian, X., LaFrance, L. V., Duquenne, C., Suarez, D. P., Newlander, K. A., Romeril, S. P., Burgess, J. L., Grant, S. W., Brackley, J. A., Graves, A. P., Scherzer, D. A., Shu, A., Thompson, C., Ott, H. M., Aller, G. S. V., Machutta, C. A., Diaz, E., Jiang, Y., Johnson, N. W., Knight, S. D., Kruger, R. G., McCabe, M. T., Dhanak, D., Tummino, P. J., Creasy, C. L., & Miller, W. H.
- Venue
- ACS Medicinal Chemistry Letters
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-10-19
- Volume
- 3
- Issue
- 12
- Pages
- 1091-1096
- ISSN
- 1948-5875 (ISSN-L)
- OpenAlex
- W1977199336
- Cited by
- 371
- References
- 9
- FWCI
- 8.83
- Type
- journal article
- Language
- en
- Open access
- green
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