The DOI matches its Crossref record; 51 of the 51 references it cites were found in a registry or an index.
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
Open accessAbstract
Protein lysine methyltransferases G9a and GLP modulate the transcriptional repression of a variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as dimethylation of non-histone targets. Here we report the discovery of UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 treatment of a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed for small hairpin RNA knockdown of G9a and GLP with the functional potency of UNC0638 being well separated from its toxicity. UNC0638 markedly reduced the clonogenicity of MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs. In mouse embryonic stem cells, UNC0638 reactivated G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation.
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A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
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Metadata
- Authors
- Vedadi, M., Barsyte-Lovejoy, D., Liu, F., Rival-Gervier, S., Allali-Hassani, A., Labrie, V., Wigle, T. J., DiMaggio, P. A., Wasney, G. A., Siarheyeva, A., Dong, A., Tempel, W., Wang, S.-C., Chen, X., Chau, I., Mangano, T. J., Huang, X.-P., Simpson, C. D., Pattenden, S. G., Norris, J. L., Kireev, D. B., Tripathy, A., Edwards, A., Roth, B. L., Janzen, W. P., Garcia, B. A., Petronis, A., Ellis, J., Brown, P. J., Frye, S. V., Arrowsmith, C. H., & Jin, J.
- Venue
- Nature Chemical Biology
- Published
- 2011-07-10
- Volume
- 7
- Issue
- 8
- Pages
- 566-574
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- OpenAlex
- W2063296278
- Cited by
- 527
- References
- 51
- FWCI
- 15.64
- Type
- journal article
- Language
- en
- Open access
- green
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- Vedadi, M., Barsyte-Lovejoy, D., Liu, F., Rival-Gervier, S., Allali-Hassani, A., Labrie, V., Wigle, T. J., DiMaggio, P. A., Wasney, G. A., Siarheyeva, A., Dong, A., Tempel, W., Wang, S.-C., Chen, X., Chau, I., Mangano, T. J., Huang, X.-P., Simpson, C. D., Pattenden, S. G., . . . Jin, J. (2011). A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nature Chemical Biology. https://doi.org/10.1038/nchembio.599
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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