The DOI matches its Crossref record; 60 of the 60 references it cites were found in a registry or an index.
Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
Open accessAbstract
Among epigenetic "writers", "readers", and "erasers", the lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9me2) and nonhistone proteins, have been implicated in a variety of human diseases. A "toolkit" of well-characterized chemical probes will allow biological and disease hypotheses concerning these proteins to be tested in cell-based and animal models with high confidence. We previously discovered potent and selective G9a/GLP inhibitors including the cellular chemical probe UNC0638, which displays an excellent separation of functional potency and cell toxicity. However, this inhibitor is not suitable for animal studies due to its poor pharmacokinetic (PK) properties. Here, we report the discovery of the first G9a and GLP in vivo chemical probe UNC0642, which not only maintains high in vitro and cellular potency, low cell toxicity, and excellent selectivity, but also displays improved in vivo PK properties, making it suitable for animal studies.
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Cites
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Cited by
Epigenetics in cancer stem cells
Toh, T. B., Lim, J. J., & Chow, E. K.-H. (2017) · Molecular Cancer · doi:10.1186/s12943-017-0596-9 · Cited by 422
Marked for death: Targeting epigenetic changes in cancer
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Chemical and Biochemical Perspectives of Protein Lysine Methylation
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Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a
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Metadata
- Authors
- Liu, F., Barsyte-Lovejoy, D., Li, F., Xiong, Y., Korboukh, V., Huang, X.-P., Allali-Hassani, A., Janzen, W. P., Roth, B. L., Frye, S. V., Arrowsmith, C. H., Brown, P. J., Vedadi, M., & Jin, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2013-10-31
- Volume
- 56
- Issue
- 21
- Pages
- 8931-8942
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2065125513
- Cited by
- 268
- References
- 60
- FWCI
- 7.13
- Type
- journal article
- Language
- en
- Open access
- green
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- Liu, F., Barsyte-Lovejoy, D., Li, F., Xiong, Y., Korboukh, V., Huang, X.-P., Allali-Hassani, A., Janzen, W. P., Roth, B. L., Frye, S. V., Arrowsmith, C. H., Brown, P. J., Vedadi, M., & Jin, J. (2013). Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm401480r
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