The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a
Open accessAbstract
SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to the discovery of 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal structure of the G9a-8 complex, the first cocrystal structure of G9a with a small molecule inhibitor, was obtained. The cocrystal structure validated our binding hypothesis and will enable structure-based design of novel inhibitors. 8 is a useful tool for investigating the biology of G9a and its roles in chromatin remodeling.
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Cites
Chromatin modifications and their function
Kouzarides, T. (2007) · Cell · doi:10.1016/j.cell.2007.02.005 · Cited by 10,883
Regulation of chromatin structure by site-specific histone H3 methyltransferases
Rea, S., Eisenhaber, F., O'Carroll, D., Strahl, B. D., Sun, Z.-W., Schmid, M., Opravil, S., Mechtler, K., Ponting, C. P., Allis, C. D., et al. (2000) · Nature · doi:10.1038/35020506 · Cited by 2,845
Bernstein, B. E., Meissner, A., & Lander, E. S. (2007) · Cell · doi:10.1016/j.cell.2007.01.033 · Cited by 2,086
Cited by
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
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., et al. (2011) · Nature Chemical Biology · doi:10.1038/nchembio.599 · Cited by 527
Self-citationFluorescence polarization assays in small molecule screening
Lea, W. A., & Simeonov, A. (2011) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2011.537322 · Cited by 379
Self-citationDiscovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
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., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm401480r · Cited by 268
Self-citationStructural Basis of Substrate Methylation and Inhibition of SMYD2
Ferguson, A. D., Larsen, N. A., Howard, T., Pollard, H., Green, I., Grande, C., Cheung, T., Garcia-Arenas, R., Cowen, S., Wu, J., et al. (2011) · Structure · doi:10.1016/j.str.2011.06.011 · Cited by 203
Lin, Y., Fan, H., Frederiksen, M., Zhao, K., Jiang, L., Wang, Z., Zhou, S., Guo, W., Gao, J., Li, S., et al. (2012) · Analytical Biochemistry · doi:10.1016/j.ab.2012.01.019 · Cited by 15
Metadata
- Authors
- Liu, F., Chen, X., Allali-Hassani, A., Quinn, A. M., Wasney, G. A., Dong, A., Barsyte, D., Kozieradzki, I., Senisterra, G., Chau, I., Siarheyeva, A., Kireev, D. B., Jadhav, A., Herold, J. M., Frye, S. V., Arrowsmith, C. H., Brown, P. J., Simeonov, A., Vedadi, M., & Jin, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2009-11-05
- Volume
- 52
- Issue
- 24
- Pages
- 7950-7953
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2083284090
- Cited by
- 239
- References
- 3
- FWCI
- 10.38
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a. https://app.cochat.ai/papers/10.1021/jm901543m
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- Liu, F., Chen, X., Allali-Hassani, A., Quinn, A. M., Wasney, G. A., Dong, A., Barsyte, D., Kozieradzki, I., Senisterra, G., Chau, I., Siarheyeva, A., Kireev, D. B., Jadhav, A., Herold, J. M., Frye, S. V., Arrowsmith, C. H., Brown, P. J., Simeonov, A., Vedadi, M., & Jin, J. (2009). Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm901543m
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
