The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.
Open accessAbstract
Protein lysine methyltransferase G9a, which catalyzes methylation of lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, is overexpressed in human cancers. Genetic knockdown of G9a inhibits cancer cell growth, and the dimethylation of p53 K373 results in the inactivation of p53. Initial SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template represented by 3a (BIX01294), a selective small molecule inhibitor of G9a and GLP, led to the discovery of 10 (UNC0224) as a potent G9a inhibitor with excellent selectivity. A high resolution X-ray crystal structure of the G9a-10 complex, the first cocrystal structure of G9a with a small molecule inhibitor, was obtained. On the basis of the structural insights revealed by this cocrystal structure, optimization of the 7-dimethylaminopropoxy side chain of 10 resulted in the discovery of 29 (UNC0321) (Morrison K(i) = 63 pM), which is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.
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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 · cited 10×
“After 5 min incubation, reactions were initiated by the addition of 5 μM H3 (1-25) peptide.”
BackgroundMethodInfluentialBernstein, B. E., Meissner, A., & Lander, E. S. (2007) · Cell · doi:10.1016/j.cell.2007.01.033 · Cited by 2,086
Li, Y., Reddy, M. A., Miao, F., Shanmugam, N., Yee, J.-K., Hawkins, D., Ren, B., & Natarajan, R. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m802800200 · Cited by 353
Control of Cognition and Adaptive Behavior by the GLP/G9a Epigenetic Suppressor Complex
Schaefer, A., Sampath, S. C., Intrator, A., Min, A., Gertler, T. S., Surmeier, D. J., Tarakhovsky, A., & Greengard, P. (2009) · Neuron · doi:10.1016/j.neuron.2009.11.019 · Cited by 317
Cited by
Epigenetic protein families: a new frontier for drug discovery
Arrowsmith, C. H., Bountra, C., Fish, P. V., Lee, K., & Schapira, M. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3674 · Cited by 1,327
Self-citationH3K9 methyltransferase G9a and the related molecule GLP
Shinkai, Y., & Tachibana, M. (2011) · Genes & Development · doi:10.1101/gad.2027411 · Cited by 558
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-citationUse of Epigenetic Drugs in Disease: An Overview
Heerboth, S., Lapinska, K., Snyder, N., Leary, M., Rollinson, S., & Sarkar, S. (2014) · Genetics & Epigenetics · doi:10.4137/geg.s12270 · Cited by 326
Discovery 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
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Metadata
- Authors
- Liu, F., Chen, X., Allali-Hassani, A., Quinn, A. M., Wigle, T. J., Wasney, G. A., Dong, A., Senisterra, G., Chau, I., Siarheyeva, A., Norris, J. L., Kireev, D. B., Jadhav, A., Herold, J. M., Janzen, W. P., Arrowsmith, C. H., Frye, S. V., Brown, P. J., Simeonov, A., Vedadi, M., & Jin, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2010-07-09
- Volume
- 53
- Issue
- 15
- Pages
- 5844-5857
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2090364875
- Cited by
- 205
- References
- 5
- FWCI
- 6.85
- Type
- journal article
- Language
- en
- Open access
- green
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- Liu, F., Chen, X., Allali-Hassani, A., Quinn, A. M., Wigle, T. J., Wasney, G. A., Dong, A., Senisterra, G., Chau, I., Siarheyeva, A., Norris, J. L., Kireev, D. B., Jadhav, A., Herold, J. M., Janzen, W. P., Arrowsmith, C. H., Frye, S. V., Brown, P. J., Simeonov, A., . . . Jin, J. (2010). Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm100478y
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