Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.

Protein lysine methyltransferase G9a, which catalyzes methylation of lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, is over expressed in human cancers. Genetic knockdown of G9a inhibits cancer cell growth and the di-methylation of p53 K373 results in the inactivation of p53. Initial SAR...

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Main Authors: Liu, Feng, Chen, Xin, Allali-Hassani, Abdellah, Quinn, Amy M., Wigle, Tim J., Wasney, Gregory A., Dong, Aiping, Senisterra, Guillermo, Chau, Irene, Siarheyeva, Alena, Norris, Jacqueline L., Kireev, Dmitri B., Jadhav, Ajit, Herold, J. Martin, Janzen, William P., Arrowsmith, Cheryl H., Frye, Stephen V., Brown, Peter J., Simeonov, Anton, Vedadi, Masoud, Jin, Jian
Format: Artigo
Sprog:Inglês
Udgivet: 2010
Fag:
Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2920043/
https://ncbi.nlm.nih.gov/pubmed/20614940
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm100478y
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