Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

[Image: see text] G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme lysine channel. A-366 is a...

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Hlavní autoři: Sweis, Ramzi F., Pliushchev, Marina, Brown, Peter J., Guo, Jun, Li, Fengling, Maag, David, Petros, Andrew M., Soni, Nirupama B., Tse, Chris, Vedadi, Masoud, Michaelides, Michael R., Chiang, Gary G., Pappano, William N.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2014
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027767/
https://ncbi.nlm.nih.gov/pubmed/24900801
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400496h
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