Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas

[Image: see text] Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of PRC2 function correlates with certain malignancies and poor prognosis. EZH2 is the catalytic eng...

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Publicat a:J Med Chem
Autors principals: Vaswani, Rishi G., Gehling, Victor S., Dakin, Les A., Cook, Andrew S., Nasveschuk, Christopher G., Duplessis, Martin, Iyer, Priyadarshini, Balasubramanian, Srividya, Zhao, Feng, Good, Andrew C., Campbell, Robert, Lee, Christina, Cantone, Nico, Cummings, Richard T., Normant, Emmanuel, Bellon, Steven F., Albrecht, Brian K., Harmange, Jean-Christophe, Trojer, Patrick, Audia, James E., Zhang, Ying, Justin, Neil, Chen, Shuyang, Wilson, Jon R., Gamblin, Steven J.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2016
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5451150/
https://ncbi.nlm.nih.gov/pubmed/27739677
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01315
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