Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

[Image: see text] Histone methyltransferase EZH2, which is the catalytic subunit of the PRC2 complex, catalyzes the methylation of histone H3K27—a transcriptionally repressive post-translational modification (PTM). EZH2 is commonly mutated in hematologic malignancies and frequently overexpressed in...

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Опубликовано в: :ACS Med Chem Lett
Главные авторы: Khanna, Avinash, Côté, Alexandre, Arora, Shilpi, Moine, Ludivine, Gehling, Victor S., Brenneman, Jehrod, Cantone, Nico, Stuckey, Jacob I., Apte, Shruti, Ramakrishnan, Ashwin, Bruderek, Kamil, Bradley, William D., Audia, James E., Cummings, Richard T., Sims, Robert J., Trojer, Patrick, Levell, Julian R.
Формат: Artigo
Язык:Inglês
Опубликовано: American Chemical Society 2020
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC7294713/
https://ncbi.nlm.nih.gov/pubmed/32551002
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00045
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