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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Pubblicato in:ACS Med Chem Lett
Autori principali: 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.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2020
Accesso online: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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