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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Publicat a:ACS Med Chem Lett
Autors principals: 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.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2020
Accés en línia: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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