Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity

ASH1L histone methyltransferase plays a crucial role in the pathogenesis of different diseases, including acute leukemia. While ASH1L represents an attractive drug target, developing ASH1L inhibitors is challenging, as the catalytic SET domain adapts an inactive conformation with autoinhibitory loop...

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Publicado no:Nat Commun
Main Authors: Rogawski, David S., Deng, Jing, Li, Hao, Miao, Hongzhi, Borkin, Dmitry, Purohit, Trupta, Song, Jiho, Chase, Jennifer, Li, Shuangjiang, Ndoj, Juliano, Klossowski, Szymon, Kim, EunGi, Mao, Fengbiao, Zhou, Bo, Ropa, James, Krotoska, Marta Z., Jin, Zhuang, Ernst, Patricia, Feng, Xiaomin, Huang, Gang, Nishioka, Kenichi, Kelly, Samantha, He, Miao, Wen, Bo, Sun, Duxin, Muntean, Andrew, Dou, Yali, Maillard, Ivan, Cierpicki, Tomasz, Grembecka, Jolanta
Formato: Artigo
Idioma:Inglês
Publicado em: Nature Publishing Group UK 2021
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8121805/
https://ncbi.nlm.nih.gov/pubmed/33990599
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41467-021-23152-6
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