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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Vydáno v:Nat Commun
Hlavní autoři: 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
Médium: Artigo
Jazyk:Inglês
Vydáno: Nature Publishing Group UK 2021
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On-line přístup: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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