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

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

The histone methyltransferase ASH1L plays a role in various diseases, including cancer, and has been validated as a therapeutic target; however, no inhibitors of ASH1L have been reported. Here the authors present small molecule inhibitors of ASH1L and demonstrate their on-target activity in leukemia...

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Main Authors: David S. Rogawski, Jing Deng, Hao Li, Hongzhi Miao, Dmitry Borkin, Trupta Purohit, Jiho Song, Jennifer Chase, Shuangjiang Li, Juliano Ndoj, Szymon Klossowski, EunGi Kim, Fengbiao Mao, Bo Zhou, James Ropa, Marta Z. Krotoska, Zhuang Jin, Patricia Ernst, Xiaomin Feng, Gang Huang, Kenichi Nishioka, Samantha Kelly, Miao He, Bo Wen, Duxin Sun, Andrew Muntean, Yali Dou, Ivan Maillard, Tomasz Cierpicki, Jolanta Grembecka
Format: article
Language:EN
Published: Nature Portfolio 2021
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Science
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Online Access:https://doaj.org/article/a51c519c90294569ac5da97219844f37
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https://doaj.org/article/a51c519c90294569ac5da97219844f37

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