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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Nature Portfolio
2021
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oai:doaj.org-article:a51c519c90294569ac5da97219844f372021-12-02T15:43:05ZDiscovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity10.1038/s41467-021-23152-62041-1723https://doaj.org/article/a51c519c90294569ac5da97219844f372021-05-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-23152-6https://doaj.org/toc/2041-1723The 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 cells and a mouse model of leukemia.David S. RogawskiJing DengHao LiHongzhi MiaoDmitry BorkinTrupta PurohitJiho SongJennifer ChaseShuangjiang LiJuliano NdojSzymon KlossowskiEunGi KimFengbiao MaoBo ZhouJames RopaMarta Z. KrotoskaZhuang JinPatricia ErnstXiaomin FengGang HuangKenichi NishiokaSamantha KellyMiao HeBo WenDuxin SunAndrew MunteanYali DouIvan MaillardTomasz CierpickiJolanta GrembeckaNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-14 (2021) |
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Science Q 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 Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity |
| description |
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 cells and a mouse model of leukemia. |
| format |
article |
| author |
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 |
| author_facet |
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 |
| author_sort |
David S. Rogawski |
| title |
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity |
| title_short |
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity |
| title_full |
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity |
| title_fullStr |
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity |
| title_full_unstemmed |
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity |
| title_sort |
discovery of first-in-class inhibitors of ash1l histone methyltransferase with anti-leukemic activity |
| publisher |
Nature Portfolio |
| publishDate |
2021 |
| url |
https://doaj.org/article/a51c519c90294569ac5da97219844f37 |
| work_keys_str_mv |
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