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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8121805/
https://www.ncbi.nlm.nih.gov/pubmed/33990599
http://dx.doi.org/10.1038/s41467-021-23152-6

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