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Covalent inhibition of NSD1 histone methyltransferase

The NSD family of histone methyltransferases is associated with various malignancies, including aggressive acute leukemia with NUP98-NSD1 translocation. While NSD proteins represent attractive drug targets, their catalytic SET domains exist in autoinhibited conformation, presenting significant chall...

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Veröffentlicht in:Nat Chem Biol
Hauptverfasser: Huang, Huang, Howard, Christina A., Zari, Sergei, Cho, Hyo Je, Shukla, Shirish, Li, Hao, Ndoj, Juliano, González-Alonso, Paula, Nikolaidis, Caroline, Abbott, Joshua, Rogawski, David S., Potopnyk, Mykhaylo A., Kempinska, Katarzyna, Miao, Hongzhi, Purohit, Trupta, Henderson, Andrew, Mapp, Anna, Sulis, Maria Luisa, Ferrando, Adolfo, Grembecka, Jolanta, Cierpicki, Tomasz
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2020
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Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7669657/
https://ncbi.nlm.nih.gov/pubmed/32868895
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41589-020-0626-6
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