Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2

Increased activity of the lysine methyltransferase NSD2 driven by translocation and activating mutations is associated with multiple myeloma and acute lymphoblastic leukemia, but no NSD2-targeting chemical probe has been reported to date. Here, we present the first antagonists that block the protein...

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Autores principales: Renato Ferreira de Freitas, Yanli Liu, Magdalena M. Szewczyk, Naimee Mehta, Fengling Li, David McLeod, Carlos Zepeda‐Velázquez, David Dilworth, Ronan P. Hanley, Elisa Gibson, Peter J. Brown, Rima Al‐awar, Lindsey I. James, C.H. Arrowsmith, Dalia Baršytė-Lovejoy, Jinrong Min, Masoud Vedadi, Matthieu Schapira, Abdellah Allali‐Hassani
Formato: Artigo
Lenguaje:inglés
Publicado: 2021
Acceso en línea:https://doi.org/10.1021/acs.jmedchem.0c01768
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