A Menin-MLL inhibitor induces specific chromatin changes and eradicates disease in models of MLL-rearranged leukemia

Inhibition of the Menin (MEN1) and MLL (MLL1, KMT2A) interaction is a potential therapeutic strategy for MLL-rearranged (MLL-r) leukemia. Structure-based design yielded the potent, highly selective and orally-bioavailable small molecule inhibitor VTP50469. Cell lines carrying MLL-rearrangements were...

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Pubblicato in:Cancer Cell
Autori principali: Krivtsov, Andrei V., Evans, Kathryn, Gadrey, Jayant Y., Eschle, Benjamin K., Hatton, Charlie, Uckelmann, Hannah J., Ross, Kenneth N., Perner, Florian, Olsen, Sarah N., Pritchard, Tara, McDermott, Lisa, Jones, Connor D., Jing, Duohui, Braytee, Ali, Chacon, Diego, Earley, Eric, McKeever, Brian M., Claremon, David, Gifford, Andrew J., Lee, Heather J., Teicher, Beverly A., Pimanda, John E., Beck, Dominik, Perry, Jennifer A., Smith, Malcolm A., McGeehan, Gerard M., Lock, Richard B., Armstrong, Scott A.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2019
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7227117/
https://ncbi.nlm.nih.gov/pubmed/31821784
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ccell.2019.11.001
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