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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Published in:Cancer Cell
Main Authors: 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.
Format: Artigo
Language:Inglês
Published: 2019
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Article
Online Access: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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