Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong in vivo Antitumor Activity

Targeting the menin-MLL protein-protein interaction is a new therapeutic strategy for the treatment of acute leukemia carrying MLL fusion (MLL leukemia). We describe herein the structure-based optimization of a class of covalent menin inhibitors, which led to the discovery of M-808 (16) as a highly...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Xu, Shilin, Aguilar, Angelo, Huang, Liyue, Xu, Tianfeng, Zheng, Ke, McEachern, Donna, Przybranowski, Sally, Foster, Caroline, Zawacki, Kaitlin, Liu, Zhaomin, Chinnaswamy, Krishnapriya, Stuckey, Jeanne, Wang, Shaomeng
Formato: Artigo
Idioma:Inglês
Publicado em: 2020
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7981784/
https://ncbi.nlm.nih.gov/pubmed/32338903
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c00547
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