In vivo efficacy of mutant IDH1 inhibitor HMS-101 and structural resolution of distinct binding site

Mutations in isocitrate dehydrogenase 1 (IDH1) are found in 6% of AML patients. Mutant IDH produces R-2-hydroxyglutarate (R2HG), which induces histone- and DNA-hypermethylation through inhibition of epigenetic regulators, thus linking metabolism to tumorigenesis. Here we report the biochemical chara...

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Publicado no:Leukemia
Main Authors: Chaturvedi, Anuhar, Goparaju, Ramya, Gupta, Charu, Weder, Julia, Klünemann, Thomas, Araujo Cruz, Michelle Maria, Kloos, Arnold, Goerlich, Kerstin, Schottmann, Renate, Othman, Basem, Struys, Eduard A., Bähre, Heike, Grote-Koska, Denis, Brand, Korbinian, Ganser, Arnold, Preller, Matthias, Heuser, Michael
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6995692/
https://ncbi.nlm.nih.gov/pubmed/31586149
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41375-019-0582-x
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