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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Détails bibliographiques
Publié dans:Leukemia
Auteurs principaux: 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
Format: Artigo
Langue:Inglês
Publié: 2019
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Article
Accès en ligne: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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