Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo

[Image: see text] Optimization of a series of R132H IDH1 inhibitors from a high throughput screen led to the first potent molecules that show robust tumor 2-HG inhibition in a xenograft model. Compound 35 shows good potency in the U87 R132H cell based assay and ∼90% tumor 2-HG inhibition in the corr...

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Detalhes bibliográficos
Main Authors: Popovici-Muller, Janeta, Saunders, Jeffrey O., Salituro, Francesco G., Travins, Jeremy M., Yan, Shunqi, Zhao, Fang, Gross, Stefan, Dang, Lenny, Yen, Katharine E., Yang, Hua, Straley, Kimberly S., Jin, Shengfang, Kunii, Kaiko, Fantin, Valeria R., Zhang, Shunan, Pan, Qiongqun, Shi, Derek, Biller, Scott A., Su, Shinsan M.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2012
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025665/
https://ncbi.nlm.nih.gov/pubmed/24900389
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml300225h
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