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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書誌詳細
主要な著者: 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.
フォーマット: Artigo
言語:Inglês
出版事項: American Chemical Society 2012
オンライン･アクセス: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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