Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

[Image: see text] Somatic point mutations at a key arginine residue (R132) within the active site of the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) confer a novel gain of function in cancer cells, resulting in the production of d-2-hydroxyglutarate (2-HG), an oncometabolite. Elevated 2-HG le...

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Udgivet i:ACS Med Chem Lett
Main Authors: Popovici-Muller, Janeta, Lemieux, René M., Artin, Erin, Saunders, Jeffrey O., Salituro, Francesco G., Travins, Jeremy, Cianchetta, Giovanni, Cai, Zhenwei, Zhou, Ding, Cui, Dawei, Chen, Ping, Straley, Kimberly, Tobin, Erica, Wang, Fang, David, Muriel D., Penard-Lacronique, Virginie, Quivoron, Cyril, Saada, Véronique, de Botton, Stéphane, Gross, Stefan, Dang, Lenny, Yang, Hua, Utley, Luke, Chen, Yue, Kim, Hyeryun, Jin, Shengfang, Gu, Zhiwei, Yao, Gui, Luo, Zhiyong, Lv, Xiaobing, Fang, Cheng, Yan, Liping, Olaharski, Andrew, Silverman, Lee, Biller, Scott, Su, Shin-San M., Yen, Katharine
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2018
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5900343/
https://ncbi.nlm.nih.gov/pubmed/29670690
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00421
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