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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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5900343/
https://www.ncbi.nlm.nih.gov/pubmed/29670690
http://dx.doi.org/10.1021/acsmedchemlett.7b00421

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