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Nature Medicine, ISSN 1078-8956, 2014, Volume 20, Issue 1, pp. 87 - 92
Journal Article
by McDonald, E. Robert and de Weck, Antoine and Schlabach, Michael R and Billy, Eric and Mavrakis, Konstantinos J and Hoffman, Gregory R and Belur, Dhiren and Castelletti, Deborah and Frias, Elizabeth and Gampa, Kalyani and Golji, Javad and Kao, Iris and Li, Li and Megel, Philippe and Perkins, Thomas A and Ramadan, Nadire and Ruddy, David A and Silver, Serena J and Sovath, Sosathya and Stump, Mark and Weber, Odile and Widmer, Roland and Yu, Jianjun and Yu, Kristine and Yue, Yingzi and Abramowski, Dorothee and Ackley, Elizabeth and Barrett, Rosemary and Berger, Joel and Bernard, Julie L and Billig, Rebecca and Brachmann, Saskia M and Buxton, Frank and Caothien, Roger and Caushi, Justina X and Chung, Franklin S and Cortés-Cros, Marta and deBeaumont, Rosalie S and Delaunay, Clara and Desplat, Aurore and Duong, William and Dwoske, Donald A and Eldridge, Richard S and Farsidjani, Ali and Feng, JiaJia and Feng, Fei and Flemming, Daisy and Forrester, William and Galli, Giorgio G and Gao, Zhenhai and Gauter, François and Gibaja, Veronica and Haas, Kristy and Hattenberger, Marc and Hood, Tami and Hurov, Kristen E and Jagani, Zainab and Jenal, Mathias and Johnson, Jennifer A and Jones, Michael D and Kapoor, Avnish and Korn, Joshua and Liu, Jilin and Liu, Shumei and Liu, Qiumei and Liu, Yue and Loo, Alice T and Macchi, Kaitlin J and Martin, Typhaine and McAllister, Gregory and Meyer, Amandine and Mollé, Sandra and Pagliarini, Raymond A and Phadke, Tanushree and Repko, Brian and Schouwey, Tanja and Shanahan, Frances and Shen, Qiong and Stamm, Christelle and Stephan, Christine and Stucke, Volker M and Tiedt, Ralph and Varadarajan, Malini and Venkatesan, Kavitha and Vitari, Alberto C and Wallroth, Marco and Weiler, Jan and Zhang, Jing and Mickanin, Craig and Myer, Vic E and Porter, Jeffery A and Lai, Albert and Bitter, Hans and Lees, Emma and Keen, Nicholas and Kauffmann, Audrey and Stegmeier, Frank and Hofmann, Francesco and Schmelzle, Tobias and Sellers, William R
Cell, ISSN 0092-8674, 07/2017, Volume 170, Issue 3, pp. 577 - 592.e10
Journal Article
Molecular cancer therapeutics, ISSN 1535-7163, 08/2019
KRAS, an oncogene mutated in nearly one-third of human cancers, remains a pharmacological challenge for direct inhibition except for recent advances in... 
Journal Article
Structure, ISSN 0969-2126, 03/2017, Volume 25, Issue 3, pp. 506 - 513
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 10/2017, Volume 8, Issue 10, pp. 1116 - 1121
Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg132. Having identified... 
Mutant IDH1 | clinical candidate | inhibition of 2-HG production | in vivo anticancer activity | brain penetration | ISOCITRATE DEHYDROGENASE 1 | SELECTIVE-INHIBITION | CHEMISTRY, MEDICINAL | SMALL-MOLECULE | ACUTE MYELOID-LEUKEMIA | OPPORTUNITIES | HYPOXIA | Mutant IDHI | METABOLISM | MUTATIONS
Journal Article
Molecular Cancer Therapeutics, ISSN 1535-7163, 12/2015, Volume 14, Issue 12 Supplement 2, pp. LB-B04 - LB-B04
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 07/2018, Volume 9, Issue 7, pp. 746 - 751
Mutant isocitrate dehydrogenase 1 (IDH1) is an attractive therapeutic target for the treatment of various cancers such as AML, glioma, and glioblastoma. We... 
Mutant IDH1 | clinical candidate | inhibition of 2-HG production | in vivo anticancer activity | brain penetration | ISOCITRATE DEHYDROGENASE 1 | SELECTIVE-INHIBITION | CHEMISTRY, MEDICINAL | SMALL-MOLECULE | GLIOMA | MECHANISMS | IDENTIFICATION | REVEAL | DISCOVERY | IN-VIVO | MUTATIONS
Journal Article
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