Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
Author:
Affiliation:
1. Agios Pharmaceuticals Inc., Cambridge, Massachusetts 02139, United States
2. PharmaResources, Shanghai 201201, China
3. INSERM U1170 and Gustave Roussy, Villejuif 94800, France
4. ChemPartner, Shanghai 201203, China
Funder
Association pour la Recherche sur le Cancer
Ligue Contre le Cancer
Minist?re des Affaires Sociales et de la Sant?
Institut National Du Cancer
Minist?re de l'Education Nationale, de l'Enseignement Superieur et de la Recherche
Agios Pharmaceuticals Inc.
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry,Drug Discovery,Biochemistry
Link
http://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.7b00421
Reference18 articles.
1. Isocitrate Dehydrogenase Mutation and (R)-2-Hydroxyglutarate: From Basic Discovery to Therapeutics Development
2. Cancer-associated IDH1 mutations produce 2-hydroxyglutarate
3. Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation
4. IDH mutation impairs histone demethylation and results in a block to cell differentiation
5. An Inhibitor of Mutant IDH1 Delays Growth and Promotes Differentiation of Glioma Cells
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