...in research to better understand or leverage the MOAs of well-established drug classes. These include 2-HG...
...the figure include proteins and metabolites that are targets or biomarkers for marketed drugs, including 2-HG...
...Angeles, Calif. University of Kansas, Lawrence, Kan. University of Pittsburgh, Pittsburgh, Pa. Targets 2-HG - 2-hydroxyglutarate...

...to gain-of-function in a tumor’s ability to catalyze the conversion of a-ketoglutarate into 2-hydroxyglutarate (2-HG) . 2-HG...
...found that AML cells with mutations in IDH1 and IDH2 also produce 2-HG and that 2-HG...
...Drug Administration (FDA), Silver Spring, Md. References Dang, L., et al. “Cancer-associated IDH1 mutations produce 2-hydroxyglutarate.”...

...inhibited tumor growth in IDH1-mutant mouse xenograft models compared to vehicle controls. The scientists identified 2-hydroxyglutarate...

...Indication: Treat recurrent IDH1-mutant glioma Endpoint: Dose-limiting toxicities (DLTs); safety, pharmacokinetics, change from baseline in 2-hydroxyglutarate (2-HG)...

...Intraoperative identification of isocitrate dehydrogenase 1 (IDH1)-mutant brain tumors via rapid mass spectrometric detection of 2-hydroxyglutarate (2-HG)...
...for detecting 2-HG correctly distinguished IDH1-mutant tumors from those without the mutation and showed that 2-HG...

...In primary human AML cells with mutant IDH2, AGI-6780 decreased levels of the (R)-enantiomer of 2-hydroxyglutarate (2-HG)...

...In a mouse xenograft model for human glioma, AGI-5198 decreased levels of the (R)-enantiomer of 2-hydroxyglutarate (2-HG)...

...the mutant enzyme can further convert a-KG to an oncogenic metabolite called ( R )- 2-hydroxyglutarate...

...additional ability to catalyze the formation of the ( R ) enantiomer of 2-hydroxyglutarate ( 2-HG...
...mutations in IDH1 can produce large quantities of 2-HG, though it was still unclear how 2-HG...
...show that the ( R ) enantiomer of 2-HG drove leukemogenesis and that ( S )-2-HG...

...whereas (S)-2-HG and vehicle did not. In the two cell lines, a compound that blocked 2-HG...
...markers of leukemic transformation, whereas vehicle did not. Next steps include evaluating the inhibition of (R)-2-HG...