Vorasidenib (AG-881) is an Orally Available, Brain Penetrant and dual mIDH1/2 Inhibitor
Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes. They catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. However, mutant IDH1/2 (mIDH1/2) reduces α-KG to the oncometabolite 2-hydroxyglutarate (2-HG). Inhibition of the mutant IDH (mIDH) protein represents a targeted approach to cancer treatment for...
FAPI-46 is a Quinoline-Based Fibroblast Activation Protein (FAP)-Targeted Radiotracer
The proline-selective serine protease fibroblast activation protein (FAP) is a type II transmembrane glycoprotein. It is related to the dipeptidyl peptidases (DPPs) DPP2, DPP4, DPP8 and DPP9 and furthermore related to the endopeptidase prolyl oligopeptidase (PREP). FAP combines DPP and endopeptidase activities. FAP is not detectable in most healthy...