Category: Fibrosarcoma

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...

CRT0044876 is a Potent and Selective APE1 Inhibitor

The base excision repair (BER) pathway is essential for the removal of DNA bases damaged by alkylation or oxidation. This pathway also handles a variety of other lesions including deaminated bases and DNA single-strand breaks. A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate...