E235 is an ATF4 Expression Regulator for Tumor Research
Activates transcription factor 4 (ATF4) is a cAMP-responsive element binding protein, belonging to the cAMP-responsive element binding protein (CREB)-2 protein family. This protein is divided into several structural domains that are crucial for the function and degradation of ATF4. Specifically, ATF4 is a stress-induced transcription factor that is frequently...
BLU2864 is An Orally Active PRKACA Kinase Inhibitor
Fibrolamellar carcinoma (FLC) is a rare, difficult-to-treat liver cancer primarily affecting pediatric and adolescent patients. An analysis of FLC tumor samples shows that protein kinase A (PKA) alpha catalytic subunit (PRKACA) is a critical molecular event in FLC pathogenesis. In this article, we will introduce an orally active, highly selective, ATP-competitive PRKACA...
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...