TfR-1-IN-1

TfR-1-IN-1 is a small molecule inhibitor of Transferrin Receptor 1 (TFRC, also known as CD71). TFRC is a transmembrane glycoprotein that mediates cellular iron uptake by binding and internalizing iron-saturated transferrin via receptor-mediated endocytosis. Because rapidly dividing cancer cells have an elevated requirement for iron, TFRC is frequently overexpressed in various malignancies, including gastric adenocarcinoma. TfR-1-IN-1 functions by blocking the TFRC-mediated iron uptake pathway, leading to intracellular iron depletion and subsequent inhibition of cell proliferation. Recent research has highlighted its potential in treating extrachromosomal DNA (ecDNA)-positive gastric cancers, which appear to be selectively vulnerable to TFRC inhibition, particularly when used in synergistic combination with DNA damage response inhibitors such as CHK1 inhibitors.

Other names

TFRC inhibitor 1Transferrin Receptor 1 Inhibitor 1