Figure 1.
Schematic illustration of iron metabolism dysregulation in drug-resistant cancer cells leading to ferroptosis. Transferrin-bound Fe³+ binds to transferrin receptor 1 (TfR1) on the cell membrane; iron regulatory proteins (IRP1/IRP2) upregulate TfR1 transcription/translation, promoting endocytosis of the transferrin-iron complex. In the acidic endosomal environment (pH 5.5–6.0), Fe³+ dissociates, is reduced to Fe²+ by STEAP3, and is exported to the cytosol via DMT1. Meanwhile, nuclear receptor coactivator 4 (NCOA4) recognizes ferritin heavy chain 1 (FTH1) of the ferritin complex (FTH1-FTL, storing ~4,500 Fe³+ ions), mediating ferritin sequestration into autophagosomes. Autophagosome-lysosome fusion triggers ferritin degradation by cathepsin B, releasing additional Fe³+ (subsequently reduced to Fe²+). The accumulated Fe²+ expands the labile iron pool (LIP), mediating the Fenton reaction to generate hydroxyl radicals (•OH). These radicals induce lipid peroxidation, leading to phospholipid hydroperoxide (PLOOH) accumulation, membrane damage, and ultimately ferroptosis in drug-resistant cancer cells.
