TRF-DOX

**TRF-DOX** is a targeted conjugate of doxorubicin (DOX), an anthracycline antibiotic, covalently linked to transferrin (TRF) via a Schiff base stable at physiological pH 7.4 but releasable at acidic pH 5 in endosomes/lysosomes. It exploits overexpression of transferrin receptors on cancer cells for selective delivery, enhancing cytotoxicity in leukemia cell lines (e.g., CCRF-CEM, K562, doxorubicin-resistant K562/DOX) compared to free DOX, while showing reduced toxicity to normal PBMCs. DOX induces apoptosis via ROS generation, mitochondrial membrane potential collapse, cytochrome c release, and elevated intracellular calcium; the conjugate amplifies these effects, particularly overcoming P-gp-mediated multidrug resistance by lower substrate affinity and less P-gp conformational change/induction. In vivo, it selectively binds tumors, inhibits growth better than unmodified DOX, and improves survival.[1][2][3][5]

Other names

DOX-TRFdoxorubicin-transferrin conjugate