TY - JOUR T1 - Targeted Drug Delivery via the Transferrin Receptor-Mediated Endocytosis Pathway JF - Pharmacological Reviews JO - Pharmacol Rev SP - 561 LP - 587 DO - 10.1124/pr.54.4.561 VL - 54 IS - 4 AU - Zhong Ming Qian AU - Hongyan Li AU - Hongzhe Sun AU - Kwokping Ho Y1 - 2002/12/01 UR - http://pharmrev.aspetjournals.org/content/54/4/561.abstract N2 - The membrane transferrin receptor-mediated endocytosis or internalization of the complex of transferrin bound iron and the transferrin receptor is the major route of cellular iron uptake. This efficient cellular uptake pathway has been exploited for the site-specific delivery not only of anticancer drugs and proteins, but also of therapeutic genes into proliferating malignant cells that overexpress the transferrin receptors. This is achieved either chemically by conjugation of transferrin with therapeutic drugs, proteins, or genetically by infusion of therapeutic peptides or proteins into the structure of transferrin. The resulting conjugates significantly improve the cytotoxicity and selectivity of the drugs. The coupling of DNA to transferrin via a polycation or liposome serves as a potential alternative to viral vector for gene therapy. Moreover, the OX26 monoclonal antibody against the rat transferrin receptor offers great promise in the delivery of therapeutic agents across the blood-brain barrier to the brain. ER -