Synthesis of doxorubicin–peptide conjugate with multidrug resistant tumor cell killing activity

Cell penetrating peptide TAT was introduced into doxorubicin structure. Synthesized doxorubicin–TAT conjugate showed different intracellular distribution pattern and cell killing activity from those of free doxorubicin. Unlike free doxorubicin, doxorubicin–TAT conjugate was highly permeable to drug-resistant cells and was able to kill drug-resistant tumor cells efficiently.