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.
Liang
Jun F
JF
Department of Chemistry and Chemical Biology, Stevens Institute of Technology, Hoboken, NJ 07030, USA. jliang2@stevens.edu
Yang
Victor C
VC
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002463:Cell Membrane Permeability / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000737:chemistry* / Q000494:pharmacology*; D018432:Drug Resistance, Multiple; D006801:Humans; D008969:Molecular Sequence Data; D015394:Molecular Structure; D009369:Neoplasms / Q000473:pathology*; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D000970:Antineoplastic Agents; D010455:Peptides; D004317:Doxorubicin