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Cancer chemotherapy targeted to angiogenic vessels is expected to cause indirect tumor regression through the damage of the neovasculature without the induction of drug resistance. To develop a tool for neovasculaturespeci®c drug delivery, we isolated novel peptides homing to angiogenic vessels formed by a dorsal air sac method from a phage-displayed peptide library. Three distinct phage clones that markedly accumulated in murine tumor xenografts presented PRPGAPLAGSWPGTS-, DRWRPALPVVLFPLH-or ASSSYPLIHWRPWARpeptide respectively. After the determination of the epitope sequences of these peptides, we modi®ed liposomes with epitope penta-peptides. Liposome modi®ed with APRPG-peptide showed high accumulation in murine tumor xenografts, and APRPG-modi®ed liposome encapsulating adriamycin eectively suppressed experimental tumor growth. Finally, speci®c binding of APRPG-modi®ed liposome to human umbilical endothelial cells, and that of PRP-containing peptide to angiogenic vessels in human tumors, i.e., islet cell tumor and glioblastoma, were demonstrated. The present study indicates the usefulness of APRPG-peptide as a tool for anti-neovascular therapy, a novel modality of cancer treatment.

During the process of sensitization to FITC, DBP, and DPP exert strong adjuvant effects that are associated with enhancement of trafficking of antigen-presenting dendritic cells from the skin to draining lymph nodes.

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