Synthesis of angiogenesis-targeted peptide and hydrophobized polyethylene glycol conjugate

For the purpose of cancer antineovascular therapy, a novel angiogenesis-targeted peptide, Ala-Pro-Arg-Pro-Gly, (APRPG) was attached to hydrophobized polyethylene glycol (distearoylphosphatidylethanolamine [DSPE]-PEG). DSPE-PEG and the 5-mer peptide were condensed with DCC-HOBt method. Liposome modified with this DSPE-PEG-APRPG conjugate highly accumulated in tumor of tumor-bearing mice.