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.
Maeda
Noriyuki
N
Department of Medical Biochemistry and COE Program in the 21st Century, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Takeuchi
Yoshito
Y
Takada
Miki
M
Namba
Yukihiro
Y
Oku
Naoto
N
D000818:Animals; D003110:Colonic Neoplasms / Q000378:metabolism*; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D057927:Hydrophobic and Hydrophilic Interactions; D008055:Lipids / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D008081:Liposomes; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D010455:Peptides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D010714:Phosphatidylethanolamines / Q000737:chemistry; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
C490868:DSPE-PEG-SA; D004337:Drug Carriers; D008055:Lipids; D008081:Liposomes; D009842:Oligopeptides; D010455:Peptides; D010714:Phosphatidylethanolamines; C490869:alanyl-prolyl-arginyl-prolyl-glycine; C038089:1,2-distearoylphosphatidylethanolamine; D011092:Polyethylene Glycols