Effect of RGD-4C Position is More Important Than Disulfide Bonds on Antiangiogenic Activity of RGD-4C Modified Endostatin Derived Synthetic Polypeptide

• DOI: 10.1021/bc900292y
• Publication Date: 2010-06-01T19:01:09Z
• Authors: Runting Yin; Heng Zheng; Tao Xi; Han-Mei Xu
• Keywords: Endostatin

ES-2 (IVRRADRAAVP), an endostatin-derived synthetic polypeptide, contains the amino acids 50-60 of endostatin from its N terminus, and it had no inhibitory effects on tumor growth in vivo. In order to increase targeted delivery tumors further enhance activity, polypeptide RGD-4C (ACDCRGDCFC) was introduced into ES-2, position disulfide bonds polypeptides activity were investigated. When (with or without bonds) N-terminals synthesized modified showed significant antitumor Cell proliferation chicken chorioallantoic membrane (CAM) assay results that RGD-4C-modified antiangiogenic activity. Furthermore, target peptides integrin alpha5beta1, rather than alphavbeta3 as previous studies mentioned.