Effect of RGD-4C position is more important than disulfide bonds on antiangiogenic activity of RGD-4C modified endostatin derived synthetic polypeptide.

Abstract	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 the targeted delivery of ES-2 to tumors and further enhance the activity, the polypeptide RGD-4C (ACDCRGDCFC) was introduced into ES-2, and the effects of RGD-4C position and RGD-4C disulfide bonds on polypeptides activity were investigated. When RGD-4C polypeptides (with or without disulfide bonds) were introduced to the N-terminals of synthesized ES-2, the modified ES-2 showed significant antitumor activity in vivo. Cell proliferation and chicken chorioallantoic membrane (CAM) assay results showed that disulfide bonds had no significant effects on RGD-4C-modified ES-2 antiangiogenic activity. Furthermore, the target of modified peptides was integrin alpha5beta1, rather than integrin alphavbeta3 as previous studies mentioned.
Authors	Runting Yin, Heng Zheng, Tao Xi, Han-Mei Xu
Journal	Bioconjugate chemistry (Bioconjug Chem) Vol. 21 Issue 7 Pg. 1142-7 (Jul 21 2010) ISSN: 1520-4812 [Electronic] United States
PMID	20515045 (Publication Type: Journal Article)
Chemical References	AP25 peptide Angiogenesis Inhibitors Antineoplastic Agents Disulfides Endostatins Integrin alpha5beta1 Peptide Fragments Peptides
Topics	Angiogenesis Inhibitors (chemical synthesis, chemistry, pharmacology) Animals Antineoplastic Agents (chemical synthesis, chemistry, pharmacology) Binding, Competitive Cattle Cell Line Cell Proliferation (drug effects) Chickens Chorioallantoic Membrane (drug effects) Disulfides (metabolism) Drug Screening Assays, Antitumor Endostatins (chemical synthesis, chemistry, pharmacology) Endothelial Cells (drug effects) Female Humans Integrin alpha5beta1 (chemistry) Mice Mice, Inbred C57BL Peptide Fragments (chemical synthesis, chemistry, pharmacology) Peptides (chemical synthesis, chemistry, pharmacology)

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