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Amino acids and peptides. XXIX. Synthesis and antimetastatic effects of peptides and peptide-poly(ethylene glycol) hybrids related to the core sequence of the type III connecting segment domain of fibronectin.

Abstract
Peptides (H-Glu-Ile-Leu-Asp-Val-NH2, H-Glu-Ile-Leu-Asp-Val-Pro-Ser-Thr-NH2, H-Arg-Glu-Asp-Val-NH2) and their poly(ethylene glycol) (PEG) hybrids related to the core sequence of the type III connecting segment domain of fibronectin A chain were prepared by the solution method or the solid phase method. Their inhibitory effects on the adhesion and migration of B16-BL6 melanoma cells to fibronectin were assessed in vitro, and their therapeutic potency against tumor metastasis were also examined. Anti-adhesive and anti-migrative effects of the synthetic fibronectin-related peptids were superior to those of their PEG hybrids, so we found that the in vitro bioactivity of peptides decreased by PEGylation. In the in vivo assay, we found that the synthetic peptides containing Glu-Ile-Leu-Asp-Val and Arg-Glu-Asp-Val sequences exhibited an inhibitory effect on the experimental metastasis of B16-BL6 melanoma. Of the synthetic peptides, H-Glu-Ile-Leu-Asp-Val-NH2 exhibited the most potent inhibitory effect. Hybrid formation of Arg-Glu-Asp-Val with poly(ethylene glycol) resulted in potentiation of the inhibitory effect of the parent peptides. A mixture composed of PEG hybrids of Glu-Ile-Leu-Asp-Val, Arg-Glu-Asp-Val and Tyr-Ile-Gly-Ser-Arg dramatically inhibited tumor metastasis.
AuthorsK Kawasaki, M Maeda, S Inoue, Y Yamashiro, Y Kaneda, Y Mu, Y Tsutsumi, S Nakagawa, T Mayumi
JournalBiological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 19 Issue 12 Pg. 1574-9 (Dec 1996) ISSN: 0918-6158 [Print] Japan
PMID8996642 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Fibronectins
  • Peptides
  • Polyethylene Glycols
Topics
  • Animals
  • Antineoplastic Agents (chemical synthesis, pharmacology)
  • Cell Adhesion (drug effects)
  • Cell Movement (drug effects)
  • Fibronectins (chemistry)
  • Lung Neoplasms (prevention & control, secondary)
  • Melanoma, Experimental (drug therapy, pathology)
  • Mice
  • Mice, Inbred C57BL
  • Neoplasm Transplantation
  • Peptides (chemical synthesis, pharmacology)
  • Polyethylene Glycols (chemical synthesis, pharmacology)

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