A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis

Michiya Kawaguchi, Ryo Hosotani, Shinya Ohishi, Nobutaka Fujii, Sidhartha Singh Tulachan, Masayuki Koizumi, Eiji Toyoda, Toshihiko Masui, Sanae Nakajima, Shoichiro Tsuji, Jun Ida, Koji Fujimoto, Michihiko Wada, Ryuichiro Doi, Masayuki Imamura

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Arg-Gly-Asp (RGD)-containing peptide is a ligand for integrin αvβ3 and acts as an angiogenic inhibitor. A novel cyclic RGD peptide, cyclo(-RGDf=V-) (f=V), was synthesized and its biological activities were characterized and compared with its analogs, cyclo(-RGDfV-) (fV) and cyclo(-RGDf-MeV-) (fMeV). It bound to integrin αvβ3 with almost the same affinity as the fV and fMeV analogs. All three compounds inhibited the adhesion and growth of HUVEC cells in a dose-dependent manner in vitro. Out of three, fMeV had the strongest effect, f=V was almost as strong as fMeV, and fV had the least effect. However, in vivo, f=V significantly decreased the intratumoral microvessel density (MVD) in the DLD-1 (human colon cancer cell) inoculated mice, while fMeV had little effect. These results suggest the potential usefulness of the cyclo-(-RGDf=V-) as an antiangiogenic agent for clinical use in the future.

Original languageEnglish
Pages (from-to)711-717
Number of pages7
JournalBiochemical and Biophysical Research Communications
Issue number3
Publication statusPublished - 02-11-2001


All Science Journal Classification (ASJC) codes

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

Cite this

Kawaguchi, M., Hosotani, R., Ohishi, S., Fujii, N., Singh Tulachan, S., Koizumi, M., Toyoda, E., Masui, T., Nakajima, S., Tsuji, S., Ida, J., Fujimoto, K., Wada, M., Doi, R., & Imamura, M. (2001). A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis. Biochemical and Biophysical Research Communications, 288(3), 711-717. https://doi.org/10.1006/bbrc.2001.5809