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, Shouichiro Tsuji, Jun Ida, Koji Fujimoto, Michihiko Wada, Ryuichiro Doi, Masayuki Imamura

研究成果: Article査読

23 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)711-717
ページ数7
ジャーナルBiochemical and Biophysical Research Communications
288
3
DOI
出版ステータスPublished - 02-11-2001

All Science Journal Classification (ASJC) codes

  • 生物理学
  • 生化学
  • 分子生物学
  • 細胞生物学

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