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

Research output: Contribution to journalArticle

23 Citations (Scopus)

Abstract

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
Volume288
Issue number3
DOIs
Publication statusPublished - 02-11-2001

Fingerprint

Angiogenesis Inhibitors
Integrins
Cyclic Peptides
Peptides
Human Umbilical Vein Endothelial Cells
Microvessels
Bioactivity
Colonic Neoplasms
Adhesion
Cells
Ligands
Growth
arginyl-glycyl-aspartic acid
In Vitro Techniques
cyclo(arginyl-glycyl-aspartyl-phenylalanyl-valyl)
cyclic arginine-glycine-aspartic acid peptide

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., ... 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
Kawaguchi, Michiya ; Hosotani, Ryo ; Ohishi, Shinya ; Fujii, Nobutaka ; Singh Tulachan, Sidhartha ; Koizumi, Masayuki ; Toyoda, Eiji ; Masui, Toshihiko ; Nakajima, Sanae ; Tsuji, Shoichiro ; Ida, Jun ; Fujimoto, Koji ; Wada, Michihiko ; Doi, Ryuichiro ; Imamura, Masayuki. / A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis. In: Biochemical and Biophysical Research Communications. 2001 ; Vol. 288, No. 3. pp. 711-717.
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title = "A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis",
abstract = "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.",
author = "Michiya Kawaguchi and Ryo Hosotani and Shinya Ohishi and Nobutaka Fujii and {Singh Tulachan}, Sidhartha and Masayuki Koizumi and Eiji Toyoda and Toshihiko Masui and Sanae Nakajima and Shoichiro Tsuji and Jun Ida and Koji Fujimoto and Michihiko Wada and Ryuichiro Doi and Masayuki Imamura",
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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, vol. 288, no. 3, pp. 711-717. https://doi.org/10.1006/bbrc.2001.5809

A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis. / Kawaguchi, Michiya; Hosotani, Ryo; Ohishi, Shinya; Fujii, Nobutaka; Singh Tulachan, Sidhartha; Koizumi, Masayuki; Toyoda, Eiji; Masui, Toshihiko; Nakajima, Sanae; Tsuji, Shoichiro; Ida, Jun; Fujimoto, Koji; Wada, Michihiko; Doi, Ryuichiro; Imamura, Masayuki.

In: Biochemical and Biophysical Research Communications, Vol. 288, No. 3, 02.11.2001, p. 711-717.

Research output: Contribution to journalArticle

TY - JOUR

T1 - A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis

AU - Kawaguchi, Michiya

AU - Hosotani, Ryo

AU - Ohishi, Shinya

AU - Fujii, Nobutaka

AU - Singh Tulachan, Sidhartha

AU - Koizumi, Masayuki

AU - Toyoda, Eiji

AU - Masui, Toshihiko

AU - Nakajima, Sanae

AU - Tsuji, Shoichiro

AU - Ida, Jun

AU - Fujimoto, Koji

AU - Wada, Michihiko

AU - Doi, Ryuichiro

AU - Imamura, Masayuki

PY - 2001/11/2

Y1 - 2001/11/2

N2 - 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.

AB - 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.

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U2 - 10.1006/bbrc.2001.5809

DO - 10.1006/bbrc.2001.5809

M3 - Article

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AN - SCOPUS:0035798080

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EP - 717

JO - Biochemical and Biophysical Research Communications

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