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

doi:10.1006/bbrc.2001.5809

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

Gastrointestinal Surgery

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23 Citations (Scopus)

Abstract

Arg-Gly-Asp (RGD)-containing peptide is a ligand for integrin α_vβ₃ 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 α_vβ₃ 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 language	English
Pages (from-to)	711-717
Number of pages	7
Journal	Biochemical and Biophysical Research Communications
Volume	288
Issue number	3
DOIs	https://doi.org/10.1006/bbrc.2001.5809
Publication status	Published - 02-11-2001

All Science Journal Classification (ASJC) codes

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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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, 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, Shouichiro ; 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.

@article{ccddb81742b64fbb8e2e0908ae176c6f,

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

note = "Funding Information: This work was supported in part by a Grant-in-Aid for Scientific Research from the Japan Ministry of Education, Science and Culture. We thank Y. Tani (DAKO), N. Yawata, and K. Ajito (Meiji Pharmaceuticals) for their excellent technical support.",

year = "2001",

month = nov,

day = "2",

doi = "10.1006/bbrc.2001.5809",

language = "English",

volume = "288",

pages = "711--717",

journal = "Biochemical and Biophysical Research Communications",

issn = "0006-291X",

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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, Shouichiro; 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 journal › Article › peer-review

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, Shouichiro

AU - Ida, Jun

AU - Fujimoto, Koji

AU - Wada, Michihiko

AU - Doi, Ryuichiro

AU - Imamura, Masayuki

N1 - Funding Information: This work was supported in part by a Grant-in-Aid for Scientific Research from the Japan Ministry of Education, Science and Culture. We thank Y. Tani (DAKO), N. Yawata, and K. Ajito (Meiji Pharmaceuticals) for their excellent technical support.

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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DO - 10.1006/bbrc.2001.5809

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JO - Biochemical and Biophysical Research Communications

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SN - 0006-291X

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ER -

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

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