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 language | English |
|---|---|
| Pages (from-to) | 711-717 |
| Number of pages | 7 |
| Journal | Biochemical and Biophysical Research Communications |
| Volume | 288 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 02-11-2001 |
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All Science Journal Classification (ASJC) codes
- Biophysics
- Biochemistry
- Molecular Biology
- Cell Biology
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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 journal › Article
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
VL - 288
SP - 711
EP - 717
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
SN - 0006-291X
IS - 3
ER -