A Novel Synthetic Arg-Gly-Asp-Containing Peptide Cyclo(-RGDfV-) Is the Potent Inhibitor of Angiogenesis
| Autor: | Shinya Ohishi, Ryuichiro Doi, Toshihiko Masui, Masayuki Imamura, Shouichiro Tsuji, Michihiko Wada, Jun Ida, Eiji Toyoda, Michiya Kawaguchi, Ryo Hosotani, Sanae Nakajima, Sidhartha Tulachan, Nobutaka Fujii, Koji Fujimoto, Masayuki Koizumi |
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| Rok vydání: | 2001 |
| Předmět: |
Male
Stereochemistry Angiogenesis Integrin Cell Biophysics Mice Nude Peptide Peptides Cyclic Biochemistry Mice In vivo medicine Animals Humans Binding site Molecular Biology Cells Cultured chemistry.chemical_classification Mice Inbred BALB C Binding Sites Neovascularization Pathologic biology Neoplasms Experimental Cell Biology Ligand (biochemistry) In vitro Disease Models Animal medicine.anatomical_structure chemistry biology.protein Endothelium Vascular Oligopeptides Neoplasm Transplantation |
| Zdroj: | Biochemical and Biophysical Research Communications. 288:711-717 |
| ISSN: | 0006-291X |
| DOI: | 10.1006/bbrc.2001.5809 |
| Popis: | Arg-Gly-Asp (RGD)-containing peptide is a ligand for integrin alpha(V)beta3 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 alpha(V)beta3 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. |
| Databáze: | OpenAIRE |
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