M. Kawaguchi et al., A novel synthetic Arg-Gly-Asp-containing peptide cyclo(-RGDf=V-) is the potent inhibitor of angiogenesis, BIOC BIOP R, 288(3), 2001, pp. 711-717
Citations number
29
Categorie Soggetti
Biochemistry & Biophysics
Journal title
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Arg-Gly-Asp (RGD)-containing peptide is a ligand for integrin alpha (v)beta
(3) and acts as an angiogenic inhibitor. A novel cyclic RGD peptide, cyclo
(-RGDf=V-) (f=V), was synthesized and its biological activities were charac
terized and compared with its analogs, cyclo(-RGDfV-) (f=V) and cyclo(-RGDf
-MeV-) (fMeV). It bound to integrin alpha (v)beta (3) with almost the same
affinity as the fV and fMeV analogs. All three compounds inhibited the adhe
sion 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 ce
ll) inoculated mice, while fMeV had little effect. These results suggest th
e potential usefulness of the cyclo(-RGDf=V-) as an antiangiogenic agent fo
r clinical use in the future. (C) 2001 Academic Press.