We have investigated the effect of cyclo- (Arg-Gly-Asp-D-Phe-Val) (cRGDfV) peptide on survival of human malignant glioma cells in vitro and in vivo. Immunofluorescent analyses revealed the presence of α V β 3 integrin on U-87MG and U-373MG cells, but minimal expression on U …

2012年10月15日 · Molecular structures, properties and hydrogen bonding in 10 models of cyclic-five-member-ring pentapeptides containing Arginine–Glycine–Aspartic acid (RGD) have been studied at B3LYP/6-311G(d,p) theoretical level. Among the investigated models, five structures represent active RGD peptides (cRGDfV, cRGDfE, cRGDfC, cRGDyV, and cRGDfK).

1997年6月30日 · The design, synthesis and preliminary biological evaluation of carbohydrate-based non-peptide mimetics of the potent peptidic antagonist of α v β 3 and α v β 5, pentapeptide cRGD F V (1) is presented. The design was based on the NMR-determined structure of 1.

Development of alphavbeta3-integrin inhibitors has been hampered by a lack of pharmacodynamic endpoints to identify doses that inhibit alphavbeta3 in vivo. To address this need, we developed an...

2000年2月1日 · We have investigated the cellular effects of cRGDfV on a panel of human melanoma cell lines in vitro and also on the A375 melanoma cell line growing as xenografts in nude mice. cRGDfV is a potent inhibitor of ανβ3-mediated cell adhesion, however, we have found no convincing evidence that integrin ligation by cRGDfV induces apoptosis in ...

We have investigated the effect of cyclo- (Arg-Gly-Asp-D-Phe-Val) (cRGDfV) peptide on survival of human malignant glioma cells in vitro and in vivo. Immunofluorescent analyses revealed the presence of alpha (v)beta3 integrin on U-87MG and U-373MG cells, but minimal expression on U …

We tested the effect of postischemic treatment of cyclo-RGDfV (cRGDfV), a selective inhibitor of integrin alphavbeta3, in the middle cerebral artery occlusion (MCAO) model of ischemic stroke in rats. Rats were randomly divided into three groups: sham operation (n = 13), MCAO with no treatment (n = 18), and MCAO with cRGDfV treatment (n = 28).

The selective integrin alphavbeta3 inhibitor cRGDfV improves outcomes in the MCAO model by preserving the blood-brain barrier, which mechanistically may occur in a VEGF- and VEGF-receptor-dependent manner.

cRGDfV blocking peptide inhibits the NC1 (XIX) binding on αvβ3 integrin. ( A ) Effect of cRGDfV blocking peptide on SK-MEL-28 cell adhesion. Cells were preincubated in DMEM containing 0.1,...

2006年6月1日 · We studied selective inhibition of integrin αvβ3 with cyclo [Arg-Gly-Asp-d-Phe-Val] (cRGDfV) in the rat middle cerebral artery occlusion model (MCAO).