Among RGD-dependent integrins, the αvβ3 receptor has recently received increasing attention as a therapeutic target because of its critical role in tumor-induced angiogenesis and metastasis formation. Here, we describe a new peptide antagonist of α vβ3 receptor, designed on the basis of the crystal structure of integrin αvβ3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. Cell adhesion assays have demonstrated that the peptide is a potent and selective antagonist of the αvβ3 receptor. © 2006 American Chemical Society.
Novel and selective αvβ3 receptor peptide antagonist: Design, synthesis, and biological behavior
Del Gatto A.;Zaccaro L.;Zannetti A.;Del Vecchio S.;Iommelli F.;Salvatore M.;Pedone C.;Saviano M.
2006
Abstract
Among RGD-dependent integrins, the αvβ3 receptor has recently received increasing attention as a therapeutic target because of its critical role in tumor-induced angiogenesis and metastasis formation. Here, we describe a new peptide antagonist of α vβ3 receptor, designed on the basis of the crystal structure of integrin αvβ3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. Cell adhesion assays have demonstrated that the peptide is a potent and selective antagonist of the αvβ3 receptor. © 2006 American Chemical Society.File in questo prodotto:
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