Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior

J Med Chem. 2006 Jun 1;49(11):3416-20. doi: 10.1021/jm060233m.

Annarita Del Gatto ¹, Laura Zaccaro, Paolo Grieco, Ettore Novellino, Antonella Zannetti, Silvana Del Vecchio, Francesca Iommelli, Marco Salvatore, Carlo Pedone, Michele Saviano

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Affiliation

1 Institute of Biostructures and Bioimaging, CNR, Department of Biological Sciences, University of Naples Federico II, and C. I. R. Pe. B., via Mezzocannone 16, 80134 Naples, Italy.

PMID: 16722662 DOI: 10.1021/jm060233m

Abstract

Among RGD-dependent integrins, the alpha(v)beta3 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 alpha(v)beta3 receptor, designed on the basis of the crystal structure of Integrin alpha(v)beta3 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 alpha(v)beta3 receptor.

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