Novel and selective αvβ3 receptor peptide antagonist: Design, synthesis, and biological behavior

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

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
Pages (from-to)3416-3420
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number11
Publication statusPublished - Jun 1 2006

ASJC Scopus subject areas

  • Organic Chemistry

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