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Tomassi, Stefano; D’Amore, Vincenzo Maria; Di Leva, Francesco Saverio; Vannini, Andrea; Quilici, Giacomo; Weinmüller, Michael; Reichart, Florian; Amato, Jussara; Romano, Barbara; Izzo, Angelo Antonio; Di Maro, Salvatore; Novellino, Ettore; Musco, Giovanna; Gianni, Tatiana; Kessler, Horst; Marinelli, Luciana
Journal of medicinal chemistry, 05/2021, Volume: 64, Issue: 10Journal Article
Over recent years, αvβ6 and αvβ8 Arg-Gly-Asp (RGD) integrins have risen to prominence as interchangeable co-receptors for the cellular entry of herpes simplex virus-1 (HSV-1). In fact, the employment of subtype-specific integrin-neutralizing antibodies or gene-silencing siRNAs has emerged as a valuable strategy for impairing HSV infectivity. Here, we shift the focus to a more affordable pharmaceutical approach based on small RGD-containing cyclic pentapeptides. Starting from our recently developed αvβ6-preferential peptide RGD-Chg-E-CONH2 (1), a small library of N-methylated derivatives (2–6) was indeed synthesized in the attempt to increase its affinity toward αvβ8. Among the novel compounds, RGD-Chg-(NMe)E-CONH2 (6) turned out to be a potent αvβ6/αvβ8 binder and a promising inhibitor of HSV entry through an integrin-dependent mechanism. Furthermore, the renewed selectivity profile of 6 was fully rationalized by a NMR/molecular modeling combined approach, providing novel valuable hints for the design of RGD integrin ligands with the desired specificity profile.
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