In the present communication we report a cyclic isoDGR peptidomimetic as lownanomolar αvβ3 integrin ligand. In particular, the new cyclo[(3S,6R)DKP-isoDGR] ligand is ten times more potent in binding integrin αvβ3 than c[GisoDGRphg], developed by Kessler and co-workers, and only two-three times less potent than the powerful RGD ligands c[(3S,6R)DKP-RGD] and c[RGDfV]. Spectroscopic and computational studies show that the isoDGR sequence of cyclo[(3S,6R)DKP-isoDGR] can fit into the RGD-binding pocket of αvβ3 integrin, establishing the same electrostatic clamp as well as additional key interactions.

Cyclic isoDGR Peptidomimetics as Low-Nanomolar alphaVbeta3 Integrin Ligands

PIARULLI, UMBERTO;
2013

Abstract

In the present communication we report a cyclic isoDGR peptidomimetic as lownanomolar αvβ3 integrin ligand. In particular, the new cyclo[(3S,6R)DKP-isoDGR] ligand is ten times more potent in binding integrin αvβ3 than c[GisoDGRphg], developed by Kessler and co-workers, and only two-three times less potent than the powerful RGD ligands c[(3S,6R)DKP-RGD] and c[RGDfV]. Spectroscopic and computational studies show that the isoDGR sequence of cyclo[(3S,6R)DKP-isoDGR] can fit into the RGD-binding pocket of αvβ3 integrin, establishing the same electrostatic clamp as well as additional key interactions.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11383/1884124
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