A novel RGD containing dodecapeptidomimetic which exhibits selective binding to the αvβ3 receptor

We report the synthesis, bioactivity and conformational analysis by 1H NMR and computer simulations of a RGD containing dodecapeptidomimetic incorporating the β-turn mimetic BTD. This peptidomimetic exhibits potent binding to the αvβ3 receptor. The binding activity to the αvβ5 receptor is approximately tenfold weaker. Unlike most active RGD containing peptides reported to date this molecule does not show any binding to the fibronectin (αvβ1) or the IIb/IIIa receptors.