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Stable Peptides Instead of Stapled Peptides: Highly Potent αvβ6‐Selective Integrin Ligands |
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| Authors: | Dr Oleg V Maltsev Dr Udaya Kiran Marelli Tobias G Kapp Dr Francesco Saverio Di?Leva Dr Salvatore Di?Maro Dr Markus Nieberler Prof?Dr Ute Reuning Prof?Dr Markus Schwaiger Prof?Dr Ettore Novellino Prof?Dr Luciana Marinelli Prof?Dr Horst Kessler |
| Institution: | 1. Institute for Advanced Study and Center for Integrated Protein Science (CIPSM), Technische Universit?t München, Garching, Germany;2. Dipartimento di Farmacia, Università di Napoli Federico II, Napoli, Italy;3. DiSTABiF, Secondo Università di Napoli, Caserta, Italy;4. Department of Oral and Maxillofacial Surgery, University Hospital rechts der Isar, Technische Universit?t München, München, Germany;5. Klinische Forschergruppe der Frauenklinik, University Hospital rechts der Isar, Technische Universit?t München, München, Germany;6. Department of Nuclear Medicine, University Hospital rechts der Isar, Technische Universit?t München, München, Germany |
| Abstract: | The αvβ6 integrin binds the RGD‐containing peptide of the foot and mouth disease virus with high selectivity. In this study, the long binding helix of this ligand was downsized to an enzymatically stable cyclic peptide endowed with sub‐nanomolar binding affinity toward the αvβ6 receptor and remarkable selectivity against other integrins. Computational studies were performed to disclose the molecular bases underlying the high binding affinity and receptor subtype selectivity of this peptide. Finally, the utility of the ligand for use in biomedical studies was also demonstrated here. |
| Keywords: | cyclic peptides integrin inhibitors molecular imaging subtype selectivity α vβ 6 integrin |