Integrin Ligands with α/β-Hybrid Peptide Structure: Design, Bioactivity, and Conformational Aspects

Medicinal Research Reviews
Rossella De MarcoLuca Gentilucci

Abstract

Integrins are cell surface receptors for proteins of the extracellular matrix and plasma-borne adhesive proteins. Their involvement in diverse pathologies prompted medicinal chemists to develop small-molecule antagonists, and very often such molecules are peptidomimetics designed on the basis of the short native ligand-integrin recognition motifs. This review deals with peptidomimetic integrin ligands composed of α- and β-amino acids. The roles exerted by the β-amino acid components are discussed in terms of biological activity, bioavailability, and selectivity. Special attention is paid to the synthetic accessibility and efficiency of conformationally constrained heterocyclic scaffolds incorporating α/β-amino acid span.

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Citations

Nov 23, 2016·Future Medicinal Chemistry·Luca GentilucciRossella De Marco
Dec 23, 2016·Chembiochem : a European Journal of Chemical Biology·Michael H SonntagLuc Brunsveld
May 31, 2018·Physical Chemistry Chemical Physics : PCCP·C PaissoniM Ghitti
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Sep 19, 2019·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·Dmitry O BazhenovDmitry I Sokolov
Apr 21, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Arwa MorshedHanmei Xu
Mar 18, 2020·Chembiochem : a European Journal of Chemical Biology·Amila TuralićTamás A Martinek

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