title: Integrin Ligands with α/β-Hybrid Peptide Structure: Design, Bioactivity, and Conformational Aspects.
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.
authors.affiliation: Department of Chemistry "G. Ciamician,", University of Bologna, via Selmi 2, 40126, Bologna, Italy.
authors.forename: Rossella
authors.initials: R
authors.lastname: De Marco
authors.affiliation: Department of Chemistry "G. Ciamician,", University of Bologna, via Selmi 2, 40126, Bologna, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Tolomelli
authors.affiliation: Department of Chemistry, Centro de Investigacion y de Estudios Avanzados del IPN, Avenida IPN 2508, esquina Ticoman, Mexico, D.F., 07360, Mexico.
authors.forename: Eusebio
authors.initials: E
authors.lastname: Juaristi
authors.affiliation: Department of Chemistry "G. Ciamician,", University of Bologna, via Selmi 2, 40126, Bologna, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Gentilucci
mesh_terms: D016023:Integrins / Q000737:chemistry*; D008024:Ligands; D010455:Peptides / Q000737:chemistry*; D011487:Protein Conformation
chemical_list: D016023:Integrins; D008024:Ligands; D010455:Peptides
keywords: cancer; heterocycle; integrin; peptidomimetic; β-amino acid