title: Design, structural and biological characterization of a VEGF inhibitor β-hairpin-constrained peptide.
abstract: The design, structural and biological characterization of a novel VEGF inhibitor peptide is described. The peptide was designed on the β5-β6 hairpin region of Placenta Growth Factor. NMR studies showed that the peptide assumes in solution a β-hairpin conformation similarly to the corresponding region of the natural ligand. In vitro experiments on endothelial cells demonstrated that the peptide is able to inhibit VEGF biological activity. This molecule represents a novel molecular entity to modulate VEGF activity and with potential application in therapy and diagnosis of angiogenesis-dependent diseases.
authors.affiliation: Istituto di Biostrutture e Bioimmagini, CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Lucia
authors.initials: L
authors.lastname: De Rosa
authors.affiliation: Istituto di Biostrutture e Bioimmagini, CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Diana
authors.affiliation: Dipartimento di Scienze Farmaceutiche e Biomediche, Università di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
authors.forename: Anna
authors.initials: A
authors.lastname: Basile
authors.affiliation: Istituto di Biostrutture e Bioimmagini, CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Anna
authors.initials: A
authors.lastname: Russomanno
authors.affiliation: Dipartimento di Scienze e Tecnologie Ambientali Biologiche e Farmaceutiche, Seconda Università di Napoli, Via Vivaldi 43, 81100 Caserta, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Isernia
authors.affiliation: Dipartimento di Scienze Farmaceutiche e Biomediche, Università di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
authors.forename: Maria Caterina
authors.initials: MC
authors.lastname: Turco
authors.affiliation: Dipartimento di Scienze e Tecnologie Ambientali Biologiche e Farmaceutiche, Seconda Università di Napoli, Via Vivaldi 43, 81100 Caserta, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Fattorusso
authors.affiliation: Istituto di Biostrutture e Bioimmagini, CNR, Via Mezzocannone 16, 80134 Napoli, Italy. Electronic address: ldandrea@unina.it.
authors.forename: Luca Domenico
authors.initials: LD
authors.lastname: D'Andrea
mesh_terms: D015153:Blotting, Western; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D019906:Nuclear Magnetic Resonance, Biomolecular; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000072483:Placenta Growth Factor; D011257:Pregnancy Proteins / Q000737:chemistry*; D011487:Protein Conformation; D015202:Protein Engineering; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism*; D040281:Vascular Endothelial Growth Factor Receptor-1 / Q000037:antagonists & inhibitors*
chemical_list: C000608036:PGF protein, human; D010456:Peptides, Cyclic; D011257:Pregnancy Proteins; D042461:Vascular Endothelial Growth Factor A; D000072483:Placenta Growth Factor; D040281:Vascular Endothelial Growth Factor Receptor-1
keywords: Angiogenesis; Drug design; NMR spectroscopy; Peptides; VEGF