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dc.contributor.author
Zanella, Simone
dc.contributor.author
Bocchinfuso, Gianfranco
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De Zotti, Marta
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Arosio, Daniela
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Marino, Franca
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Raniolo, Stefano
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Pignataro, Luca
dc.contributor.author
Sacco, Giovanni
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Palleschi, Antonio
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Siano, Alvaro Sebastían
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Piarulli, Umberto
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Belvisi, Laura
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Formaggio, Fernando
dc.contributor.author
Gennari, Cesare
dc.contributor.author
Stella, Lorenzo
dc.date.available
2020-05-11T11:57:42Z
dc.date.issued
2019-03
dc.identifier.citation
Zanella, Simone; Bocchinfuso, Gianfranco; De Zotti, Marta; Arosio, Daniela; Marino, Franca; et al.; Rational design of antiangiogenic helical oligopeptides targeting the vascular endothelial growth factor receptors; Frontiers Media S.A.; Frontiers in Chemistry; 7; 3-2019; 1-13
dc.identifier.issn
2296-2646
dc.identifier.uri
http://hdl.handle.net/11336/104696
dc.description.abstract
Tumor angiogenesis, essential for cancer development, is regulated mainly by vascular endothelial growth factors (VEGFs) and their receptors (VEGFRs), which are overexpressed in cancer cells. Therefore, the VEGF/VEGFR interaction represents a promising pharmaceutical target to fight cancer progression. The VEGF surface interacting with VEGFRs comprises a short α-helix. In this work, helical oligopeptides mimicking the VEGF-C helix were rationally designed based on structural analyses and computational studies. The helical conformation was stabilized by optimizing intramolecular interactions and by introducing helix-inducing C α,α -disubstituted amino acids. The conformational features of the synthetic peptides were characterized by circular dichroism and nuclear magnetic resonance, and their receptor binding properties and antiangiogenic activity were determined. The best hits exhibited antiangiogenic activity in vitro at nanomolar concentrations and were resistant to proteolytic degradation.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Frontiers Media S.A.
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
ANGIOGENESIS
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CAlpha
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HELICAL FOLDED PEPTIDES
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PROTEIN-PROTEIN INTERACTIONS
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VEGF-C
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Química Orgánica
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Rational design of antiangiogenic helical oligopeptides targeting the vascular endothelial growth factor receptors
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-05-04T20:57:33Z
dc.journal.volume
7
dc.journal.pagination
1-13
dc.journal.pais
Estados Unidos
dc.description.fil
Fil: Zanella, Simone. Università degli Studi di Milano; Italia
dc.description.fil
Fil: Bocchinfuso, Gianfranco. Universita Tor Vergata; Italia
dc.description.fil
Fil: De Zotti, Marta. Università di Padova; Italia
dc.description.fil
Fil: Arosio, Daniela. Consiglio Nazionale delle Ricerche; Italia
dc.description.fil
Fil: Marino, Franca. Università Degli Studi Dell'insubria;
dc.description.fil
Fil: Raniolo, Stefano. Universita Tor Vergata; Italia
dc.description.fil
Fil: Pignataro, Luca. Università degli Studi di Milano; Italia
dc.description.fil
Fil: Sacco, Giovanni. Università degli Studi di Milano; Italia
dc.description.fil
Fil: Palleschi, Antonio. Universita Tor Vergata; Italia
dc.description.fil
Fil: Siano, Alvaro Sebastían. Universidad Nacional del Litoral; Argentina
dc.description.fil
Fil: Piarulli, Umberto. Università Degli Studi Dell'insubria;
dc.description.fil
Fil: Belvisi, Laura. Università degli Studi di Milano; Italia. Consiglio Nazionale delle Ricerche; Italia
dc.description.fil
Fil: Formaggio, Fernando. Università di Padova; Italia
dc.description.fil
Fil: Gennari, Cesare. Università degli Studi di Milano; Italia. Consiglio Nazionale delle Ricerche; Italia
dc.description.fil
Fil: Stella, Lorenzo. Universita Tor Vergata; Italia
dc.journal.title
Frontiers in Chemistry
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.3389/fchem.2019.00170
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