Biochemical and Structural Analysis of the Binding Determinants of a Vascular Endothelial Growth Factor Receptor Peptidic Antagonist (Articolo in rivista)

Type
Label
  • Biochemical and Structural Analysis of the Binding Determinants of a Vascular Endothelial Growth Factor Receptor Peptidic Antagonist (Articolo in rivista) (literal)
Anno
  • 2010-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm1002167 (literal)
Alternative label
  • Gautier B., Goncalves V, Diana D, Di Stasi R, Teillet F, Lenoir C, Huguenot F, Garbay C, Fattorusso R, D'Andrea L, Vidal M, Inguimbert N (2010)
    Biochemical and Structural Analysis of the Binding Determinants of a Vascular Endothelial Growth Factor Receptor Peptidic Antagonist
    in Journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Gautier B., Goncalves V, Diana D, Di Stasi R, Teillet F, Lenoir C, Huguenot F, Garbay C, Fattorusso R, D'Andrea L, Vidal M, Inguimbert N (literal)
Pagina inizio
  • 4428 (literal)
Pagina fine
  • 4440 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 53 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Gautier B., Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France Goncalves V, Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France Diana D, Univ Naples 2, Dipartimento Sci Ambientali, I-81100 Caserta, Italy Di Stasi R, CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy Teillet F, Univ Paris 05, UFR Biomed, Lab Pharmacol Toxicol & Signalisat Cellulaire, INSERM,UMR S 747, F-75006 Paris, France Lenoir C, Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France Huguenot F, Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France Garbay C, Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France Fattorusso R, Univ Naples 2, Dipartimento Sci Ambientali, I-81100 Caserta, Italy D'Andrea L, CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy Vidal M, Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France Inguimbert N, Univ Paris 05, UFR Biomed, INSERM, Lab Pharmacochim Mol & Cellulaire,U648, F-75006 Paris, France (literal)
Titolo
  • Biochemical and Structural Analysis of the Binding Determinants of a Vascular Endothelial Growth Factor Receptor Peptidic Antagonist (literal)
Abstract
  • Cyclic peptide antagonist c[YYDEGLEE1-NH(2), which disrupts the interaction between vascular endothelial growth factor (VEGF) and its receptors (VEGERs), represents a promising tool in the fight against cancer and age-related macular degeneration. Furthermore, coupled to a cyclen derivative, this ligand could be used as a medicinal imaging agent. Nevertheless, before generating such molecular probes, son-le preliminary studies need to be undertaken in order to define the more suitable positions for introduction of the cyclen macrocycle. Through an Ala-scan study on this peptide, we identified its binding motif, and an NMR study highlights its binding sites on the VEGFR-1D2 Ig-like domain. Guided by the structural relationship results deduced from the effect of the peptides on endothelial cells, new peptides were synthesized and grafted on beads. Used in a pull-down assay, these new peptides trap the VEGFRs, thus confirming that the identified amino acid positions are suitable for further derivatization. (literal)
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