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Molecules 2014, 19(10), 15391-15407;

Design and Synthesis of C-Terminal Modified Cyclic Peptides as VEGFR1 Antagonists

UMR 8638 CNRS, Faculté de Pharmacie de Paris, Université Paris Descartes, Sorbonne Paris Cité, 4 avenue de l'observatoire, Paris 75006, France
UF Pharmacocinétique et pharmacochimie, hôpital Cochin, AP-HP, 27 rue du Faubourg Saint Jacques, Paris 75014, France
Authors to whom correspondence should be addressed.
Received: 7 August 2014 / Revised: 12 September 2014 / Accepted: 17 September 2014 / Published: 26 September 2014
(This article belongs to the Special Issue Design and Study of Kinase Inhibitors)
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Previously designed cyclic peptide antagonist c[YYDEGLEE]-NH2 disrupts the interaction between vascular endothelial growth factor (VEGF) and its receptors (VEGFRs). It represents a promising tool in the fight against cancer and age-related macular degeneration. We described in this paper the optimization of the lead peptide by C-terminal modification. A new strategy for the synthesis of cyclic peptides is developed, improving the cyclisation efficiency. At 100 µM, several new peptides with an aromatic group flexibly linked at C-terminal end showed significantly increased receptor binding affinities in competition ELISA test. The most active peptide carrying a coumarin group may be a useful tool in anti-angiogenic biological studies. View Full-Text
Keywords: VEGF; VEGFR; angiogenesis; cyclic peptides VEGF; VEGFR; angiogenesis; cyclic peptides

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Wang, L.; Gagey-Eilstein, N.; Broussy, S.; Reille-Seroussi, M.; Huguenot, F.; Vidal, M.; Liu, W.-Q. Design and Synthesis of C-Terminal Modified Cyclic Peptides as VEGFR1 Antagonists. Molecules 2014, 19, 15391-15407.

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