Next Article in Journal
Editorial to the Organophosphorus Chemistry Special Issue of Molecules (2012–2014)
Next Article in Special Issue
Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part II
Previous Article in Journal
Identification of Three Elicitins and a Galactan-Based Complex Polysaccharide from a Concentrated Culture Filtrate of Phytophthora infestans Efficient against Pectobacterium atrosepticum
Previous Article in Special Issue
Several Human Cyclin-Dependent Kinase Inhibitors, Structurally Related to Roscovitine, As New Anti-Malarial Agents
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Molecules
Volume 19
Issue 10
10.3390/molecules191015391
molecules-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

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

by
Lei Wang
1,
Nathalie Gagey-Eilstein
1,
Sylvain Broussy
1,
Marie Reille-Seroussi
1,
Florent Huguenot
1,
Michel Vidal
1,2,* and
Wang-Qing Liu
1,*
1
UMR 8638 CNRS, Faculté de Pharmacie de Paris, Université Paris Descartes, Sorbonne Paris Cité, 4 avenue de l'observatoire, Paris 75006, France
2
UF Pharmacocinétique et pharmacochimie, hôpital Cochin, AP-HP, 27 rue du Faubourg Saint Jacques, Paris 75014, France
*
Authors to whom correspondence should be addressed.
Molecules 2014, 19(10), 15391-15407; https://doi.org/10.3390/molecules191015391
Submission 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)
Browse Figures
Versions Notes

Abstract

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.
Keywords: VEGF; VEGFR; angiogenesis; cyclic peptides VEGF; VEGFR; angiogenesis; cyclic peptides

Share and Cite

MDPI and ACS Style

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. https://doi.org/10.3390/molecules191015391

AMA Style

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(10):15391-15407. https://doi.org/10.3390/molecules191015391

Chicago/Turabian Style

Wang, Lei, Nathalie Gagey-Eilstein, Sylvain Broussy, Marie Reille-Seroussi, Florent Huguenot, Michel Vidal, and Wang-Qing Liu. 2014. "Design and Synthesis of C-Terminal Modified Cyclic Peptides as VEGFR1 Antagonists" Molecules 19, no. 10: 15391-15407. https://doi.org/10.3390/molecules191015391

APA Style

Wang, L., Gagey-Eilstein, N., Broussy, S., Reille-Seroussi, M., Huguenot, F., Vidal, M., & Liu, W.-Q. (2014). Design and Synthesis of C-Terminal Modified Cyclic Peptides as VEGFR1 Antagonists. Molecules, 19(10), 15391-15407. https://doi.org/10.3390/molecules191015391

Article Metrics

Back to TopTop