Skip to Main content Skip to Navigation
Journal articles

Sugar-based peptidomimetics as potential inhibitors of the vascular endothelium growth factor binding to neuropilin-1

Abstract : Neuropilin-1 (NRP-1) is a co-receptor of VEGFR165 and molecules interfering with VEGF165 binding to NRP-1 seem to be promising candidates as new angiogenesis modulators. Based on the minimal four amino acid sequence of peptidic ligands known to bind NRP-1, we describe here the design, synthesis and biological evaluation of series of original sugar-based peptidomimetics using a C-glycosyl compound, derived from D-gulonolactone, as a scaffold, which was functionalized with side chains of the amino-acids arginine, and tryptophane or threonine. At 100 μM, all compounds exhibited a weak affinity for NRP-1, the most efficient being the bis-guanidinylated compound 32 (IC50 = 92 μM) which could be considered as a new NRP-1 non-peptidic ligand. © 2010 Elsevier Science. All rights reserved
Document type :
Journal articles
Complete list of metadata

https://hal.archives-ouvertes.fr/hal-00476266
Contributor : Didier Wolf Connect in order to contact the contributor
Submitted on : Sunday, April 25, 2010 - 8:56:29 PM
Last modification on : Friday, February 26, 2021 - 3:24:02 PM

Identifiers

Collections

Citation

Alexandre Novoa, Nadia Pellegrini-Moïse, Denise Bechet, Muriel Barberi-Heyob, Yves Chapleur. Sugar-based peptidomimetics as potential inhibitors of the vascular endothelium growth factor binding to neuropilin-1. Bioorganic and Medicinal Chemistry, Elsevier, 2010, 18 (8), pp.3285-3298. ⟨10.1016/j.bmc.2010.03.012⟩. ⟨hal-00476266⟩

Share

Metrics

Record views

174