Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 24, Issue 21, Pages 5315-5325Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.08.052
Keywords
Neuropilin-1; VEGF; Carbohydrate scaffolds; Peptidomimetics; Molecular modeling
Funding
- Region Lorraine
- Institut Jean Barriol
- Ministere de l'Enseignement Superieur et de la Recherche
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Neuropilin-1 (NRP-1), a transmembrane glycoprotein acting as a co-receptor of VEGF-A, is expressed by cancer and angiogenic endothelial cells and is involved in the angiogenesis process. Taking advantage of functionalities and stereodiversities of sugar derivatives, the design and the synthesis of carbohydrate based peptidomimetics are here described. One of these compounds (56) demonstrated inhibition of VEGF-A(165) binding to NRP-1 (IC50 = 39 mu M) and specificity for NRP-1 over VEGF-R2. Biological evaluations were performed on human umbilical vein endothelial cells (HUVECs) through activation of downstream proteins (AKT and ERK phosphorylation), viability/proliferation assays and in vitro measurements of antiangiogenic abilities. (C) 2016 Published by Elsevier Ltd.
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