Structure‐based design of a bicyclic peptide antagonist of the vascular endothelial growth factor receptors | Zendy

Goncalves Victor | Zendy; Gautier Benoit | Zendy; Garbay Christiane | Zendy; Vidal Michel | Zendy; Inguimbert Nicolas | Zendy

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Structure‐based design of a bicyclic peptide antagonist of the vascular endothelial growth factor receptors

Author(s) -

Goncalves Victor,

Gautier Benoit,

Garbay Christiane,

Vidal Michel,

Inguimbert Nicolas

Publication year - 2008

Publication title -

journal of peptide science

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.475

H-Index - 66

eISSN - 1099-1387

pISSN - 1075-2617

DOI - 10.1002/psc.965

Subject(s) - receptor , peptide , angiogenesis , vascular endothelial growth factor , chemistry , signal transduction , microbiology and biotechnology , bicyclic molecule , in vitro , cancer research , vegf receptors , biochemistry , biology , stereochemistry

Dysregulated angiogenesis is implicated in several pathologies, including cancer and age‐related macular degeneration. A potential antiangiogenic strategy consists in developing VEGF receptor ligands capable of preventing VEGF binding and the subsequent activation of these receptors. Herein, we describe the structure‐based design of a VEGF‐mimicking peptide, VG3F. This 25‐mer peptide was doubly cyclized, on‐resin, by formation of both a disulfide bridge and an intramolecular amide bond to constrain it to adopt a bioactive conformation. Tested on in vitro assays, VG3F was able to prevent VEGF binding to VEGF receptor 1 and inhibit both VEGF‐induced signal transduction and cell migration. Copyright © 2007 European Peptide Society and John Wiley & Sons, Ltd.

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