1197191-85-7Relevant academic research and scientific papers
Ultrasmall particle of iron oxide-RGD peptidomimetic conjugate: synthesis and characterisation
Rerat, Vincent,Laurent, Sophie,Burtéa, Carmen,Driesschaert, Beno?t,Pourcelle, Vincent,Vander Elst, Luce,Muller, Robert N.,Marchand-Brynaert, Jacqueline
, p. 1861 - 1865 (2010)
Ultrasmall particles of iron oxide (USPIOs) coated with 3,3′-bis(phosphonate)propionic acid were covalently coupled to a home-made Arg-Gly-Asp (RGD) peptidomimetic molecule via a short oligoethyleneglycol (OEG) spacer. The conjugation rate was measured by X-ray photoelectron spectroscopy (XPS). The particle size and magnetic characteristics were kept. Our novel conjugate targeted efficiently Jurkat cells (increase of 229% vs the control).
αvβ3 integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers
Rerat, Vincent,Dive, Georges,Cordi, Alex A.,Tucker, Gordon C.,Bareille, Reine,Amédée, Jo?lle,Bordenave, Laurence,Marchand-Brynaert, Jacqueline
experimental part, p. 7029 - 7043 (2010/07/05)
RGD peptides are used in biomaterials science for surface modifications with a view to elicit selective cellular responses. Our objective is to replace peptides by small peptidomimetics acting similarly. We designed novel molecules targeting αvβ3 integrin and featuring spacer-arms (for surface grafting), which do not disturb the biological activity, from (L) N-(3-(trifluoromethyl)benzenesulfonyl) tyrosine used as scaffold. Various Arg-mimics were fixed on the phenol function, and the ortho position was used for the coupling of OEG spacers. All peptidomimetics were active in the nM range in a binding test toward human αvβ 3 integrin (IC50 = 0.1 to 1.7 nM) and selective versus platelet integrin αIIbβ3. Selected compounds revealed excellent ability to inhibit bone cells adhesion on vitronectin. Modeling and docking studies were performed for comparing the most active RGD peptidomimetic to cilengitide, i.e., cyclo-[RGDfN(Me)V]-. Lastly, the adhesion of endothelial cells on a cultivation support grafted with RGD peptidomimetics was significantly improved. 2009 American Chemical Society.
