From medicinal chemistry to functionalized biomaterials: development of graftable RGD-peptitomimetics for cell adhesion and cell addressing

Marchand-Brynaert, Jacqueline

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  • Marchand-Brynaert, JacquelineUCLouvain
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Abstract
Arg-Gly-Asp (RGD) peptidomimetics constructed on the tyrosine scaffold were equipped with an oligoethylene glycol (OEG) spacer-arm for surface grafting. Their in vitro activities as alphaVbeta3 integrin antagonists were in the range of 0.3-0.7 nM. Poly (ethylene terephthalate) (PET) membranes derivatized with peptidomimetics (50-120 pmol/cm2) allowed the adhesion and proliferation of endothelial cells (HSV) in serum-free medium. Iron oxide particles for MR Imaging grafted with peptidomimetics (2-3 molecules/particle of 20 nm diameter) were selectively targeted to activated tumour cells (Jurkat).
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