Affiliation:
1. Université Catholique de Louvain
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 V3 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).
Publisher
Trans Tech Publications, Ltd.
Subject
Mechanical Engineering,Mechanics of Materials,Condensed Matter Physics,General Materials Science
Reference6 articles.
1. We considered magnetite crystals (forming USPIO) with a volume of 0. 592 nm3 per unit cell. Surfaces of USPIO and unit cell are respectively 1256 nm2 and 0. 71 nm2, thus giving a number of 1769 unit cell faces displayed on one particle. Assuming the presence of 2 Fe atoms per unit cell face, there are 3538 Fe atoms on the surface of one particle. With an organic covering of 1. 6 %, we determine the number of 56 phophonate molecules per particle. The % of derivatization was calculated from the experimental (XPS) F/C atomic ratio as described in note.
2. with the formula: F/C = 3y / (3x + 44 y) for the grafting of Pept-EG6 (C3 for organic covering and C41N5F3 for Pept-EG6). We found: 3 x 4. 35 / [(3 x 95. 65) + (44 x 4. 35)] = 0. 027 (F/C experimental= 0. 028), giving 4. 35 % of derivatization (y) and 0. 0435 x 56 = 2. 43 molecules / particle.
3. B. Manger, K. J. Hardy, A. Weiss, J. D. Stodo: J. Clinical Invest. Vol. 77 (1986) p.1501.
4. J. Marchand-Brynaert: Cardiovascular Pathology Vol. 17 (2008) p.276.
5. B. Driesschaert, N. Charlier, B. Gallez, J. Marchand-Brynaert: Bioorg. Med. Chem. Lett. Vol. 18 (2008) p.4291.