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2014-10-09 - Colloque/Présentation - poster - Anglais - 1 page(s)

Circelli Géraldine , Vander Elst Luce , Muller Robert , Laurent Sophie , "Design of contrast agent for neurodegenerative diseases diagnosis" in journée scientifique annuelle de la SRC, "Nanochimie : Réalisations et Perspectives.", Namur, Belgique, 2014

  • Codes CREF : Physico-chimie générale (DI1320), Chimie des colloïdes (DI1329)
  • Unités de recherche UMONS : Chimie générale, organique et biomédicale (M108)
  • Instituts UMONS : Institut des Sciences et Technologies de la Santé (Santé), Institut des Biosciences (Biosciences)
  • Centres UMONS : Centre de Recherche en Microscopie et Imagerie Médicale (CMMI)

Abstract(s) :

(Anglais) DESIGN OF CONTRAST AGENT FOR NEURODEGENERATIVE DISEASES DIAGNOSIS G. Circelli 1, L. Vander Elst 1,2, R. N. Muller 1,2, S. Laurent 1,2 1 NMR and Molecular Imaging Laboratory, University of Mons; 2 Center for Microscopy and Molecular Imaging, Gosselies. In the last decades, molecular imaging technologies began to attract increased interest for the targeting of diseases. In particular, Alzheimer disease diagnosis is nowadays investigated through the design of tailor-made contrast agents able to cross over the blood-brain barrier (BBB). Conventional contrast agents are composed of three parts: contrast agent, spacer and vector. Over the last three decades, gadolinium complex of DOTA macrocycle has exhibited enhanced stability properties as compared to other first generation contrast agents. In addition, the versatility of the complexes confers to DOTA-based contrast agents the ability to be used in a large range of imaging modalities, including magnetic resonance (MR), positron emission tomography (PET), single photon emission computed tomography (SPECT) and fluorescence imaging.1 Variations on the arms of the DOTA macrocycle appears as the way towards the generation of highly stable responsive and selective probes.2 In this context, the specific targeting of diseases has been drastically enhanced by the incorporation of peptides as vectors. In the present study, the design of L-DOPA functionalized Gd-DOTA complex as a bluilding block for further modifications is under consideration. The synthetic strategy involves the following steps : (i) the selective three-arms protection of cyclene by tert-butyl acetate moeities; (ii) the incorporation of a fourth arm exhibiting a primary amine moeity; (iii) amidation reaction on the fourth arm with Boc-L-DOPA; (iv) BOC deprotection; (v) Gd3+ complexation by the modified DOTA macrocycle. For instance, the two first steps were successfully achieved. Both NMR and ESI-MS characterization techniques were used to follow the progress of the reactions. The next steps are under progress. 1. G. J. Stasiuk, N.J. Long, Chem. Commun., 49, 2732 (2013). 2. C.F.G.C. Geraldes, S. Laurent, Contrast Media & Molecular Imaging, 4(1), 1 (2009)