Karine Estieu-Gionnet

Publications (4)14.66 Total impact

• Article: Design, synthesis, and evaluation of original carriers for targeting vascular endothelial growth factor receptor interactions.

  Mario Gonçalves, Karine Estieu-Gionnet, Thomas Berthelot, Georges Laïn, Mireille Bayle, Xavier Canron, Natacha Betz, Andreas Bikfalvi, Gérard Déléris
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  ABSTRACT: Angiogenesis is a key event in tumor growth and metastasis, chronic inflammatory disease, and cardiovascular disease. It is controlled by positive and negative regulators, which include vascular endothelial growth factor (VEGF) as the most active of these. VEGF/VEGF receptors are important targets not only for therapy but also for imaging. Based on the structural study of VEGF, we developed a novel cyclopeptide (cyclo-VEGI) that exhibits powerful antitumor properties. We herein report the design of novel molecules derived from cyclo-VEGI as potential targeting agents in cancer and other angiogenesis-related diseases. We performed selective chemical modification of the most active VEGF-derived cyclopeptide (cyclo-VEGI). Original hydrophilic linkers were synthesized and coupled to cyclo-VEGI. These reactions provide nanocarriers for delivery. The inhibitory effect of the different compounds on VEGF binding was evaluated in competition assays with 125I-VEGF. A fluorescent cyclo-VEGI peptide was synthezised to assess direct binding and internalization of cyclo-VEGI. Chemical modifications of cyclo-VEGI do not diminish the biological activity of cyclo-VEGI as measured in competition assays; in fact, it is even increased. Moreover there is a strong cellular accumulation of the fluorescent-labeled cyclo-VEGI. Conjugates synthesized in this study may be useful leads to design delivery systems for targeting approaches in cancer and other angiogenesis-related diseases. The modified cyclo-VEGIs may have a wide range of applications and represent a useful tool to develop delivery/carrier systems for therapeutic targeting or imaging.
  Pharmaceutical Research 09/2005; 22(8):1411-21. · 4.09 Impact Factor
• Article: Synthesis and evaluation of organosilicon inhibitors of active purine transport in human osteoblasts.

  Sol Ciro, Cyril Rubio, Karine Estieu-Gionnet, Laurent Latxague, Gérard Déléris, Reine Bareille, Joëlle Amédée, Charles Baquey
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  ABSTRACT: In the search for new compounds that might, once incorporated into biomaterials, stimulate the natural processes of bone regeneration, a new series of silicon-containing alkyl nucleobase analogues has been synthesized. An active hypoxanthine transport process in human osteoblasts was demonstrated, with an apparent Michaelis constant of 2.3 microM and a maximum possible rate of 0.47 pmol s(-1) x 10(6) cell. The synthesized analogues were tested for toxicity in human osteoblasts. Nontoxic analogues were tested in competition transport studies with [(14)C]hypoxanthine. Two of them were found to inhibit the active transport of hypoxanthine in human osteoblasts, with IC(50) values of 6.5 and 11.6 microM.
  ChemBioChem 05/2002; 3(4):341-7. · 3.94 Impact Factor
• Article: Synthesis and Evaluation of Organosilicon Inhibitors of Active Purine Transport in Human Osteoblasts

  Sol Ciro, Cyril Rubio, Karine Estieu‐Gionnet, Laurent Latxague, Gérard Déléris, Reine Bareille, Joëlle Amédée, Charles Baquey
  ChemBioChem 03/2002; 3(4):341 - 347. · 3.94 Impact Factor
• Article: Synthesis of N-Fmoc-4-[(diethylphosphono)-2′,2′-difluoro-1′-hydroxyethyl]phenylalanine, a novel phosphotyrosyl mimic for the preparation of signal transduction inhibitory peptides

  Svitlana Chetyrkina, Karine Estieu-Gionnet, Georges Laı̈n, Mireille Bayle, Gérard Déléris
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  ABSTRACT: The synthesis of a novel non-hydrolyzable phosphotyrosyl mimic N-Fmoc-4-[(diethylphosphono)-2′,2′-difluoro-1′-hydroxyethyl]-DL-phenylalanine is reported.
  Tetrahedron Letters 41(12):1923-1926. · 2.68 Impact Factor