Publications (87) View all
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Article: An Efficient Synthesis of the Enantiomers of Methadone‐D10
B. M. Gérardy, J. Poupaert, P. Dumont[show abstract] [hide abstract]
ABSTRACT: A reactions sequence is described to prepare the enantiomers of Methadone-d10. The proposed scheme allows to synthesize racemic Methadone-d10 with 14% overall yield, starting from benzene-d6. (-)-Methadone-d10 hydrochloride is assigned the (R)-absolute configuration on the basis of its ORD curve.Bulletin des Sociétés Chimiques Belges. 08/2010; 90(9):977 - 980. -
Article: Stoichiometric complexes tin‐methylenediphosphonate: Composition, biodistribution and elements of structure
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ABSTRACT: Stoichiometric methylenediphosphonate (MDP) complexes of tin were prepared and their composition was determined as Sn (II)-(MDP)2 and Sn (IV)-MDP. Biodistribution studies in mice have shown differences in organ uptake related to the valence of the metal ion and the nature of the injection solvent. N.M.R. spectra and gel filtration experiments indicated a simple, homogeneous structure for the stannous complex and the heterogeneous nature (hexa- and tetra-coordinated) as well as a high apparent molecular weight for stannic species.Journal of Labelled Compounds 07/2006; 27(5):515 - 531. -
Article: In vivo electrically mediated protein and gene transfer in murine melanoma.
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ABSTRACT: We show that efficient permeabilization of murine melanoma can be obtained in vivo by applying electric pulses. More than 80% of the cell population is affected as shown by the penetration of propidium iodide. A protein, beta-galactosidase, can be transferred and expressed into the cells by incorporating either the protein or a plasmid carrying the reporter gene with respective efficiencies of 20% and 4%. This is obtained by a direct injection of either the protein or the plasmid in the tumor, followed by the application of electric pulses with surface electrodes in contact with the skin. This approach is simple and safe to use, reproducible, and specific; moreover, it is potentially applicable to a wide variety of tissues, cell types, and animals.Nature Biotechnology 03/1998; 16(2):168-71. · 23.27 Impact Factor -
Article: Autocrine induction of invasion and metastasis by tumor-associated trypsin inhibitor in human colon cancer cells.
V Gouyer, D Fontaine, P Dumont, O de Wever, H Fontayne-Devaud, E Leteurtre, S Truant, D Delacour, H Drobecq, J-P Kerckaert, Y de Launoit, M Bracke, C Gespach, J-L Desseyn, G Huet[show abstract] [hide abstract]
ABSTRACT: From the conditioned medium of the human colon carcinoma cells, HT-29 5M21 (CM-5M21), expressing a spontaneous invasive phenotype, tumor-associated trypsin inhibitor (TATI) was identified and characterized by proteomics, cDNA microarray approaches and functional analyses. Both CM-5M21 and recombinant TATI, but not the K18Y-TATI mutant at the protease inhibitor site, trigger collagen type I invasion by several human adenoma and carcinoma cells of the colon and breast, through phosphoinositide-3-kinase, protein kinase C and Rho-GTPases/Rho kinase-dependent pathways. Conversely, the proinvasive action of TATI in parental HT29 cells was alleviated by the TATI antibody PSKAN2 and the K18Y-TATI mutant. Stable expression of K18Y-TATI in HT-29 5M21 cells downregulated tumor growth, angiogenesis and the expression of several metastasis-related genes, including CSPG4 (13.8-fold), BMP-7 (9.7-fold), the BMP antagonist CHORDIN (5.2-fold), IGFBP-2 and IGF2 (9.6- and 4.6-fold). Accordingly, ectopic expression of KY-TATI inhibited the development of lung metastases from HT-29 5M21 tumor xenografts in immunodeficient mice. These findings identify TATI as an autocrine transforming factor potentially involved in early and late events of colon cancer progression, including local invasion of the primary tumor and its metastatic spread. Targeting TATI, its molecular partners and effectors may bring novel therapeutic applications for high-grade human solid tumors in the digestive and urogenital systems.Oncogene 08/2008; 27(29):4024-33. · 6.37 Impact Factor -
Article: The methyl-CpG-binding protein MECP2 is required for prostate cancer cell growth.
D Bernard, J Gil, P Dumont, S Rizzo, D Monté, B Quatannens, D Hudson, T Visakorpi, F Fuks, Y de Launoit[show abstract] [hide abstract]
ABSTRACT: The incidence of prostate cancer is increasing in western countries because of population aging. Prostate cancer begins as an androgen-dependent disease, but it can become androgen independent at a later stage or in tumors recurring after an antihormonal treatment. Although many genetic events have been described to be involved in androgen-dependent and/or -independent prostate cancer growth, little is known about the contribution of epigenetic events. Here we have examined the possibility that the methyl-CpG-binding protein MECP2 might play a role in controlling the growth of prostate cancer cells. Inhibition of MECP2 expression by stable short hairpin RNA stopped the growth of both normal and cancer human prostate cells. In addition, ectopic expression of the MECP2 conferred a growth advantage to human prostate cancer cells. More importantly, this expression allowed androgen-dependent cells to grow independently of androgen stimulation and to retain tumorigenic properties in androgen-depleted conditions. Analysis of signaling pathways showed that this effect is independent of androgen receptor signaling. Instead, MECP2 appears to act by maintaining a constant c-myc level during antihormonal treatment. We further show that MECP2-expressing cells possess a functional p53 pathway and are still responsive to chemotherapeutic drugs.Oncogene 04/2006; 25(9):1358-66. · 6.37 Impact Factor