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19 results on '"Isabel, Elise"'

5. Difluoroethylamines as an amide isostere in inhibitors of cathepsin K

Author

Isabel, Elise, Mellon, Christophe, Boyd, Michael J., Chauret, Nathalie, Deschênes, Denis, Desmarais, Sylvie, Falgueyret, Jean-Pierre, Gauthier, Jacques Yves, Khougaz, Karine, Lau, Cheuk K., Léger, Serge, Levorse, Dorothy A., Li, Chun Sing, Massé, Frédéric, David Percival, M., Roy, Bruno, Scheigetz, John, Thérien, Michel, Truong, Vouy Linh, Wesolowski, Gregg, Young, Robert N., Zamboni, Robert, and Cameron Black, W.

Published
2011
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8. The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor

Author

Isabel, Elise, Bateman, Kevin P., Chauret, Nathalie, Cromlish, Wanda, Desmarais, Sylvie, Duong, Le T., Falgueyret, Jean-Pierre, Gauthier, Jacques Yves, Lamontagne, Sonia, Lau, Cheuk K., Léger, Serge, LeRiche, Tammy, Lévesque, Jean-François, Li, Chun Sing, Massé, Frédéric, McKay, Daniel J., Mellon, Christophe, Nicoll-Griffith, Deborah A., Oballa, Renata M., Percival, M. David, Riendeau, Denis, Robichaud, Joël, Rodan, Gideon A., Rodan, Sevgi B., Seto, Carmai, Thérien, Michel, Truong, Vouy Linh, Wesolowski, Gregg, Young, Robert N., Zamboni, Robert, and Black, W. Cameron

Published
2010
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10. Electron-ligand interchange reactions between palladium(II) complexes and mercury and single-crystal X-ray characterization of the d10-d10 binuclear (Hg2(dppm)2Cl3)Cl complex

Author

Harvey, Pierre D., Aye, Khin T., Hierso, Karine, Isabel, Elise, Lognot, Isabelle, Mugnier, Yves, and Rochon, F.D.

Subjects
Coordination compounds -- Research, Mercury compounds -- Research, Palladium -- Research, Chemistry
Abstract

Addition of mercury(I) to Pd(II) complexes Pd(dppm)X2 (dppm = ((C6H5)2P)2CH2; X = Cl, Br) leads to reduction, producing Pd(0), and the reduction proceeds through an inner-sphere mechanism. Coordination between the oxidized metal (Hg2+) and the released ligands produces d10 dinuclear complexes. Spectroscopic studies help identify the products and x-ray crystallography enables the determination of the structure of the binuclear (Hg2(dppm)2Cl3)Cl complex.

Published
1994

13. Identification of a Nonbasic, Nitrile-Containing Cathepsin K Inhibitor (MK-1256) that is Efficacious in a Monkey Model of Osteoporosis

Author

Robichaud, Jöel, primary, Black, W. Cameron, additional, Thérien, Michel, additional, Paquet, Julie, additional, Oballa, Renata M., additional, Bayly, Christopher I., additional, McKay, Daniel J., additional, Wang, Qingping, additional, Isabel, Elise, additional, Léger, Serge, additional, Mellon, Christophe, additional, Kimmel, Donald B., additional, Wesolowski, Gregg, additional, Percival, M. David, additional, Massé, Fréderic, additional, Desmarais, Sylvie, additional, Falgueyret, Jean-Pierre, additional, and Crane, Sheldon N., additional

Published
2008
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14. Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors

Author

Mellon, Christophe, primary, Aspiotis, Reneé, additional, Black, Cameron W., additional, Bayly, Christopher I., additional, Grimm, Erich L., additional, Giroux, André, additional, Han, Yongxin, additional, Isabel, Elise, additional, McKay, Daniel J., additional, Nicholson, Donald W., additional, Rasper, Dita M., additional, Roy, Sophie, additional, Tam, John, additional, Thornberry, Nancy A., additional, Vaillancourt, John P., additional, Xanthoudakis, Steven, additional, and Zamboni, Robert, additional

Published
2005
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15. Nicotinyl aspartyl ketones as inhibitors of caspase-3

Author

Isabel, Elise, primary, Black, W.Cameron, additional, Bayly, Christopher I, additional, Grimm, Erich L, additional, Janes, Marc K, additional, McKay, Daniel J, additional, Nicholson, Donald W, additional, Rasper, Dita M, additional, Renaud, Johanne, additional, Roy, Sophie, additional, Tam, John, additional, Thornberry, Nancy A, additional, Vaillancourt, John P, additional, Xanthoudakis, Steven, additional, and Zamboni, Robert, additional

Published
2003
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17. Reversible Cysteine Protease Inhibitors Show Promise for a Chagas Disease Cure

Author

Ndao, Momar, Beaulieu, Christian, Black, W. Cameron, Isabel, Elise, Vasquez-Camargo, Fabio, Nath-Chowdhury, Milli, Massé, Frédéric, Mellon, Christophe, Methot, Nathalie, and Nicoll-Griffith, Deborah A.

Abstract

ABSTRACTThe cysteine protease cruzipain is essential for the viability, infectivity, and virulence of Trypanosoma cruzi, the causative agent of Chagas disease. Thus, inhibitors of cruzipain are considered promising anti-T. cruzichemotherapeutic agents. Reversible cruzipain inhibitors containing a nitrile “warhead” were prepared and demonstrated 50% inhibitory concentrations (IC50s) as potent as 1 nM in baculovirus-generated cruzipain enzyme assays. In epimastigote and intracellular amastigote in vitroassays, the most potent compounds demonstrated antiparasitic behavior in the 5 to 10 μM IC50range; however, trypomastigote production from the amastigote form was ∼90 to 95% inhibited at 2 μM. Two key compounds, Cz007 and Cz008, with IC50s of 1.1 and 1.8 nM, respectively, against the recombinant enzyme were tested in a murine model of acute T. cruziinfection, with oral dosing in chow for 28 days at doses from 3 to 50 mg/kg of body weight. At 3 mg/kg of Cz007 and 3 mg/kg of Cz008, the blood parasitemia areas under the concentration-time curves were 16% and 25% of the untreated group, respectively. At sacrifice, 24 days after immunosuppression with cyclophosphamide, parasite presence in blood, heart, and esophagus was evaluated. Based on negative quantitative PCR results in all three tissues, cure rates in surviving animals were 90% for Cz007 at 3 mg/kg, 78% for Cz008 at 3 mg/kg, and 71% for benznidazole, the control compound, at 50 mg/kg.

Published
2013
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19. Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors

Author

Mellon, Christophe, Aspiotis, Reneé, Black, Cameron W., Bayly, Christopher I., Grimm, Erich L., Giroux, André, Han, Yongxin, Isabel, Elise, McKay, Daniel J., Nicholson, Donald W., Rasper, Dita M., Roy, Sophie, Tam, John, Thornberry, Nancy A., Vaillancourt, John P., Xanthoudakis, Steven, and Zamboni, Robert

Subjects
*DRUG lipophilicity, *DRUG solubility, *PHASE partition, *DISEASES
Abstract

Abstract: Caspase 3 is a cysteinyl protease that mediates apoptotic cell death. Its inhibition may have an important impact in the treatment of several degenerative diseases. The P1 aspartic acid residue is a required element of recognition for this enzyme that was maintained constant along with the adjacent natural valine as the P2 group. The thiobenzylmethylketone warhead on the aspartate was conveniently handled through solid-phase synthesis allowing modification in the P3 region that eventually led to simpler derivatives with increased potency against caspase 3. The key to such an effect is the introduction of hydroxyl group alpha to the P3 carbonyl. [Copyright &y& Elsevier]

Published
2005
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