Zobrazeno 1 - 10
of 75
pro vyhledávání: '"Jean-Pierre Falgueyret"'
Publikováno v:
PLoS ONE, Vol 10, Iss 4, p e0124459 (2015)
Morphinan alkaloids are the most powerful narcotic analgesics currently used to treat moderate to severe and chronic pain. The feasibility of morphinan synthesis in recombinant Saccharomyces cerevisiae starting from the precursor (R,S)-norlaudanosoli
Externí odkaz:
https://doaj.org/article/e709d90b36094462b4cefd377e7a806f
Autor:
Monica Bubenik, Pavel Mader, Philippe Mochirian, Fréderic Vallée, Jillian Clark, Jean-François Truchon, Alexander L. Perryman, Victor Pau, Igor Kurinov, Karl E. Zahn, Marie-Eve Leclaire, Robert Papp, Marie-Claude Mathieu, Martine Hamel, Nicole M. Duffy, Claude Godbout, Matias Casas-Selves, Jean-Pierre Falgueyret, Prasamit S. Baruah, Olivier Nicolas, Rino Stocco, Hugo Poirier, Giovanni Martino, Alexanne Bonneau Fortin, Anne Roulston, Amandine Chefson, Stéphane Dorich, Miguel St-Onge, Purvish Patel, Charles Pellerin, Stéphane Ciblat, Thomas Pinter, Francis Barabé, Majida El Bakkouri, Paranjay Parikh, Christian Gervais, Agnel Sfeir, Yael Mamane, Stephen J. Morris, W. Cameron Black, Frank Sicheri, Michel Gallant
Publikováno v:
Journal of Medicinal Chemistry. 65:13198-13215
Autor:
Monica, Bubenik, Pavel, Mader, Philippe, Mochirian, Fréderic, Vallée, Jillian, Clark, Jean-François, Truchon, Alexander L, Perryman, Victor, Pau, Igor, Kurinov, Karl E, Zahn, Marie-Eve, Leclaire, Robert, Papp, Marie-Claude, Mathieu, Martine, Hamel, Nicole M, Duffy, Claude, Godbout, Matias, Casas-Selves, Jean-Pierre, Falgueyret, Prasamit S, Baruah, Olivier, Nicolas, Rino, Stocco, Hugo, Poirier, Giovanni, Martino, Alexanne Bonneau, Fortin, Anne, Roulston, Amandine, Chefson, Stéphane, Dorich, Miguel, St-Onge, Purvish, Patel, Charles, Pellerin, Stéphane, Ciblat, Thomas, Pinter, Francis, Barabé, Majida, El Bakkouri, Paranjay, Parikh, Christian, Gervais, Agnel, Sfeir, Yael, Mamane, Stephen J, Morris, W Cameron, Black, Frank, Sicheri, Michel, Gallant
Publikováno v:
Journal of medicinal chemistry. 65(19)
DNA polymerase theta (Polθ) is an attractive synthetic lethal target for drug discovery, predicted to be efficacious against breast and ovarian cancers harboring BRCA-mutant alleles. Here, we describe our hit-to-lead efforts in search of a selective
Autor:
Jay A. Grobler, Meizhen Feng, Yuan Li, Yves Ducharme, Jean-Pierre Falgueyret, Bernard Cote, Youwei Yan, Louis-Charles Campeau, Ernest Asante-Appiah, Ming-Tain Lai, Jason Burch, Marc V. Witmer, Daria J. Hazuda, Michael D. Miller, Nancy A. Sachs, Elizabeth Cauchon, Paul Tawa, Daniel J. DiStefano, Meiqing Lu
Publikováno v:
Antimicrobial Agents and Chemotherapy. 58:1652-1663
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for treating human immunodeficiency type 1 virus (HIV-1)-infected patients. MK-1439 is a novel NNRTI with a 50% inhibitory concentration (IC 50 ) of 12, 9.7, and 9.7 nM
Autor:
Sébastien Gagné, Amandine Chefson, Sylvie Toulmond, Patrick Lacombe, Mélissa Arbour, Austin Chen, Dan McKay, Elizabeth Cauchon, Erich L. Grimm, Yeeman K. Ramtohul, M. David Percival, Jean-François Lévesque, Yves Ducharme, Dwight Macdonald, Yongxin Han, René St-Jacques, Robert Houle, Bruce Mackay, Jean-Pierre Falgueyret, Pierre-André Fournier
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2670-2674
The design and optimization of a novel isoxazole S(1) linker for renin inhibitor is described herein. This effort culminated in the identification of compound 18, an orally bioavailable, sub-nanomolar renin inhibitor even in the presence of human pla
Autor:
Stephen M. Soisson, Tom Y.-H. Wu, Michel Gallant, Austin Chen, Dwight Macdonald, Daniel Dube, Robert Houle, Jean-Pierre Falgueyret, Renee Aspiotis, Dan McKay, Jean-François Lévesque, Patrick Roy, Helene Juteau, Sébastien Gagné, M. David Percival, Erich L. Grimm, Sebastien Laliberte, Patrick Lacombe, Elizabeth Cauchon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2430-2436
The incorporation of a carboxylic acid within in a series of 3-amido-4-aryl substituted piperidines (represented by general structure 32) led to the discovery of potent, zwitterionic, renin inhibitors with improved off-target profiles (CYP3A4 time-de
Autor:
Yeeman K. Ramtohul, Sathesh Bhat, Lei Zhang, Zheng Huang, Kathryn Skorey, Paul Tawa, Jean-Pierre Falgueyret, David A. Powell, Renata Oballa, Sébastien Guiral, Marie-Eve Lebrun
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6366-6369
A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. The compounds possess suitable cellular activity and pharmacokinetic properties which render them capable
Autor:
W. Cameron Black, Jean-François Lévesque, Denis Riendeau, Jean-Pierre Falgueyret, Kevin P. Bateman, M. David Percival, Elise Isabel, Tammy LeRiche, Vouy Linh Truong, Jacques Yves Gauthier, Michel Therien, Robert Zamboni, Sevgi B. Rodan, Sylvie Desmarais, Christophe Mellon, Deborah A. Nicoll-Griffith, Renata Oballa, Gregg Wesolowski, Sonia Lamontagne, Carmai Seto, Nathalie Chauret, Chun Sing Li, Robert N. Young, Frédéric Massé, Wanda Cromlish, Daniel J. McKay, Le T. Duong, Cheuk K. Lau, Serge Leger, Joel Robichaud, Gideon A. Rodan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:887-892
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo st
Autor:
Joel Robichaud, Chidambaram Ramachandran, Jean-Pierre Falgueyret, Robert Zamboni, Pierre-Olivier Hétu, Denis Riendeau, Marc Ouellet
Publikováno v:
Archives of Biochemistry and Biophysics. 477:155-162
We have characterized the structures of cyclooxygenase-2 (COX-2) and microsomal prostaglandin E2 synthase-1 (mPGES-1) in intact cells using bifunctional and photo-activatable crosslinking agents. A dimeric complex was detected for COX-2 by both cross
Autor:
Serge Leger, Denis Deschenes, Chun Sing Li, Donald B. Kimmel, M. David Percival, Michel Therien, Mary E. McGrath, Robert Zamboni, Daniel J. McKay, Sevgi B. Rodan, Gregg Wesolowski, Denis Riendeau, W. Cameron Black, Jean-Pierre Falgueyret, Sylvie Desmarais, Frédéric Massé, Jacques Yves Gauthier, Vouy-Linh Truong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1985-1989
Based on our previous study with trifluoroethylamine as a P2–P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound s