Zobrazeno 1 - 10
of 53
pro vyhledávání: '"Jocelyne Guay"'
Autor:
E. Scott Priestley, Jacques Banville, Daniel Deon, Laurence Dubé, Marc Gagnon, Julia Guy, Philippe Lapointe, Jean-François Lavallée, Alain Martel, Serge Plamondon, Roger Rémillard, Edward Ruediger, François Tremblay, Shana L. Posy, Victor R. Guarino, Jeremy M. Richter, Jianqing Li, Anuradha Gupta, Muthalagu Vetrichelvan, T. J. Balapragalathan, Arvind Mathur, Ji Hua, Mario Callejo, Jocelyne Guay, Chi Shing Sum, Mary Ellen Cvijic, Carol Watson, Pancras Wong, Jing Yang, Michel Bouvier, David A. Gordon, Ruth R. Wexler, Anne Marinier
Publikováno v:
Journal of Medicinal Chemistry. 65:8843-8854
Protease-activated receptor 4 (PAR4) is a G-protein coupled receptor that is expressed on human platelets and activated by the coagulation enzyme thrombin. PAR4 plays a key role in blood coagulation, and its importance in pathological thrombosis has
Autor:
William A. Schumacher, Jocelyne Guay, J.Eileen Bird, David A. Gordon, Mary Giancarli, Ruth R. Wexler, Pancras C. Wong, Mario Callejo, Michael M. Miller, Carol A. Watson, Julia Guy, Anne Marinier, Brad D. Maxwell, Ji Hua, E. Scott Priestley, Dietmar A. Seiffert, David G. Harden, Michel Bouvier, R. Michael Lawrence, Jacques Banville, Jing Yang, Nick J. Allegretto, Jeffrey S. Bostwick
Publikováno v:
Science translational medicine. 9(371)
Antiplatelet agents are proven efficacious treatments for cardiovascular and cerebrovascular diseases. However, the existing drugs are compromised by unwanted and sometimes life-threatening bleeding that limits drug usage or dosage. There is a substa
Autor:
Zheng Huang, Jocelyne Guay, Lei Zhang, David A. Powell, Joel Robichaud, Elise Isabel, Jean-Philippe Leclerc, Cameron Black, Serge Leger, Renata Oballa, Sébastien Guiral, Sheldon Crane, Chun Sing Li, Yeeman K. Ramtohul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5692-5696
Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eye
Autor:
Sheldon Crane, Lei Zhang, Jocelyne Guay, Sébastien Guiral, Chun Sing Li, Cameron Black, Lijing Xu, Yeeman K. Ramtohul, Renata Oballa, Zheng Huang, Chi-Chung Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1593-1597
Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Compound 3j, a potent SCD inhibitor (human HepG2 IC50 = 1 nM) was identified from the optimization of a lead th
Autor:
Jocelyne Guay, Lei Zhang, Hao Wang, Yeeman K. Ramtohul, Sébastien Gagné, Zheng Huang, Angela Styhler
Publikováno v:
SLAS Discovery. 15:169-176
A multiplexed cell assay has been optimized to measure the activities of fatty acyl-CoA elongase, delta-5 desaturase (Delta5D), delta-6 desaturase (Delta6D), and delta-9 desaturase (Delta9D) together using (14)C-labeled tracers in HepG2 cells, which
Autor:
Richard Frenette, Jocelyne Guay, Christine Brideau, Evelyn Martins, Marc Gagnon, Denis Riendeau, Joseph A. Mancini, Andre Giroux, Bernard Cote, Louise Boulet, David Claveau, Diane Ethier, Frédéric Massé, Richard Friesen, Daigen Xu, Anh Chau, Nathalie Méthot, Joel Rubin, Yves Ducharme, Hongping Yu, Sébastien Guiral
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5837-5841
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human who
Autor:
Zheng Huang, Lei Zhang, Liette Belair, Wayne Sturkenboom, Chun Sing Li, Yeeman K. Ramtohul, Jocelyne Guay, Renata Murgasva
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5214-5217
SCD1 inhibition may represent a novel treatment for obesity, type-2 diabetes and related metabolic disorders. A prototype thiazole amide analog 13 (MF-152) was identified as an excellent tool in the study of SCD biology in animals.
Autor:
Joel Rubin, Erich L. Grimm, Joseph A. Mancini, Richard Friesen, Diane Ethier, Denis Riendeau, Nathalie Méthot, Renee Aspiotis, Jocelyne Guay, Helene Juteau, Sébastien Guiral, Yves Gareau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3352-3355
A series of potent and selective inhibitors of the inducible microsomal PGE2 synthase (mPGES-1) has been developed based on the indole FLAP inhibitor MK-886. Compounds 23 and 30 inhibit mPGES-1 with potencies in the low nanomolar range and with selec
Publikováno v:
Journal of Biological Chemistry. 279:24866-24872
Peripheral inflammation involves an increase in cyclooxygenase-2 (COX-2)-mediated prostaglandin (PG) synthesis in the central nervous system (CNS), which contributes to allodynia and hyperalgesia. In the present study we have determined the changes i
Autor:
Jocelyne Guay, Joseph A. Mancini, David Claveau, Denis Riendeau, Chi-Chung Chan, Katherine Blood, R. Gordon
Publikováno v:
Journal of Biological Chemistry. 276:4469-4475
We have cloned and expressed the inducible form of prostaglandin (PG) E synthase from rat and characterized its regulation of expression in several tissues after in vivo lipopoylsaccharide (LPS) challenge. The rat PGE synthase is 80% identical to the