Zobrazeno 1 - 10
of 51
pro vyhledávání: '"Michel, Gallant"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::947c93bf7b6803db8ed4beb935e92af5
https://doi.org/10.1021/acs.jmedchem.2c00998
https://doi.org/10.1021/acs.jmedchem.2c00998
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::531f44b082fb5f00fe6c2f82d97a48bc
https://pubmed.ncbi.nlm.nih.gov/36126059
https://pubmed.ncbi.nlm.nih.gov/36126059
Autor:
John W. Phillips, Xin Gu, Mihai Petcu, Molly M. Lin, Ronald E. Painter, Michel Gallant, Lynn Miesel, Kathryn Skorey, Kenneth E. Wilson, David Claveau, Liliana L. Benton-Perdomo, Kathleen Deschamps, Christopher M. Tan, Katherine Young, Andrew Galgoci, John Tam, Christian Lebeau-Jacob, Alexandre Caron, Young-Whan Park, Suzy Lee, Simon Wong, Patrick Beaulieu, Craig A. Parish, Aimie M. Ogawa, Josiane Lafleur, Alex G. Therien, Nancy J. Kevin, Sherman T. Waddell, Robert G. K. Donald, Penny Sue Leavitt, Mary Ann Powles, Joann Huber, Anna A. Michels
Publikováno v:
Antimicrobial Agents and Chemotherapy. 56:4662-4670
The resistance of methicillin-resistant Staphylococcus aureus (MRSA) to all β-lactam classes limits treatment options for serious infections involving this organism. Our goal is to discover new agents that restore the activity of β-lactams against
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2bc01435a04348f73f58cdb283cf572
https://doi.org/10.1128/aac.00726-12
https://doi.org/10.1128/aac.00726-12
Autor:
Kelly Bleasby, Dwight Macdonald, Bruce Mackay, Richard Tschirret-Guth, Robert Houle, Sebastien Laliberte, Patrick Lacombe, Robert Papp, Erich L. Grimm, Amandine Chefson, Jean-François Lévesque, Michael J. Hafey, Pierre-André Fournier, Sébastien Gagné, Yongxin Han, Yves Ducharme, Michel Gallant, Austin Chen, Daniel Dube
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5547-5551
An oral bioavailability issue encountered during the course of lead optimization in the renin program is described herein. The low F(po) of pyridone analogs was shown to be caused by a combination of poor passive permeability and gut efflux transport
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2b390428a9f09b127996a8190fb39ae
https://doi.org/10.1016/j.bmcl.2011.06.095
https://doi.org/10.1016/j.bmcl.2011.06.095
Autor:
Robert Houle, Jean François Lévesque, Daniel Simard, François G. Gervais, Carl Berthelette, Carmela Molinaro, Yves Leblanc, Martine Hamel, Michel Gallant, Helmi Zaghdane, Nicole Sawyer, Susan Sillaots, Zhaoyin Wang, Michael J. Boyd, John Colucci, Rino Stocco
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3471-3474
A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a09028c83914f05337f367fe720b7f52
https://doi.org/10.1016/j.bmcl.2011.03.085
https://doi.org/10.1016/j.bmcl.2011.03.085
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5869451b5d4a9f35f5a8af8a027ba80
https://doi.org/10.1016/j.bmcl.2011.02.067
https://doi.org/10.1016/j.bmcl.2011.02.067
Autor:
Danielle Denis, François G. Gervais, Rino Stocco, Stephen Lau, Birgit Kosjek, Michel Gallant, Vouy Linh Truong, Helmi Zaghdane, Dan Sørensen, Deborah Slipetz, Christophe Mellon, Gary P. O'Neill, Ernest E. Lee, Robert Houle, Yves Leblanc, Carl Berthelette, Daniel Guay, Carmela Molinaro, Jean-François Lévesque, Elizabeth Wong, Jin Wu, Yves Ducharme, Michael A. Crackower, John Colucci, Connie M. Krawczyk, Richard Friesen, Paul D. O’Shea, Nicole Sawyer, Susan Sillaots, Zhaoyin Wang, Christian Beaulieu, Daniel Simard, Chad Dalton, Wayne Mullet, Martine Hamel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:288-293
In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences enabling the preparation of this novel class of CRTH2 antagonist are r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62517a8c6d9944543c6229358efce07b
https://doi.org/10.1016/j.bmcl.2010.11.015
https://doi.org/10.1016/j.bmcl.2010.11.015
Autor:
Michel Gallant, William M. Abraham, Deborah Slipetz, Elizabeth Wong, Martine Hamel, Rino Stocco, Nicole Sawyer, Susan Sillaots, Zhaoyin Wang, François G. Gervais, Danielle Denis, Michael A. Crackower, Connie M. Krawczyk, Gary P. O'Neill
Publikováno v:
Molecular Pharmacology. 79:69-76
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor that has been reported to modulate inflammatory responses in various rodent models of asthma, allergic rhinitis and atopic der
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b80f4db8e25ec96d9d785bd7722e9d97
https://doi.org/10.1124/mol.110.068585
https://doi.org/10.1124/mol.110.068585
Autor:
Christopher I. Bayly, Dan McKay, Tom Y.-H. Wu, Patrick Roy, Suzanna Liu, Michel Gallant, Austin Chen, Helene Juteau, Rejean Fortin, Daniel Dube, Renee Aspiotis, Patrick Lacombe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5822-5826
The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple, substituted aromatic ring suc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86c8a097e1c75222e7013c703f6e14c4
https://doi.org/10.1016/j.bmcl.2010.07.127
https://doi.org/10.1016/j.bmcl.2010.07.127
Autor:
Kenneth Ho, Meenakshi Sundaram, Yves L. Marcel, Ming-Dong Wang, Michel Gallant, Robert S. Kiss, Vivian Franklin
Publikováno v:
Journal of Biological Chemistry. 282:22525-22533
Niemann-Pick type C1 (Npc1) protein inactivation results in lipid accumulation in late endosomes and lysosomes, leading to a defect of ATP binding cassette protein A1 (Abca1)-mediated lipid efflux to apolipoprotein A-I (apoA-I) in macrophages and fib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8094152256f95318e7a5efe4a208d600
https://doi.org/10.1074/jbc.m700326200
https://doi.org/10.1074/jbc.m700326200