Zobrazeno 1 - 10
of 51
pro vyhledávání: '"W Cameron, Black"'
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:
W. Cameron Black, Michael Zinda, Jordan T.F. Young, Zuomei Li, Yael Mamane, Rino Stocco, Martine Hamel, Artur Veloso, Victoria Rimkunas, Amina Mulani, Kathryn Skorey, Sabrina Vignini-Hammond, Chloe Fugère-Desjardins, William Yang, Hunain Alam, Amandine Chefson, Shou Yun Yin, Marie-Eve Leclaire, Li Li, Sara Fournier, Lee D. Fader, Stéphane Dorich, Valerie Dumais, Émilie Dumas-Bérube, Charles Pellerin, Alexander Skeldon, Robert Papp, Michal Zimmermann, Anne Roulston
Supplementary Methods, Tables, Figures and References
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::062cfaf9177f49a3206feb599326f494
https://doi.org/10.1158/1535-7163.22896018
https://doi.org/10.1158/1535-7163.22896018
Autor:
W. Cameron Black, Michael Zinda, Jordan T.F. Young, Zuomei Li, Yael Mamane, Rino Stocco, Martine Hamel, Artur Veloso, Victoria Rimkunas, Amina Mulani, Kathryn Skorey, Sabrina Vignini-Hammond, Chloe Fugère-Desjardins, William Yang, Hunain Alam, Amandine Chefson, Shou Yun Yin, Marie-Eve Leclaire, Li Li, Sara Fournier, Lee D. Fader, Stéphane Dorich, Valerie Dumais, Émilie Dumas-Bérube, Charles Pellerin, Alexander Skeldon, Robert Papp, Michal Zimmermann, Anne Roulston
Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-stage ATR kinase inhibitor (NCT04497116). RP-3500 is highly potent with IC50 values of 1.0 and 0.33
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a51beae2425d617ba7d0ef61e96c7e6
https://doi.org/10.1158/1535-7163.c.6651330.v1
https://doi.org/10.1158/1535-7163.c.6651330.v1
Autor:
Anne Roulston, Michal Zimmermann, Robert Papp, Alexander Skeldon, Charles Pellerin, Émilie Dumas-Bérube, Valerie Dumais, Stéphane Dorich, Lee D. Fader, Sara Fournier, Li Li, Marie-Eve Leclaire, Shou Yun Yin, Amandine Chefson, Hunain Alam, William Yang, Chloe Fugère-Desjardins, Sabrina Vignini-Hammond, Kathryn Skorey, Amina Mulani, Victoria Rimkunas, Artur Veloso, Martine Hamel, Rino Stocco, Yael Mamane, Zuomei Li, Jordan T.F. Young, Michael Zinda, W. Cameron Black
Publikováno v:
Molecular Cancer Therapeutics. 21:245-256
Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-stage ATR kinase inhibitor (NCT04497116). RP-3500 is highly potent with IC50 values of 1.0 and 0.33
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5c5c2c693c809fd51b04d00ce59692a4
https://doi.org/10.1158/1535-7163.mct-21-0615
https://doi.org/10.1158/1535-7163.mct-21-0615
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:
Joel Robichaud, Nicolas Morin, Sébastien Gagné, Michel Belley, Lianhai Li, Genevieve Lavallee, Geoffrey K. Tranmer, Yves Gareau, Erin F. Mulrooney, W. Cameron Black, Stacia Kargman, Jean-François Lévesque, Joseph A. Mancini, Jacques Yves Gauthier, Jean-François Fournier, Denis Deschenes, Jin Wu, Martine Hamel, Zhaoyin Wang, Michel Therien, Martin Henault, Yaël Mamane, Huda Hyjazie
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2836-2839
A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY(14) with a naphthoic acid core was identified through high-throughput screening. Optimization provided compounds with improved potency but poor pharmacokinetics. Acylglucuronidati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e882d0ef4cdd630e17158a34b627a7e
https://doi.org/10.1016/j.bmcl.2011.03.081
https://doi.org/10.1016/j.bmcl.2011.03.081
Autor:
Robert Gordon, Lijing Xu, Michel Therien, W. Cameron Black, Martin Henault, Yaël Mamane, Chi-Chung Chan, Vouy Linh Truong, Michel Belley, Huda Hyjazie, Daniel Guay, Geoffrey K. Tranmer, Jeancarlo DeLuca, Zhaoyin Wang, Stacia Kargman, Christian Beaulieu, Martine Hamel, Sheldon Crane, Joseph A. Mancini, Lianhai Li, Nicolas Morin, Yves Gareau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2832-2835
A weak antagonist of the pyrimidinergic receptor P2Y(14) containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists and represent the first report
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f402223a76e1d1b4bfb68e56fd6b8f8f
https://doi.org/10.1016/j.bmcl.2011.03.084
https://doi.org/10.1016/j.bmcl.2011.03.084
Autor:
Christophe Mellon, Nathalie Méthot, Deborah A. Nicoll-Griffith, Momar Ndao, Frédéric Massé, Christian Beaulieu, Angélique Fortier, Hyeram Park, W. Cameron Black, Elise Isabel, Doris Lee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7444-7449
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease is described. The identified inhibitors bearing an amino nitrile warhead in P1 exhibit low nanomolar in vitro potency against cruzipain. Further SAR in P
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6582e07a38a94405e3fdc8c323756d1
https://doi.org/10.1016/j.bmcl.2010.10.015
https://doi.org/10.1016/j.bmcl.2010.10.015
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04ce075aa9949065722c92768a34c9f4
https://doi.org/10.1016/j.bmcl.2009.12.083
https://doi.org/10.1016/j.bmcl.2009.12.083
Autor:
Maureen Pickarski, Denis Riendeau, Paul Tawa, Le Thi Duong, Sonia Lamontagne, W. Cameron Black, M. David Percival, Renata Oballa, Sylvie Desmarais
Publikováno v:
Molecular Pharmacology. 73:147-156
Cathepsin K is a lysosomal cysteine protease that is a pharmacological target for the treatment of osteoporosis. Previous studies showed that basic, lipophilic cathepsin K inhibitors are lysosomotropic and have greater activities in cell-based assays
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61a7d4edad73f4f59f727b1a27283b6c
https://doi.org/10.1124/mol.107.039511
https://doi.org/10.1124/mol.107.039511