Zobrazeno 1 - 10
of 22
pro vyhledávání: '"François G. Gervais"'
Autor:
Jason D. Katz, François G. Gervais, Lauren Dorosh, Milenko Cicmil, Khamir Mehta, Joey L. Methot, Janice D Woodhouse, Hongshi Yu, Hani Houshyar, Prasanthi Geda, Gretchen A. Baltus, Malgorzata A Gil, Antonio Cabal, Sanjiv J. Shah, Robbie L. McLeod, Dapeng Chen, Alan S. Bass, Stephen E. Alves, Michael Caniga
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 369:223-233
We leveraged a clinical pharmacokinetic (PK)/pharmacodynamics (PD)/efficacy relationship established with an oral phosphatidylinositol 3-kinase (PI3K)δ inhibitor (Idelalisib) in a nasal allergen challenge study to determine whether a comparable PK/P
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ae30672ed16800c8692f183b1d4851d
https://doi.org/10.1124/jpet.118.252551
https://doi.org/10.1124/jpet.118.252551
Autor:
Craig C. Correll, Robert G. Aslanian, Li Xiao, Rema Bitar, Wei Zhou, John W. Butcher, Charles G. Garlisi, Joshua Close, Rachel N. Maccoss, Joon Jung, Scott Crawford, Kevin M. Maloney, Purakkattle Biju, Anandan Palani, Xianhai Huang, Xiaoxin Yang, Kevin D. McCormick, Scott Peterson, Hongjun Zhang, Diane Rindgen, Ying Huang, Alexei V. Buevich, Ning Shao, Li Dong, Phieng Siliphaivanh, Jason D. Brubaker, Michelle Martinez, Hongchen Qiu, François G. Gervais, Ravi P. Nargund, Zhidan Liu
Publikováno v:
ACS Medicinal Chemistry Letters. 9:679-684
[Image: see text] A novel series of tricyclic tetrahydroquinolines were identified as potent and selective CRTh2 receptor antagonists. The agonism and antagonism switch was achieved through structure-based drug design (SBDD) using a CRTh2 receptor ho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8efda955acd4eb892808b6d65e2545f5
https://doi.org/10.1021/acsmedchemlett.8b00145
https://doi.org/10.1021/acsmedchemlett.8b00145
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:
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:
YiLi Ding, Yongxin Han, François G. Gervais, Shilan Liu, Leanne Bedard, Robert B. Lobell, Hongmei Wang, Shuhui Chen, Angela Wong, Martin Henault, Jingchao Dong, David M. Stout, Hao Wu, Ge Li, Stacia Kargman, Nicole Sawyer, R. W. Friesen, Yinhui Liu, Manuel Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5741-5745
We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dffc3d9548b1256ab1668d8e9a829d4a
https://doi.org/10.1016/j.bmcl.2009.08.014
https://doi.org/10.1016/j.bmcl.2009.08.014
Autor:
Mark Leppert, Mary Beth Scholand, Michel Boutin, François G. Gervais, Carl Berthelette, Kevin P. Bateman, Pierre Thibault, John R. Hoidal
Publikováno v:
Analytical Chemistry. 81:1881-1887
Chronic obstructive pulmonary disease (COPD) is characterized by the degradation of elastin, the major insoluble protein of lung tissues. The degradation of elastin gives rise to desmosine (DES) and isodesmosine (IDES), two major urinary products typ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1e054f08e4240b37bb620211617c757
https://doi.org/10.1021/ac801745d
https://doi.org/10.1021/ac801745d
Autor:
Gary P. O'Neill, A. Daniel Malebranche, Jean-Pierre Morello, Gillian Greig, François G. Gervais, Danielle Denis, Nicole Sawyer, Christian Beaulieu
Publikováno v:
Molecular Pharmacology. 67:1834-1839
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor whose function in vivo has been incompletely characterized. One of the reasons is that its current known ligands, prostaglandi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1271b64f9fc61533a8ac582ed4db32a4
https://doi.org/10.1124/mol.104.009068
https://doi.org/10.1124/mol.104.009068
Autor:
Kathleen M. Metters, Martin Desrosiers, Gary P. O'Neill, François G. Gervais, Carolyn Fong, Sonia Lamontagne, François Nantel, D. Hamish Wright, Adel Giaid
Publikováno v:
Prostaglandins & Other Lipid Mediators. 73:87-101
Rationale Prostaglandin D 2 (PGD 2 ) is released from mast cells during the allergic response. Since PGD 2 has been shown to induce nasal congestion in humans, we investigated the distribution of hematopoietic Prostaglandin D synthase (PGDS) and the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::542b9126bad8759d153ff820eba525a0
https://doi.org/10.1016/j.prostaglandins.2003.12.002
https://doi.org/10.1016/j.prostaglandins.2003.12.002
Autor:
Elizabeth Cauchon, Nicole Sawyer, François G. Gervais, Rani P.G. Cruz, Gary P. O'Neill, Donald W. Nicholson, Kathleen M. Metters, Anne Chateauneuf
Publikováno v:
British Journal of Pharmacology. 137:1163-1172
1. The recombinant human prostaglandin D(2) (PGD(2)) receptor, hCRTH2, has been expressed in HEK293(EBNA) and characterized with respect to radioligand binding and signal transduction properties. High and low affinity binding sites for PGD(2) were id
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1053bc5b72b1ddfa9a7ff4a5f33abcfe
https://doi.org/10.1038/sj.bjp.0704973
https://doi.org/10.1038/sj.bjp.0704973