Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Hussien A. Al-Shamma"'
Autor:
Michelle Solomon, Laurent Peyrin-Biroulet, Hussien A. Al-Shamma, H. Kiyomi Komori, John E. Adams, Karin Lehmann-Bruinsma, Chris Carroll
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 369:311-317
Lymphocyte trafficking out of secondary lymphoid organs is regulated by concentration gradient-dependent interactions between the membrane-derived lysophospholipid signaling molecule sphingosine 1-phosphate (S1P) and the G-protein-coupled receptor, S
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01355e304cf7ad94955531e69d39dbe0
https://doi.org/10.1124/jpet.118.254268
https://doi.org/10.1124/jpet.118.254268
Autor:
Michelle Solomon, Lars Thoresen, Robert M. Jones, Andrew J. Grottick, David J. Unett, Abu J.M. Sadeque, Chuan Chen, Ibragim Gaidarov, Hussien A. Al-Shamma, Jayant Thatte, Graeme Semple, Jae-Kyu Jung, Amin Usmani, Jeremy Barden, Xiuwen Zhu, Woo Hyun Yoon, Sangdon Han, Christopher Ronald J
Publikováno v:
ACS Medicinal Chemistry Letters. 8:1309-1313
The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6 was efficacious in a rat model of osteoarthritis pain following oral administration and, in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f1f3e8c8d79ed5129b2137300ee1326f
https://doi.org/10.1021/acsmedchemlett.7b00396
https://doi.org/10.1021/acsmedchemlett.7b00396
Autor:
Hussien A. Al-Shamma, Michael Morgan, Ibragim Gaidarov, Huong T. Dang, Joel Gatlin, Marc Decaire, David J. Unett, Karoline Choi, Jeff Edwards, Dawei Yue, Abu J.M. Sadeque, Kevin Whelan, Yifeng Xiong, Lixia Fu, Jayant Thatte, Graeme Semple, Sonja Strah-Pleynet, Sangdon Han, Michelle Solomon, Dominic P. Behan, Jae-Kyu Jung, Sanju Narayanan, Lars Thoresen, Robert M. Jones, Chuan Chen, Xiuwen Zhu, Khawja A. Usmani, Cameron Pride, Ruoping Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:322-326
The design and synthesis of novel 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamide CB2 selective ligands for the potential treatment of pain is described. Compound (R,R)-25 has good balance between CB2 agonist potency and selecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b59f936b671e7316d482a837b15c5aa1
https://doi.org/10.1016/j.bmcl.2014.11.040
https://doi.org/10.1016/j.bmcl.2014.11.040
Autor:
Ben Johnson, Tawfik Gharbaoui, Moody Jeanne, David J. Unett, Kevin Whelan, Ibragim Gaidarov, Michael Morgan, Lars Thoresen, Michelle Kasem, Abu J.M. Sadeque, Robert M. Jones, Chuan Chen, Sun Hee Kim, Hussien A. Al-Shamma, Minh Le, Joel Gatlin, Lorene Calvano, Andrew M. Kawasaki, Lixia Fu, Yinghong Gao, Scott Stirn, Weichao Chen, Jeremy Barden, Dominic P. Behan, Krishnan Ashwin M, Xiuwen Zhu, Graeme Semple, Dipanjan Sengupta, Christopher Ronald J, Jeff Edwards, Luis Lopez, Jayant Thatte, Daniel J. Buzard, Anthony C. Blackburn, Michelle Solomon, Todd Anthony, Thomas O. Schrader, Khawja A. Usmani
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1334-1339
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fc0ba742321c1acedff3bc45fe90e44
https://doi.org/10.1021/ml500422m
https://doi.org/10.1021/ml500422m
Autor:
Weichao Chen, Andrew M. Kawasaki, Dominic P. Behan, Jeff Edwards, You-An Ma, Tawfik Gharbaoui, Sun Hee Kim, Jayant Thatte, Hussien A. Al-Shamma, Carleton R. Sage, Jeremy Barden, Anthony C. Blackburn, Michelle Solomon, Xiuwen Zhu, Christopher Ronald J, David Mills, Ibragim Gaidarov, Antonio Garrido Montalban, Sangdon Han, Luis Lopez, Dipanjan Sengupta, Michael Morgan, Juerg Lehmann, Daniel J. Buzard, Graeme Semple, Kevin Whelan, Yinghong Gao, Joel Gatlin, Moody Jeanne, David J. Unett, Imelda Calderon, Lars Thoresen, Robert M. Jones, Brett Ullman, Todd Anthony, Chuan Chen, Minh Le, Khawja A. Usmani, Scott Stirn, Jaimie Karyn Rueter, Lixia Fu, Lorene Calvano, Abu J.M. Sadeque
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1313-1317
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases. APD3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d5c928b700e5c29f65a914afc10b3e5
https://doi.org/10.1021/ml500389m
https://doi.org/10.1021/ml500389m
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease
Autor:
Joel Gatlin, Kevin Whelan, Michael Morgan, Juerg Lehmann, Lixia Fu, Yinghong Gao, Moody Jeanne, Minh Le, Hussien A. Al-Shamma, Jeremy Barden, Khawja A. Usmani, Jeff Edwards, Chuan Chen, Jayant Thatte, Dipanjan Sengupta, Xiuwen Zhu, Abu J.M. Sadeque, Imelda Calderon, Michelle Solomon, Lars Thoresen, Tawfik Gharbaoui, Robert M. Jones, Ling Liu, Luis Lopez, Daniel J. Buzard, Brett Ullman, Krishnan Ashwin M, Sheryll Espinola, Charles Xing, Sangdon Han, Andrew M. Kawasaki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4404-4409
Two series of fused tricyclic indoles were identified as potent and selective S1P(1) agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6722bc3de77ac97d0eefdb7ba4c15536
https://doi.org/10.1016/j.bmcl.2012.04.129
https://doi.org/10.1016/j.bmcl.2012.04.129
Autor:
Marc Decaire, Graeme Semple, Yifeng Xiong, Andrew J. Grottick, Woo H. Yoon, Kevin Whelan, Sonja Strah-Pleynet, Martin C. Cherrier, Brett Ullman, John Frazer, Hussien A. Al-Shamma, Jin-Sun Karoline Choi, Konrad Feichtinger, Erin K. Sanabria
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1870-1873
A series of fused bicyclic heterocycles was identified as potent and selective 5-HT 2A receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d847b773d26b55ba6e956b096b7717df
https://doi.org/10.1016/j.bmcl.2012.01.080
https://doi.org/10.1016/j.bmcl.2012.01.080
Autor:
Lixia Fu, Jeremy Barden, Joel Gatlin, Andrew M. Kawasaki, Minh Le, Jeff Edwards, Hussien A. Al-Shamma, Jayant Thatte, Charles Xing, Yinghong Gao, Moody Jeanne, Michelle Solomon, Sangdon Han, Carleton R. Sage, Thomas O. Schrader, Sheryll Espinola, Luis Lopez, Daniel J. Buzard, Ling Liu, Lars Thoresen, Robert M. Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6013-6018
S1P1 receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P1 receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0116d2d9cbafd603a96e49505c156afd
https://doi.org/10.1016/j.bmcl.2011.05.110
https://doi.org/10.1016/j.bmcl.2011.05.110
Autor:
Andrew L. Frelinger, Karin Przyklenk, Hussien A. Al-Shamma, Michael Morgan, Matthew D. Linden, YouFu Li, Marc R. Barnard, John W. Adams, Alan D. Michelson, Peter Whittaker
Publikováno v:
Journal of Thrombosis and Haemostasis. 8:331-340
Release of serotonin and activation of serotonin 5HT2A receptors on platelet surfaces is a potent augmentative stimulus for platelet aggregation. However, earlier-generation serotonin receptor antagonists were not successfully exploited as antiplatel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a3edf0d75e70939f58c81f12bd54cc2
https://doi.org/10.1111/j.1538-7836.2009.03693.x
https://doi.org/10.1111/j.1538-7836.2009.03693.x
Autor:
Peter I. Dosa, Yunqing Shi, Bradley Teegarden, Hussien A. Al-Shamma, Dominic P. Behan, John W. Adams, Michael Morgan, Jeremy G. Richman, William Thomsen, Daniel T. Connolly, Juan Ramirez, Danny Ortuno
Publikováno v:
European Journal of Pharmacology. 586:234-243
We have evaluated the anti-platelet and vascular pharmacology of AR246686, a novel 5-hydroxytryptamine2A (5-HT2A) receptor antagonist. AR246686 displayed high affinity binding to membranes of HEK cells stably expressing recombinant human and rat 5-HT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4fe1cc907ef4cb76ec4b2a20df224a97
https://doi.org/10.1016/j.ejphar.2007.11.056
https://doi.org/10.1016/j.ejphar.2007.11.056