Zobrazeno 1 - 10
of 63
pro vyhledávání: '"Linus S. Lin"'
Autor:
Catherine Abbadie, Raul F. Alvaro, Lin-Lin Shiao, Mark Rosenbach, Lisa F. Frey, Marc D. Chioda, Ravi P. Nargund, Richard Hajdu, Kathleen Sullivan, Robert J. DeVita, Joseph F. Leone, Kevin M. Belyk, Jenna L. Terebetski, Amanda K. Makarewicz, Elliot J. Martel, Gino Salituro, Bindhu V. Karanam, Raman K. Bakshi, James Dellureficio, Selena Fung, Ping Liu, Linda Chang, Nina Jochnowitz, Shruti Mistry, Joyce Shuman, Linus S. Lin, Yan Guo, Maria Madeira, Shane W. Krska, Mark McLaughlin, Erin McGowan, Harry R. Chobanian, Jessica Alexander, Matthew J. Wyvratt, Qingmei Hong, Thomas J. Lanza
Publikováno v:
ACS Medicinal Chemistry Letters. 5:717-721
We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal chemistry efforts focused on optimizing of FAAH inhibition in vitro pot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0dbc5aefed73bfbd91d72c5b2ca7e347
https://doi.org/10.1021/ml5001239
https://doi.org/10.1021/ml5001239
Autor:
Luis Sojo, Alla Yurevna Zenova, Margaret van Heek, David Percival, Andrea Lindgren, Linus S. Lin, Michael Winther, Shaoyi Sun, Pritpaul Samra, Celene Grayson, Jianmin Fu, Qi Jia, Jing Zhong, Richard A. Dean, Zaihui Zhang, Clark Xie
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:7724-7734
Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease. We describe here the discover
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd21e301ade6e99457ae74b5012bce97
https://doi.org/10.1016/j.bmc.2013.10.023
https://doi.org/10.1016/j.bmc.2013.10.023
Autor:
Richard Hargreaves, Maria Madeira, Patricia Miller, Joyce Powell, Richard Hajdu, Selena Fung, Lin-Lin Shiao, Mark Rosenbach, Ping Liu, Zhizhen Zeng, Qingmei Hong, Catherine Abbadie, Tsing-Bau Chen, Aniket Joshi, Wenping Li, Suzanne M. Mandala, Diane Posavec, Jacquelynn J. Cook, Bindhu V. Karanam, Ling Xu, Jenna L. Terebetski, Marc D. Chioda, Kerry Riffel, Nina Jochnowitz, Robert J. DeVita, Joseph F. Leone, David L. Williams, Mangay Williams, Ravi P. Nargund, Stacey O'Malley, Marie A. Holahan, Linus S. Lin, Sandra Sanabria, Raman K. Bakshi, Mona Purcell, Kathleen A. Sullivan, Yan Guo, Terence G. Hamill, James Dellureficio, Linda Chang, Harry R. Chobanian, Jessica Alexander, Gino Salituro, Hong Jin
Publikováno v:
ACS Medicinal Chemistry Letters. 4:509-513
We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ed1503c306a4b117735b46a064c5a03
https://doi.org/10.1021/ml4000996
https://doi.org/10.1021/ml4000996
Autor:
Linda Chang, Yanqing Kan, Alison M. Strack, Yan Guo, Judith N. Gorski, Linus S. Lin, Maria Madeira, Oksana C. Palyha, Thomas J. Lanza, Randy R. Miller, Jasminka Dragovic, Theresa M. Kelly, Ping Liu, Marc L. Reitman, Ravi P. Nargund, Joseph M. Metzger, Harry R. Chobanian, Donald J. Marsh, Kathy Lyons, Jianmei Pang, Kate A. Raustad, Marc D. Chioda, Xiao-Ming Guan, Sheng-Ping Wang
Publikováno v:
ACS Medicinal Chemistry Letters. 3:252-256
Extensive structure-activity relationship studies of a series derived from atropisomer 1, a previously described chiral benzodiazepine sulfonamide series, led to a potent, brain penetrant and selective compound with excellent preclinical pharmacokine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97ff5cc4464b6f25f4e8bebfcd480a62
https://doi.org/10.1021/ml200304j
https://doi.org/10.1021/ml200304j
Autor:
Oksana C. Palyha, Terry D. Faidley, Joseph M. Metzger, Xiao-Ming Guan, Sheng-Ping Wang, Jennifer A. Kosinski, Ravi P. Nargund, Stephanie K. Spann, Marc L. Reitman, Liming Yang, Linus S. Lin, Lauren P. Shearman, Kate A. Raustad, Donald J. Marsh, Kathy Lyons, Theresa M. Kelly, Stephanie Craw, Alison M. Strack, Yanqing Kan, Hong Yu, Jasminka Dragovic, Iyassu K. Sebhat
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 336:356-364
Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor implicated in the regulation of energy homeostasis. Here, we report the biologic effects of a highly optimized BRS-3 agonist, (2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)pheny
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f83aba6c5ca83619726b27f1351081f
https://doi.org/10.1124/jpet.110.174763
https://doi.org/10.1124/jpet.110.174763
Autor:
Laurie G. Castonguay, Sookhee Ha, Lex H.T. Van der Ploeg, Chun-Pyn Shen, Ihor E. Kopka, Zhege J. Lao, Mark T. Goulet, Linus S. Lin, William K. Hagmann, Tung M. Fong, James P. Jewell, Thomas J. Lanza
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4757-4761
The design, synthesis, and binding activity of ring constrained analogs of the acyclic cannabinoid-1 receptor (CB1R) inverse agonist taranabant 1 are described. The initial inspiration for these taranabant derivatives was its conformation 1a, determi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::737e62d3613615a82eb8f34fb466c9e0
https://doi.org/10.1016/j.bmcl.2010.06.127
https://doi.org/10.1016/j.bmcl.2010.06.127
Autor:
Nathan X. Yu, Thomas J. Lanza, Koppara Samuel, Sanjeev Kumar, George A. Doss, Vijay Bhasker G. Reddy, Ralph A. Stearns, Bindhu V. Karanam, Linus S. Lin, Conrad E. Raab, Andy Shiqiang Zhang
Publikováno v:
Xenobiotica. 40:650-662
The metabolism and excretion of taranabant (MK-0364, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2{[5-(trifluoromethyl)pyridine-2-yl]oxy}propanamide), a potent cannabinoid-1 receptor inverse agonist, were evaluated in rat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::018365d6fb66bbbdd95a6bcd0041c218
https://doi.org/10.3109/00498254.2010.501117
https://doi.org/10.3109/00498254.2010.501117
Autor:
Marc L. Reitman, Cheng Guo, Theresa M. Kelly, Constantin Tamvakopoulos, Joseph M. Metzger, Tianying Jian, Howard Y. Chen, Arthur A. Patchett, Oksana C. Palyha, Alison M. Strack, Allan J. Goodman, Ravi P. Nargund, Peter H. Dobbelaar, Yanqing Kan, Mark Hadden, Larry Yet, Peter R. Guzzo, Qianping Peng, Linus S. Lin, Shuwen He, Lauren P. Shearman, Alan J. Henderson, Carina P. Tan, Sargent Bruce J, Xiao-Ming Guan, Scott D. Feighner, Iyassu K. Sebhat, Jie Pan, Jian Liu, Donald J. Marsh, Matthew J. Wyvratt, Andrew D. Howard, Megan Ruenz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1913-1917
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rode
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c9388422b542c24893358d41aa77156
https://doi.org/10.1016/j.bmcl.2010.01.154
https://doi.org/10.1016/j.bmcl.2010.01.154
Autor:
Gerard R. Kieczykowski, Carrie P. Jones, Ping Liu, Junying Wang, Conrad E. Raab, Qian Si, Xinchun Tong, Thomas J. Lanza, Anne Schuelke, Kelly M. Treonze, Richard A. Mumford, Salony Manior, Stella H. Vincent, James V. Pivnichny, Gloria C. Koo, James P. Jewell, William K. Hagmann, Regina W. Wang, Philip Davies, Linus S. Lin, Malcolm MacCoss
Publikováno v:
Journal of Medicinal Chemistry. 52:3449-3452
Extremely potent very late antigen-4 (VLA-4) antagonists with picomolar, whole blood activity and slow dissociation rates were discovered by incorporating an amino substituent on the proline fragment of the initial lead structure. This level of poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a2b44376091abb5e0b00c51b9e55a39
https://doi.org/10.1021/jm900257b
https://doi.org/10.1021/jm900257b
Autor:
Terence G. Hamill, Brett Connolly, Ping Liu, Tung M. Fong, Christine Ryan, Richard Hargreaves, Linus S. Lin, Mark T. Goulet, Amy Vanko, Wai-Si Eng, William K. Hagmann, James P. Jewell, H. Donald Burns, Sandra Sanabria
Publikováno v:
Molecular Imaging and Biology. 11:246-252
The in vitro and in vivo evaluation of the selective, high affinity (human CB1 IC(50) 0.49 nM) inverse agonist CB1R tracer [(11)C]CB-119, a close analog of the previously disclosed [(18)F]MK-9470, was undertaken.[(11)C]CB-119 was synthesized with hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59bc2ff712b2f92b6b1cb1730f93c1a0
https://doi.org/10.1007/s11307-008-0194-8
https://doi.org/10.1007/s11307-008-0194-8