Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Douglas C. Harnish"'
Autor:
Mark J. Evans, Paige Erin Mahaney, Jay E. Wrobel, Matthew L. Crawley, Ray Unwalla, Kim Callain Younghee, John F. Mehlmann, Joseph T. Lundquist, Douglas C. Harnish
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5289-5292
Pyrrole[2,3-d]azepines have been identified as potent agonists of the farnesoid X receptor (FXR). Based on the planar X-ray crystal structure of WAY-362450 1 in the ligand binding domain and molecular modeling studies, non-planar reduced compounds we
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87fc54b4c31896488fb9960b3d992553
https://doi.org/10.1016/j.bmcl.2009.07.148
https://doi.org/10.1016/j.bmcl.2009.07.148
Autor:
Janet E. Paulsen, Zhijian Lu, Grace Yan, Jocelyn Sanford, Heather H. Shih, Adam Reid Root, Khetemenee Lam, Douglas C Harnish, Richard Zollner, Wei Cao, Lioudmila Tchistiakova, Mostafa Ait-Zahra, Valerie Calabro, Rita Agostinelli, Stephane Olland, Davinder Gill, Angela Robak
Publikováno v:
FEBS Journal. 276:4909-4920
LOX-1 is a scavenger receptor that functions as the primary receptor for oxidized low-density lipoprotein (OxLDL) in endothelial cells. The binding of OxLDL to LOX-1 is believed to lead to endothelial activation, dysfunction, and injury, which consti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f02942f24cebe8e4a9b6be49bf5a02f0
https://doi.org/10.1111/j.1742-4658.2009.07190.x
https://doi.org/10.1111/j.1742-4658.2009.07190.x
Autor:
Lisa Borges-Marcucci, Christine Huard, KehDih Lai, George P. Vlasuk, Douglas C. Harnish, Stephen J. Gardell, Mark J. Evans, Paige E. Mahaney, Julie A. Krueger, Shuguang Wang, Robert V. Martinez
Publikováno v:
American Journal of Physiology-Gastrointestinal and Liver Physiology. 296:G543-G552
The nuclear hormone receptor farnesoid X receptor (FXR) plays a critical role in the regulation of bile acid, triglyceride (TG), and cholesterol homeostasis. WAY-362450 (FXR-450/XL335) is a potent synthetic FXR agonist as characterized in luciferase
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb4b88e8a098fdd5710036af27194aeb
https://doi.org/10.1152/ajpgi.90585.2008
https://doi.org/10.1152/ajpgi.90585.2008
Autor:
Robert John Steffan, Eugene John Trybulski, Douglas C. Harnish, Fei Ye, Paige E. Mahaney, Joseph P. Sabatucci, Michael Byron Webb, Christopher C. Chadwick
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:3455-3466
The anti-inflammatory activity of non-selective estrogens has been attributed to their ability to antagonize the activity of nuclear factor kappaB (NF-kappaB), a known mediator of inflammatory responses. Here we report the identification of a potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20476238f8753f165de44d1230e89e5b
https://doi.org/10.1016/j.bmc.2006.01.001
https://doi.org/10.1016/j.bmc.2006.01.001
Autor:
Christopher C. Chadwick, Mary-Margaret O’Donnell, Eugene John Trybulski, Douglas C. Harnish, Mark A. Ashwell, Moore William Jay, Joseph P. Sabatucci
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:854-858
The transcription factor nuclear factor-kappaB (NF-kappaB) is a key component in the onset of inflammation. We describe here a series of 4-hydroxyphenyl sulfonamide estrogen receptor (ER) ligands that selectively inhibit NK-kappaB transcriptional act
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3dafa8b767ce575a06811ad05cc34677
https://doi.org/10.1016/j.bmcl.2005.11.015
https://doi.org/10.1016/j.bmcl.2005.11.015
Autor:
Robert John Steffan, Lydia Mosyak, Richard C. Winneker, Susan Chippari, Lisa Borges-Marcucci, Amy Eckert, William Jay Moore, Zhang Xu, Edward Martin Matelan, Christopher C. Chadwick, Mark A. Ashwell, William Ronald Solvibile, Steven J. Adelman, Thomas Kenney, Eugene John Trybulski, Douglas C. Harnish
Publikováno v:
Current Topics in Medicinal Chemistry. 6:103-111
The discovery of novel intervention points in the inflammatory pathway has been a focus of drug development in recent years. We have identified pathway selective ligands for the estrogen receptor (ER) that inhibit NF-kappaB mediated inflammatory gene
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fed82e50c368a115db9d8021ee12b246
https://doi.org/10.2174/156802606775270279
https://doi.org/10.2174/156802606775270279
Publikováno v:
American Journal of Physiology-Gastrointestinal and Liver Physiology. 289:G267-G273
Previous studies have demonstrated a dramatic induction of inflammatory gene expression in livers from mice fed a high-fat, high-cholesterol diet containing cholate after 3–5 wk. To determine the contribution of cholate in mediating these induction
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4051b9ea84dd481ca96590b98ccd6dd
https://doi.org/10.1152/ajpgi.00043.2005
https://doi.org/10.1152/ajpgi.00043.2005
Autor:
Leo M. Albert, Yelena Leathurby, Lili Wang, Max Follettie, Lisa Borges-Marcucci, Robert John Steffan, James C. Keith, Christopher C. Chadwick, Douglas C. Harnish
Publikováno v:
Arthritis Research & Therapy
Rheumatoid arthritis (RA) is a chronic inflammatory disease that produces synovial proliferation and joint erosions. The pathologic lesions of RA are driven through the production of inflammatory mediators in the synovium mediated, in part, by the tr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8e1511545e006dd12d5076b8eb90120
http://europepmc.org/articles/PMC1174937
http://europepmc.org/articles/PMC1174937
Publikováno v:
Journal of Biological Chemistry. 278:36418-36429
Hormonal status can influence diverse metabolic pathways. Small heterodimer partner (SHP) is an orphan nuclear receptor that can modulate the activity of several transcription factors. Estrogens are here shown to directly induce expression of the SHP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fc901d98abb8bb325673a8ccc2b4aee
https://doi.org/10.1074/jbc.m303913200
https://doi.org/10.1074/jbc.m303913200
Publikováno v:
Circulation Research. 89:823-830
The functional interaction, or "cross-talk," between estrogen receptor (ER) and the proinflammatory transcription factor nuclear factor (NF)-kappaB demonstrated in vitro has been suggested to play a role in estrogen prevention of cardiovascular disea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0464e151ba24ccfbfb3ce8da4aee73d
https://doi.org/10.1161/hh2101.098543
https://doi.org/10.1161/hh2101.098543