Zobrazeno 1 - 10
of 19
pro vyhledávání: '"William J. Zavadoski"'
Autor:
Ahmed E Enayetallah, Daniel Ziemek, Michael T Leininger, Ranjit Randhawa, Jianxin Yang, Tara B Manion, Dawn E Mather, William J Zavadoski, Max Kuhn, Judith L Treadway, Shelly Ann G des Etages, E Michael Gibbs, Nigel Greene, Claire M Steppan
Publikováno v:
PLoS ONE, Vol 6, Iss 11, p e27009 (2011)
Triglyceride accumulation is associated with obesity and type 2 diabetes. Genetic disruption of diacylglycerol acyltransferase 1 (DGAT1), which catalyzes the final reaction of triglyceride synthesis, confers dramatic resistance to high-fat diet induc
Externí odkaz:
https://doaj.org/article/5661590c2bdc4b59b1a5d3906590a54f
Autor:
Qing Zhang, William J. Zavadoski, Robert J. Aiello, M.C. Holt, Nicole Barucci, Jim Valentine, A.J. Stein, Vishwas M. Paralkar, Stéphane De Lombaert, Daniel R. Goldberg, Patricia Bourassa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:413-419
As a follow-up to the discovery of our spirocyclic proline-based TPH1 inhibitor lead, we describe the optimization of this scaffold. Through a combination of X-ray co-crystal structure guided design and an in vivo screen, new substitutions in the lip
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d832bfe964546651027bc5ad2f1478f
https://doi.org/10.1016/j.bmcl.2016.12.053
https://doi.org/10.1016/j.bmcl.2016.12.053
Autor:
Nicole Barucci, Stéphane De Lombaert, Vishwas M. Paralkar, Jim Valentine, William J. Zavadoski, Patricia Bourassa, Robert J. Aiello, A.J. Stein, Daniel R. Goldberg, Qing Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2855-2860
An increasing number of diseases have been linked to a dysfunctional peripheral serotonin system. Given that tryptophan hydroxylase 1 (TPH1) is the rate limiting enzyme in the biosynthesis off serotonin, it represents an attractive target to regulate
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb1fd6da7a2d3eccaf3ce69f8c5f867b
https://doi.org/10.1016/j.bmcl.2016.04.057
https://doi.org/10.1016/j.bmcl.2016.04.057
Autor:
Patricia Bourassa, Nicole Barucci, Stéphane De Lombaert, William J. Zavadoski, Daniel R. Goldberg, Qing Zhang, Robert J. Aiello, James J. Valentine, Vishwas M. Paralkar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1124-1129
The central role of the biogenic monoamine serotonin (5-hydroxytryptamine, 5-HT) as a neurotransmitter with important cognitive and behavioral functions is well known. However, 5-HT produced in the brain only accounts for approximately 5% of the tota
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74ee42e411b02d02f0ced871cd344fd2
https://doi.org/10.1016/j.bmcl.2016.01.064
https://doi.org/10.1016/j.bmcl.2016.01.064
Autor:
Tara B. Manion, Roberto A. Calle, Benjamin S. Maciejewski, Terrell A. Patterson, Thomas S. McDonald, Steven Watkins, Jennifer L. LaPerle, E. Michael Gibbs, Dawn Mather, Avijit Ghosh, Danny Chen, William J. Zavadoski, Claire M. Steppan, Maya Hanna
Publikováno v:
American Journal of Physiology-Gastrointestinal and Liver Physiology. 304:G958-G969
Alterations in fat metabolism, in particular elevated plasma concentrations of free fatty acids and triglycerides (TG), have been implicated in the pathogenesis of Type 2 diabetes, obesity, and cardiovascular disease. Acyl-CoA:diacylglycerol acyltran
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58851d26674ed39fe0b3016d639d84b4
https://doi.org/10.1152/ajpgi.00384.2012
https://doi.org/10.1152/ajpgi.00384.2012
Autor:
Jing Chen, Spiros Liras, Manthena V.S. Varma, Judith L. Treadway, Martha L. Minich, Laurel Sweet, John D. Knafels, Karen Atkinson, Nahor Haddish-Berhane, Angel Guzman-Perez, Benjamin D. Stevens, Alan Robertson, Sharad B. Murdande, David B. Duignan, Mark Ammirati, Timothy P. Rolph, William J. Zavadoski, Christopher S. Jones, Patricia Bourassa, Jeffrey A. Pfefferkorn, John Litchfield, Lili Yao, Kevin J. Filipski, Margit MacDougall, Levenia Baker, John C. Pettersen, Theresa D’Aquila, Ayman El-Kattan, Bo Feng, Francis Bourbonais, Meihua Tu, Robert J. Aiello, Gary Erik Aspnes, Jianwei Bian, David R. Derksen, Paul DaSilva-Jardine, Beijing Tan, James A. Landro, Over Cabrera, Rachel E. Kosa, Hud Lawrence Risley, Shenping Liu, Amanda L. Lapworth, Nicole Barucci
Publikováno v:
Journal of Medicinal Chemistry. 55:1318-1333
Glucokinase is a key regulator of glucose homeostasis, and small molecule allosteric activators of this enzyme represent a promising opportunity for the treatment of type 2 diabetes. Systemically acting glucokinase activators (liver and pancreas) hav
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa4c2ff700899b62627c8e68d3696bfd
https://doi.org/10.1021/jm2014887
https://doi.org/10.1021/jm2014887
Autor:
J. Kyle Krady, Rashmi Kumari, Shyama D. Patel, Susan J. Vannucci, Lisa B. Willing, William J. Zavadoski, E. Michael Gibbs, Ian A. Simpson
Publikováno v:
Journal of Cerebral Blood Flow & Metabolism. 30:352-360
Diabetes is an increased risk factor for stroke and results in increased brain damage in experimental animals and humans. The precise mechanisms are unclear, but our earlier studies in the db/db mice suggested that the cerebral inflammatory response
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0806597049bb7af7e4531ebc89b378b
https://doi.org/10.1038/jcbfm.2009.221
https://doi.org/10.1038/jcbfm.2009.221
Autor:
Michael Scott Visser, Michael P. DeNinno, Melissa P. Andrews, Andrew Simon Bell, Michael John Palmer, Nan Eshelby, Cynthia Eller-Zarbo, John B. Etienne, Yue Chen, E. Michael Gibbs, William J. Zavadoski, Li J. Yu, Dianna E. Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2537-2541
Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these too
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90579384bdc00653d5f3b8ed65d6fc3e
https://doi.org/10.1016/j.bmcl.2009.03.024
https://doi.org/10.1016/j.bmcl.2009.03.024
Autor:
William J. Zavadoski, Daniel R. Goldberg, Patricia-Ann Bourassa, Nicole Barucci, Stéphane De Lombaert, Qing Zhang, Robert J. Aiello, Jeffrey Dubins, Vishwas Paralkar
Publikováno v:
4.3 Pulmonary Circulation and Pulmonary Vascular Disease.
Pulmonary arterial hypertension (PAH) is a progressive disease defined by an elevation in pulmonary arterial pressure with extensive pulmonary vascular remodeling and perivascular mast cell accumulation. While the exact etiology of the disease is unk
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fb928e7ba61ce63c065b799da12796f4
https://doi.org/10.1183/13993003.congress-2015.pa4909
https://doi.org/10.1183/13993003.congress-2015.pa4909
Autor:
David E. Johnson, E. Michael Gibbs, William J. Zavadoski, Karen L. Houseknecht, Hans Rollema, Alan Robertson
Publikováno v:
Neuropsychopharmacology. 32:289-297
Although it is generally accepted that atypical antipsychotics differ in their risk for diabetic side effects, the underlying pharmacological mechanisms are unknown. Studies on the mechanisms of antipsychotic-induced hyperglycemia or insulin resistan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d5b39718f8a2dd96e8dc8e9b7cf928b
https://doi.org/10.1038/sj.npp.1301209
https://doi.org/10.1038/sj.npp.1301209