Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Karen L. MacNaul"'
Autor:
Neelam Sharma, Weiguo Liu, Nancy S. Hayes, Steve Chen, Melba Hernandez, John G. Menke, Carl P. Sparrow, Michael Robins, James F. Dropinski, Michael J. Szymonifka, Lawrence F. Colwell, Sheo B. Singh, Charlotte Burton, Karen L. MacNaul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4574-4578
A series of podocarpic acid amides were identified as potent agonists for Liver X receptor alpha and beta subtypes, which are members of a nuclear hormone receptor superfamily that are involved in the regulation of a variety of metabolic pathways inc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d98d886c2edbeb4cb3dc478b4f411a44
https://doi.org/10.1016/j.bmcl.2005.06.100
https://doi.org/10.1016/j.bmcl.2005.06.100
Autor:
Hiranthi Jayasuriya, Anne W. Dombrowski, Ziqiang Guan, John G. Ondeyka, Marvin D. Schulman, Sheo B. Singh, John G. Menke, Christine McCallum, Kithsiri Herath, Soojin S Kwon, Karen L. MacNaul, Javier Collado, Nancy S. Hayes, Neelam Sharma
Publikováno v:
The Journal of Antibiotics. 58:559-565
Cholesterol homeostasis is tightly controlled process that involves a variety of regulators including liver X receptors (LXR). Agonists of LXR are expected to increase cholesterol efflux, lower LDL, and raise HDL levels. Screening of a natural produc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::493a7fb7e07656b92b6387e04c54f8c8
https://doi.org/10.1038/ja.2005.76
https://doi.org/10.1038/ja.2005.76
Autor:
Conrad Santini, Joel P. Berger, Guo Q. Shi, James V. Heck, Melba Hernandez, Raul F. Alvaro, Yong Zhang, Arun K. Agrawal, Soumya P. Sahoo, James F. Dropinski, Samuel D. Wright, Tian-Quan Cai, Gaochao Zhou, Peter T. Meinke, David E. Moller, Karen L. MacNaul
Publikováno v:
Journal of Medicinal Chemistry. 48:5589-5599
The design and synthesis of a novel class of 2,3-dihydrobenzofuran-2-carboxylic acids as highly potent and subtype-selective PPARalpha agonists are reported. Systematic study of structure-activity relationships has identified several key structural e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7db937b8b54d80c244416af2a1c1285
https://doi.org/10.1021/jm050373g
https://doi.org/10.1021/jm050373g
Autor:
Soumya P. Sahoo, Samuel D. Wright, David E. Moller, Julia K. Boueres, Karen L. MacNaul, Marc C. Ippolito, Joel P. Berger, Arun K. Agrawal, Daniel J. Miller, Pei-Ran Wang, Hiroo Koyama
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3347-3351
A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARα agonisim. As a result, highly potent, and selective PPARα agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in ha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3db3e18a696be690baf72057ee41674b
https://doi.org/10.1016/j.bmcl.2005.05.028
https://doi.org/10.1016/j.bmcl.2005.05.028
Autor:
Joanne Baffic, Yu-Sheng Chao, A. Brian Jones, Weiguo Liu, Steve Chen, John G. Menke, Carl P. Sparrow, Melba Hernandez, Sherrie X McCormick, Xiaohua Li, Aileen Bouffard, Tom S. Chen, John G. Ondeyka, James F. Dropinski, Jianhua Wang, Neelam Sharma, Sheo B. Singh, Karen L. MacNaul, Charlotte Burton, Nancy S. Hayes, My-Hanh Lam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2824-2828
Liver X receptors are nuclear receptors that regulate metabolism of cholesterol. They are activated by oxysterols resulting in increased transcription of the ABCA1 gene, promoting cholesterol efflux and HDL formation. We have identified podocarpic ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e91291554a85a4cdd26920f44ff0310f
https://doi.org/10.1016/j.bmcl.2005.03.100
https://doi.org/10.1016/j.bmcl.2005.03.100
Autor:
Arun K. Agrawal, Thomas W. Doebber, Pei-Ran Wang, Daniel J. Miller, James V. Heck, Julia K. Boueres, Marc C. Ippolito, Soumya P. Sahoo, Linda J. Kelly, Samuel D. Wright, Yu-Sheng Chao, Hiroo Koyama, A. Brian Jones, Gaochao Zhou, Joel P. Berger, David E. Moller, Ronald B. Franklin, Karen L. MacNaul, Ranjit C. Desai, Margaret Wu
Publikováno v:
Journal of Medicinal Chemistry. 47:3255-3263
A series of chromane-2-carboxylic acid derivatives was synthesized and evaluated for PPAR agonist activities. A structure-activity relationship was developed toward PPARalpha/gamma dual agonism. As a result, (2R)-7-(3-[2-chloro-4-(4-fluorophenoxy)phe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2f8f7be20ef0493afda0cab77841421
https://doi.org/10.1021/jm030621d
https://doi.org/10.1021/jm030621d
Autor:
Joel P. Berger, Melba Hernandez, Wei Han, Carl P. Sparrow, Chhabi Biswas, Joanne Baffic, James V. Heck, Pei-Ran Wang, Samuel D. Wright, Gaochao Zhou, Yu-Sheng Chao, Qiu Guo, David E. Moller, Karen L. MacNaul, Denise P. Milot, Ranjit C. Desai, Neelam Sharma, Soumya P. Sahoo, Marc C. Ippolito, My-Hanh Lam, Linda J. Kelly, Margaret Wu, Thomas W. Doebber
Publikováno v:
Endocrinology. 145:1640-1648
Patients with type 2 diabetes mellitus exhibit hyperglycemia and dyslipidemia as well as a markedly increased incidence of atherosclerotic cardiovascular disease. Here we report the characterization of a novel arylthiazolidinedione capable of lowerin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::175dcc68b6952d7d3f93601399fd22f8
https://doi.org/10.1210/en.2003-1270
https://doi.org/10.1210/en.2003-1270
Autor:
Michael J. Forrest, Zao Hu, Roger Meurer, Alan D. Adams, Alex Elbrecht, Thomas W. Doebber, Joel P. Berger, Derek Von Langen, Adonis Dadiz, A. Brian Jones, David E. Moller, Karen L. MacNaul, Gaochao Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3185-3190
A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARα-weighted agonists do not show the typical PPARγ associated side effects of BAT proliferation and cardiac hypertro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f27d9bf40d7785a422d3d9005c964c77
https://doi.org/10.1016/s0960-894x(03)00702-9
https://doi.org/10.1016/s0960-894x(03)00702-9
Autor:
Dominick F. Gratale, James V. Heck, David E. Moller, Karen L. MacNaul, Hiroo Koyama, Edward Metzger, Soumya P. Sahoo, Victoria K. Lombardo, Ronald B. Franklin, Thomas W. Doebber, Wei Han, Joel P. Berger, Ranjit C. Desai, Kwan Leung
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3541-3544
A series of novel aryloxazolidine-2,4-diones was synthesized. A structure–activity relationship study of these compounds led to the identification of potent, orally active PPAR dual α/γ agonists. Based on the results of efficacy studies in the db
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f648cc526319a858cb2f0fdb3f282753
https://doi.org/10.1016/s0960-894x(03)00785-6
https://doi.org/10.1016/s0960-894x(03)00785-6
Autor:
John Ventre, Mona Parikh, Thomas W. Doebber, Bruce A. Johnson, Ann Petro, Gaochao Zhou, Joel Berger, Bei B. Zhang, Linda J. Kelly, Neelam Sharma, Michael R. Tanen, Alan D. Adams, Chhabi Biswas, Ralph T. Mosley, Richard S. Surwit, Alex Elbrecht, G. Marie Thompson, David E. Moller, Karen L. MacNaul, Karen Richards
Publikováno v:
Molecular Endocrinology. 17:662-676
Antidiabetic thiazolidinediones (TZDs) and non-TZD compounds have been shown to serve as agonists of the peroxisome proliferator-activated receptor gamma (PPARgamma). Here, we report the identification and characterization of a novel non-TZD selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc313c36fc3c5d00f1f4f35a62207650
https://doi.org/10.1210/me.2002-0217
https://doi.org/10.1210/me.2002-0217