Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Stanley Wertheimer"'
Autor:
Rebecca Taub, Weiya Yun, Toni Whittard, David Robert Bolin, Yimin Qian, Shiming Li, Paul Gillespie, Sonja Kazmer, Yingsi Chen, Mushtaq Ahmad, Stanley Wertheimer, Karin Conde-Knape
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7205-7209
In a discovery effort to find safe and effective DGAT-1 inhibitors, we have identified 2-phenyloxazole 4-carboxamide 1 as a conformationally constrained analog of a hydrazide hit, which was previously identified from high-throughput screening. Furthe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22686f43ba28ecf4b6fd5f817ee02e70
https://doi.org/10.1016/j.bmcl.2011.09.039
https://doi.org/10.1016/j.bmcl.2011.09.039
Autor:
Stanley Wertheimer, Lee Apostle Mcdermott, Stuart Hayden, Weiya Yun, Yingsi Chen, Anjula Pamidimukkala, Rebecca Taub, Kuo-Sen Huang, Toni Whittard, Liang Guo, Shiming Li, Jenny Tan, Fariborz Firooznia, Adrian Wai-Hing Cheung, David Robert Bolin, Nicholas Marcopulos, Yimin Qian, Karin Conde-Knape, Mushtaq Ahmad, Gwendolyn Ramsey, Cristina M. Rondinone, Jefferson Wright Tilley, Matthew Michael Hamilton
Publikováno v:
Journal of Medicinal Chemistry. 54:2433-2446
Diacylglycerol acyltransferase-1 (DGAT-1) is the enzyme that catalyzes the final and committed step of triglyceride formation, namely, the acylation of diacylglycerol with acyl coenzyme A. DGAT-1 deficient mice demonstrate resistance to weight gain o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afd3abbb050006099c5ec3cd2f890db3
https://doi.org/10.1021/jm101580m
https://doi.org/10.1021/jm101580m
Autor:
Rebecca Taub, David Robert Bolin, Shawn David Erickson, Charles Belunis, Stanley Wertheimer, Cristina M. Rondinone, Anish Konkar, Karin Conde-Knape
Publikováno v:
Drug Discovery Today: Therapeutic Strategies. 4:129-135
Body weight is determined by the net difference in calorie consumption and energy expenditure. The balance between triglyceride biosynthesis and breakdown processes in the body determines the amount of total fat mass in an individual. Positive energy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2a914abe45c1e5047d0e0f9eeb39f17e
https://doi.org/10.1016/j.ddstr.2007.10.002
https://doi.org/10.1016/j.ddstr.2007.10.002
Autor:
Kurt Hollfelder, Charles Belunis, Robert Crowther, Pete William Dunten, David J. Weber, Ursula Kammlott, Wayne Levin, Hanspeter Michel, Gwendolyn Ramsey, Amy Swain, Stanley Wertheimer
Publikováno v:
Journal of Molecular Biology. 316:257-264
We report crystal structures of the human enzyme phosphoenolpyruvate carboxykinase (PEPCK) with and without bound substrates. These structures are the first to be determined for a GTP-dependent PEPCK, and provide the first view of a novel GTP-binding
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b36444f143990f5f5c3214390f6d95e6
https://doi.org/10.1006/jmbi.2001.5364
https://doi.org/10.1006/jmbi.2001.5364
Autor:
Douglas W. Morgan, Wayne Levin, Keren I. Hulkower, David L. DeWitt, Ting Chen, John W. Coffey, Stanley Wertheimer, William C. Hope, Robert M. Crowl, Celia M. Anderson
Publikováno v:
Arthritis & Rheumatism. 37:653-661
Objective In order to investigate potential regulatory mechanisms for the increased production of prostaglandin E2 (PGE2) in interleukin-1 beta (IL-1 beta)-stimulated rheumatoid synovial fibroblasts (RSF), this study examined the induction of phospho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5f61ff21d2e8971ce4a3737c392625d7
https://doi.org/10.1002/art.1780370508
https://doi.org/10.1002/art.1780370508
Autor:
Sherrie L. Pietranico, Ping Wang, Nicholas John Silvester Huby, Mary-Lou Gubler, Louise H. Foley, Weiya Yun, John Vermeulen, Stanley Wertheimer, Gwendolyn Ramsey, Pete William Dunten, Katherine Toth
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(14)
New modifications on the C-8 4-aminobenzyl unit of the previously reported 3-alkyl-1,8-dibenzylxanthine inhibitors of cPEPCK are presented. The most active compound reported here is the 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid amide derivati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f839692387a725882496d7a69df64713
https://pubmed.ncbi.nlm.nih.gov/17532214
https://pubmed.ncbi.nlm.nih.gov/17532214
Autor:
Stanley Wertheimer, Pete William Dunten, Mary-Lou Gubler, Ping Wang, Louise H. Foley, Gwendolyn Ramsey
Publikováno v:
ChemInform. 35
The analysis of the X-ray structures of two xanthine inhibitors bound to PEPCK and a comparison to the X-ray structure of GTP bound to PEPCK are reported. The SAR at N-1, N-7 and developing SAR at C-8 are consistent with information gained from the X
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a87a41edb840598dbd78d54413981f5
https://doi.org/10.1002/chin.200403146
https://doi.org/10.1002/chin.200403146
Autor:
Pete William Dunten, Mary-Lou Gubler, Gwendolyn Ramsey, Louise H. Foley, Ping Wang, Stanley Wertheimer
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(20)
The first non-substrate like inhibitors of human cytosolic phosphoenolpyruvate carboxykinase (PEPCK) competitive with GTP are reported. An effort to discover orally active compounds that improve glucose homeostasis in Type 2 diabetics by reversibly i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f642580914741ff6e2fa60fae2a9344
https://pubmed.ncbi.nlm.nih.gov/14505680
https://pubmed.ncbi.nlm.nih.gov/14505680
Autor:
Stanley Wertheimer, Paul Burn, Chung H. Lin, Michael J. Quon, Kurt Amrein, Hui Chen, Susan L. Katz
Publikováno v:
The Journal of biological chemistry. 272(12)
The protein-tyrosine phosphatases PTP1B and Syp have both been implicated as modulators of the mitogenic actions of insulin. However, the roles of these protein-tyrosine phosphatases in the metabolic actions of insulin are not well characterized. In
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80cee0acae8d30a7dcf70bebdcc0fcef
https://pubmed.ncbi.nlm.nih.gov/9065475
https://pubmed.ncbi.nlm.nih.gov/9065475
Publikováno v:
Inflammation research : official journal of the European Histamine Research Society ... [et al.]. 44
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d346196e432653a58a9d3a561a288af0
https://pubmed.ncbi.nlm.nih.gov/8548357
https://pubmed.ncbi.nlm.nih.gov/8548357