Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Paul D. van Poelje"'
Autor:
Scott C. Potter, Srinivas Rao Kasibthatla, Qun Dang, Frank Taplin, Paul D. van Poelje, Tony Gibson, Mark D. Erion, Tao Jiang
Publikováno v:
MedChemComm. 2:287-290
To discover an alternative heterocyclic scaffold to the thiazole series of FBPase inhibitors such as thiazole 1, oxazoles were investigated to see if replacing the sulfur of the thiazole scaffold with an oxygen is tolerated. Numerous oxazoles with a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e742e99d9c44f6af40d2d3fe13f63937
https://doi.org/10.1039/c0md00269k
https://doi.org/10.1039/c0md00269k
Autor:
Jay DaRe, Qun Dang, Mark D. Erion, Tony Gibson, Frank Taplin, Paul D. van Poelje, Yan Liu, Scott C. Potter, Srinivras Rao Kasibhatla, K. Raja Reddy, Wei Xiao, Gerard R. Scarlato
Publikováno v:
Journal of Medicinal Chemistry. 53:441-451
Efforts to enhance the inhibitory potency of the initial purine series of fructose-1,6-bisphosphatase (FBPase) inhibitors led to the discovery of a series of benzimidazole analogues with human FBPase IC(50)s < 100 nM. Inhibitor 4.4 emerged as a lead
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99b77507b9a9519ff4310d803b2ebc1e
https://doi.org/10.1021/jm901420x
https://doi.org/10.1021/jm901420x
Autor:
David L. Linemeyer, Paul D. van Poelje, Mark D. Erion, Edward Earl Cable, Jinzhao Hou, Patricia D. Finn, Bruce R. Ito, Jeffrey W. Stebbins
Publikováno v:
Hepatology. 49:407-417
Non-alcoholic fatty liver disease (NAFLD) is one of the most common forms of chronic liver disease, with a prevalence ranging from 10% to 30%. The use of thyroid hormone receptor (TR) agonists for the treatment of NAFLD has not been considered viable
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::813d05dc2619242a025aab802824ecc2
https://doi.org/10.1002/hep.22572
https://doi.org/10.1002/hep.22572
Autor:
Tao Jiang, James M. Fujitaki, Daniel K. Cashion, Srinivas Rao Kasibhatla, Yan Liu, K. Raja Reddy, Paul D. van Poelje, Scott C. Potter, Frank Taplin, William G. Schulz, Kevin Fan, Mark D. Erion, Qun Dang
Publikováno v:
Journal of Medicinal Chemistry. 51:4331-4339
Like most phosphonic acids, the recently discovered potent and selective thiazole phosphonic acid inhibitors of fructose 1,6-bisphosphatase (FBPase) exhibited low oral bioavailability (OBAV) and therefore required a prodrug to achieve oral efficacy.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65bfa7ac815f2145b3a778cc523215b4
https://doi.org/10.1021/jm8001235
https://doi.org/10.1021/jm8001235
Autor:
K. Raja Reddy, William N. Lipscomb, James M. Fujitaki, Paul D van Poelje, Srinivas Rao Kasibhatla, Tao Jiang, M. Rami Reddy, Mark D. Erion, Qun Dang, Jingwei Huang, Scott C. Potter
Publikováno v:
Journal of the American Chemical Society. 129:15491-15502
Excessive glucose production by the liver coupled with decreased glucose uptake and metabolism by muscle, fat, and liver results in chronically elevated blood glucose levels in patients with type 2 diabetes. Efforts to treat diabetes by reducing gluc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9550cb46797aacd0fe0b27fb174332eb
https://doi.org/10.1021/ja074871l
https://doi.org/10.1021/ja074871l
Autor:
David L. Linemeyer, M Venkat Reddy, Zhili Sun, James M. Fujitaki, David B. Olsen, Mark D. Erion, Serge H. Boyer, Vaibhav Varkhedkar, Kenneth A Koeplinger, Scott J. Hecker, Paul D. van Poelje, K. Raja Reddy, Malcolm Maccoss, Wenjian Huang
Publikováno v:
Journal of Medicinal Chemistry. 50:3891-3896
2'-C-Methyladenosine exhibits impressive inhibitory activity in the cell-based hepatitis C virus (HCV) subgenomic replicon assay, by virtue of intracellular conversion to the corresponding nucleoside triphosphate (NTP) and inhibition of NS5B RNA-depe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3442373ea071165cee52331065dafc15
https://doi.org/10.1021/jm0701021
https://doi.org/10.1021/jm0701021
Publikováno v:
Drug Discovery Today: Therapeutic Strategies. 4:103-109
Overproduction of glucose by gluconeogenesis is a primary determinant of hyperglycemia in patients with type 2 diabetes. Current drugs neither inhibit glucose production directly nor provide adequate glycemic control. As reviewed herein, the recent d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cd2b59766a73b29b42279487a6800e61
https://doi.org/10.1016/j.ddstr.2007.10.003
https://doi.org/10.1016/j.ddstr.2007.10.003
Bis[(para-methoxy)benzyl] phosphonate prodrugs with improved stability and enhanced cell penetration
Autor:
Timothy J. Colby, Yan Liu, Mark D. Erion, Qun Dang, Paul D. van Poelje, Robert M. Rydzewski, Brian S. Brown, Edward D. Robinson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3412-3416
A series of substituted bis[(para-methoxy)benzyl] (bisPMB) esters of 1-naphthalenemethylphosphonate (NMPA) were synthesized and evaluated as phosphonate prodrugs. BisPMB NMPA esters (4b and 4c) with significantly improved aqueous stability were ident
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3005935488121415882f1eb59b3b0868
https://doi.org/10.1016/j.bmcl.2007.03.089
https://doi.org/10.1016/j.bmcl.2007.03.089
Autor:
Qun Dang, William N. Lipscomb, Tao Jiang, Mark D. Erion, K. Raja Reddy, M. Rami Reddy, Paul D. van Poelje, Srinivas Rao Kasibhatla, Scott C. Potter
Publikováno v:
Proceedings of the National Academy of Sciences. 102:7970-7975
In type 2 diabetes, the liver produces excessive amounts of glucose through the gluconeogenesis (GNG) pathway and consequently is partly responsible for the elevated glucose levels characteristic of the disease. In an effort to find safe and efficaci
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e5273bc5549b2f4b7a4b3b8e98882cd
https://doi.org/10.1073/pnas.0502983102
https://doi.org/10.1073/pnas.0502983102
Publikováno v:
Biochemical and Biophysical Research Communications. 283:417-422
Five distinct organic anion transporter cDNAs, hOAT1-5, were isolated from human liver and kidney. hOAT1, 2, and 3 are homologous to their respective rat orthologues OAT1-3, whereas hOAT4 and 5 are novel clones that have not been identified in other
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::354f918e9dad47f31715f47e3919a7f9
https://doi.org/10.1006/bbrc.2001.4774
https://doi.org/10.1006/bbrc.2001.4774