Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Scott C. Potter"'
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:
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:
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:
Handbook of experimental pharmacology. (203)
Fructose-1,6-bisphosphatase (FBPase), a rate-controlling enzyme of gluconeogenesis, has emerged as an important target for the treatment of type 2 diabetes due to the well-recognized role of excessive endogenous glucose production (EGP) in the hyperg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::386a75c2fc230d4475b6fda8332faad7
https://pubmed.ncbi.nlm.nih.gov/21484576
https://pubmed.ncbi.nlm.nih.gov/21484576
Publikováno v:
Diabetes-Perspectives in Drug Therapy ISBN: 9783642172137
Fructose-1,6-bisphosphatase (FBPase), a rate-controlling enzyme of gluconeogenesis, has emerged as an important target for the treatment of type 2 diabetes due to the well-recognized role of excessive endogenous glucose production (EGP) in the hyperg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c7fb309ffac7a3b3eab1aa015bc5d895
https://doi.org/10.1007/978-3-642-17214-4_12
https://doi.org/10.1007/978-3-642-17214-4_12
Autor:
Jay DaRe, Tao Jiang, Scott C. Potter, Tony Gibson, Qun Dang, Frank Taplin, Yan Liu, Mark D. Erion, Daniel K. Cashion, Haiqing Li, Zhili Sun, Jason D. Jacintho, Paul D. van Poelje, Srinivas Rao Kasibhatla, Yi Fan, Lemus Robert Huerta, Feng Tian, Wenyu Li
Publikováno v:
Journal of medicinal chemistry. 54(1)
Oral delivery of previously disclosed purine and benzimidazole fructose-1,6-bisphosphatase (FBPase) inhibitors via prodrugs failed, which was likely due to their high molecular weight (>600). Therefore, a smaller scaffold was desired, and a series of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7227453a1b09fd9029c96cde2a01f99
https://pubmed.ncbi.nlm.nih.gov/21126019
https://pubmed.ncbi.nlm.nih.gov/21126019
Autor:
M. Rami Reddy, Paul D. van Poelje, Srinivas Rao Kasibthatla, Tony Gibson, Qun Dang, Scott C. Potter, Frank Taplin, Mark D. Erion, Tao Jiang, K. Raja Reddy
Publikováno v:
Journal of Diabetes & Metabolism.
To discover an alternative series of fructose 1,6-bisphosphatase (FBPase) inhibitors that is suitable for oral delivery via prodrugs, the 4-amino group was removed from the initial 4-aminobenzimidazole lead series, since the number of hydrogen bond d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fddc0fae1017c6af81721bcf2583d864
https://doi.org/10.4172/2155-6156.1000105
https://doi.org/10.4172/2155-6156.1000105
Autor:
Mark D. Erion, Paul D. van Poelje, Qun Dang, Bernard R. Landau, Scott C. Potter, Visvanathan Chandramouli
Publikováno v:
Diabetes. 55(6)
Gluconeogenesis is increased in type 2 diabetes and contributes significantly to fasting and postprandial hyperglycemia. We recently reported the discovery of the first potent and selective inhibitors of fructose 1,6-bisphosphatase (FBPase), a rate-c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ffecd56755d52ec040b48c031252053c
https://pubmed.ncbi.nlm.nih.gov/16731838
https://pubmed.ncbi.nlm.nih.gov/16731838