Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Srinivas Rao Kasibhatla"'
Autor:
Victor Hong, Andres McKenzie, Jianhua Chao, Erin K Harning, Ping Li, Francis Burrows, Jiandong Shi, Rachel Lough, Theodore J. Yun, Marcus F. Boehm, Gerardo Ibanez, Ryan Lamer, Kenneth W Weichert, Christina Boykin, Anthone W. Dunah, Istvan J. Enyedy, Christine Ambrose, Noelito Timple, Ryan Van de Water, Marilyn R. Kehry, Marco A. Biamonte, Joseph Arndt, Jeffrey Thompson, Srinivas Rao Kasibhatla, Cristina M Sandoval, Karen Lundgren, Kevin Hong, Pamela A. Snodgrass-Belt, Sarah A. Bixler
Publikováno v:
Journal of Medicinal Chemistry. 55:7786-7795
Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol (EC144), is a second generation inhibitor of heat shock protein 90 (Hsp90) and is substantially more potent in vitro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11fc27a2a6949bbbf83404c803f06d5a
https://doi.org/10.1021/jm300810x
https://doi.org/10.1021/jm300810x
Autor:
Andres McKenzie, Noel Timple, Jessica Friedman, Marcus F. Boehm, Karen Lundgren, Robert Scannevin, Kevin Hong, John Brekken, Adeela Kamal, Francis Burrows, Yong-Ching Yang, John Sensintaffar, David J. Busch, Nanni Huser, Srinivas Rao Kasibhatla, Rachel Powell, Hong Zhang, Laura Neely
Publikováno v:
Molecular Cancer Therapeutics. 8:921-929
Inhibition of heat shock protein 90 (Hsp90) results in the degradation of oncoproteins that drive malignant progression, inducing cell death, making Hsp90 a target of substantial interest for cancer therapy. BIIB021 is a novel, fully synthetic inhibi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0721b242868c8c12d8116c9dd480a53
https://doi.org/10.1158/1535-7163.mct-08-0758
https://doi.org/10.1158/1535-7163.mct-08-0758
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:
Karen Lundgren, Roy Grecko, Srinivas Rao Kasibhatla, Kevin Hong, Adeela Kamal, Rachel Lough, Gregg Timony, Lawrence C. Fritz, Edgar H. Ulm, Marco A. Biamonte, Patricia Karjian, David J. Busch, Marcus F. Boehm, Robert K. Mansfield, Francis Burrows, John Brekken, Yingqing Ran, John Sensintaffar
Publikováno v:
Journal of Medicinal Chemistry. 50:2767-2778
Heat shock protein 90 (Hsp90) is a molecular chaperone protein implicated in stabilizing the conformation and maintaining the function of many cell-signaling proteins. Many oncogenic proteins are more dependent on Hsp90 in maintaining their conformat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::256512d0ba0657d93f9e55a9f6d48e83
https://doi.org/10.1021/jm050752+
https://doi.org/10.1021/jm050752+
Autor:
Kevin Hong, Adeela Kamal, Yingqing Ran, Jiandong Shi, Marcus F. Boehm, Karen Lundgren, Gregg Timony, Khang Vu, Edgar H. Ulm, Francis Burrows, Roy Grecko, Rachel Lough, Srinivas Rao Kasibhatla, John Sensintaffar, David J. Busch, Jean-Yves Le Brazidec, Marco A. Biamonte, Robert K. Mansfield, Junhua Fan, Lin Zhang
Publikováno v:
Journal of Medicinal Chemistry. 49:5352-5362
We report on the discovery of benzo- and pyridino- thiazolothiopurines as potent heat shock protein 90 inhibitors. The benzothiazole moiety is exceptionally sensitive to substitutions on the aromatic ring with a 7'-substituent essential for activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a30163f614c02b6f0a966897c679719
https://doi.org/10.1021/jm051146h
https://doi.org/10.1021/jm051146h
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
Autor:
Leonard Petrucelli, Christopher B. Eckman, Francis Burrows, Srinivas Rao Kasibhatla, Adeela Kamal, Jason L. Eriksen, Chad A. Dickey, Mike Hutton
Publikováno v:
Current Alzheimer Research. 2:231-238
Therapeutic development for Alzheimer's disease has largely focused on the removal of beta amyloid because of its suggested role in the primary agent in initiating the disease process. However, with the recent discovery of mutations that result as pa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78a39e8ba71fa09c5695277e9029bf99
https://doi.org/10.2174/1567205053585927
https://doi.org/10.2174/1567205053585927
Publikováno v:
Journal of Medicinal Chemistry. 43:1508-1518
N3-Substituted coformycin aglycon analogues with improved AMP deaminase (AMPDA) inhibitory potency are described. Replacement of the 5-carboxypentyl substituent in the lead AMPDA inhibitor 3-(5-carboxypentyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1, 3]dia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e762cc47a37c1534e2a6bb2d0f391a90
https://doi.org/10.1021/jm990448e
https://doi.org/10.1021/jm990448e
Publikováno v:
Journal of Medicinal Chemistry. 43:1519-1524
AMP deaminase (AMPDA) inhibitors increase the levels of extracellular adenosine and preserve intracellular adenylate pools in cellular models of ATP depletion and therefore represent a potential new class of antiischemic drugs. Recently we reported t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43e20cee8e6518c40207c3b1e9dd5408
https://doi.org/10.1021/jm9905413
https://doi.org/10.1021/jm9905413