Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Fang-Tsao Hong"'
Autor:
Jude R. Canon, Ashley Callinan, Sarah Bradley, Laurie Wang, Mackenzie Kui, Ariel Wein, Gabriele Sulli, Peter Buchowiecki, Fang-Tsao Hong, Miles Kubota, Mary Walton, Victor J. Cee
Publikováno v:
Cancer Research. 83:LB318-LB318
Sumoylation is a reversible post-translational modification of proteins by small ubiquitin-like modifier (SUMO) that regulates protein function and contributes to cellular response to stress. Sumoylation is an essential pathway for all cells and is i
Autor:
Fang-Tsao Hong, Hongyan Li, Derek E. Piper, Leszek Poppe, Philip Wong, Todd Hager, Essa Hu, Jason Long, Jennifer Aral, Narender R. Gavva, Cen Xu, Les P. Miranda, Carl Davis, Dawn Zhu, Sonya G. Lehto, Licheng Shi, Kristin L. Andrews
Publikováno v:
Journal of Medicinal Chemistry. 64:3427-3438
Inhibition of the pituitary adenylate cyclase 1 receptor (PAC1R) is a novel mechanism that could be used for abortive treatment of acute migraine. Our research began with comparative analysis of known PAC1R ligand scaffolds, PACAP38 and Maxadilan, wh
Autor:
Michael D. Bartberger, Michael Croghan, Carolyn Moyer, David Lloyd, Rod Cupples, Seifu Tadesse, Nobuko Nishimura, Ke Kong, Gwyneth Van, Christopher H. Fotsch, Randall W. Hungate, David J. St. Jean, Kevin Yang, Kate Ashton, Mark H. Norman, Samer Chmait, Longbin Liu, Lewis D. Pennington, Fang-Tsao Hong, Matthew P. Bourbeau, Clarence Hale, Jiandong Zhang, Aaron C. Siegmund, Jie Chen, Christopher M. Tegley, Steven R. Jordan, Kristin L. Andrews, Klaus Michelsen, Guomin Yao, Glenn Sivits, Andreas Reichelt, Joan Helmering
Publikováno v:
Journal of Medicinal Chemistry. 58:9663-9679
The HTS-based discovery and structure-guided optimization of a novel series of GKRP-selective GK-GKRP disrupters are revealed. Diarylmethanesulfonamide hit 6 (hGK-hGKRP IC50 = 1.2 μM) was optimized to lead compound 32 (AMG-0696; hGK-hGKRP IC50 = 0.0
Autor:
Kevin Yang, Rod Cupples, Gwyneth Van, Nobuko Nishimura, Longbin Liu, David J. St. Jean, Clarence Hale, Glenn Sivits, Jie Chen, Nuria A. Tamayo, Steven R. Jordan, Fang-Tsao Hong, Mark H. Norman, Michael D. Bartberger, Yunxin Bo, Christopher H. Fotsch, Samer Chmait, Seifu Tadesse, David Lloyd
Publikováno v:
Journal of Medicinal Chemistry. 58:4462-4482
The glucokinase-glucokinase regulatory protein (GK-GKRP) complex plays an important role in controlling glucose homeostasis in the liver. We have recently disclosed a series of arylpiperazines as in vitro and in vivo disruptors of the GK-GKRP complex
Autor:
Fang-Tsao Hong, Jian Jiang, Brian A. Lanman, Victor J. Cee, Liping H. Pettus, Paul E. Hughes, Nancy Zhang, Douglas A. Whittington, Tisha San Miguel, Anthony B. Reed, Ling Wang, Erin L. Mullady, Kristin L. Andrews, John D. McCarter, Andrew Tasker, Leeanne Zalameda, Mark H. Norman, Tian Wu, Ryan Wurz, Raju Subramanian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5630-5634
Replacement of the piperazine sulfonamide portion of the PI3Kα inhibitor AMG 511 (1) with a range of aliphatic alcohols led to the identification of a truncated gem-dimethylbenzylic alcohol analog, 2-(5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-((5-fl
Autor:
Bradley J. Herberich, Tian Wu, Paul E. Hughes, Claire L. M. Jackson, Nobuko Nishimura, Nancy Zhang, Ryan Wurz, Douglas A. Whittington, Shon Booker, Sean Caenepeel, Tisha San Miguel, Jian Jiang, Anthony B. Reed, Adrian L. Smith, Seifu Tadesse, Brian A. Lanman, Andrew Tasker, Erin L. Mullady, John D. McCarter, Fang-Tsao Hong, Liping H. Pettus, Divesh Aidasani, Victor J. Cee, Ling Wang, Bin Wu, Mark H. Norman, Daniel J. Freeman, Kevin Yang, Longbin Liu, Leeanne Zalameda, Yunxin Y. Bo, Xiaochun Zhu, Kristin L. Andrews, Markian Stec, Nuria A. Tamayo, Raju Subramanian, Noel D'angelo
Publikováno v:
Journal of Medicinal Chemistry. 55:7796-7816
The phosphoinositide 3-kinase family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger which plays a critical role in important cellular functions such as metabolis
Autor:
Yunxin Y. Bo, Leeanne Zalameda, Kevin Yang, Fang-Tsao Hong, Longbin Liu, Anthony B. Reed, Kristin L. Andrews, Tisha San Miguel, Brian A. Lanman, Paul E. Hughes, Noel D'angelo, Brad Herberich, Jian Jiang, Victor J. Cee, Claire L. M. Jackson, Ryan Wurz, Nobuko Nishimura, Raju Subramanian, Seifu Tadesse, Nancy Zhang, John D. McCarter, Daniel J. Freeman, Ling Wang, Nuria A. Tamayo, Erin L. Mullady, Mark H. Norman, Liping H. Pettus, Tian Wu, Douglas A. Whittington, Sean Caenepeel, Adrian L. Smith, Shon Booker
Publikováno v:
Journal of Medicinal Chemistry. 55:5188-5219
A highly selective series of inhibitors of the class I phosphatidylinositol 3-kinases (PI3Ks) has been designed and synthesized. Starting from the dual PI3K/mTOR inhibitor 5, a structure-based approach was used to improve potency and selectivity, res
Autor:
Fang-Tsao Hong, Christopher H. Fotsch, Xianghong Wang, Qingping Zeng, John G. Allen, G. Erich Wohlhieter, Chun Li, Yihong Zhou, Guomin Yao, Seifu Tadesse, Matthew P. Bourbeau, Chester Chenguang Yuan, Sekhar Surapaneni, Matthew R. Lee, Gary L. Skiles, Raju Subramanian, Xiaochun Zhu
Publikováno v:
Chemical Research in Toxicology. 23:653-663
A 2-aminothiazole derivative 1 was developed as a potential inhibitor of the oncology target AKT, a serine/threonine kinase. When incubated in rat and human liver microsomes in the presence of NADPH, 1 underwent significant metabolic activation on it
Autor:
Andrew Tasker, Pedro J. Beltran, Darren L. Reid, Robert Radinsky, Jian J. Chen, Dina A. Andrews, David J. St. Jean, Keegan Cooke, Ryan Wurz, Tian Wu, Nataraj Kalyanaraman, Essa Hu-Harrington, Faye Hsieh, Simon J. Hedley, Kristin L. Andrews, Brad Herberich, Nancy E. Everds, Seifu Tadesse, Michele Kubryk, Jinghui Zhan, Jason S. Tedrow, Kate Ashton, Petia Mitchell, Andrew T. Parsons, Roberto E. Guzman, Liping H. Pettus, James Brown, Dean Hickman, Tom Nguyen, Matthew S. Potter, Edward K. Lobenhofer, David Bauer, Fang-Tsao Hong, Oliver R. Thiel
Publikováno v:
ACS medicinal chemistry letters. 6(9)
In nonsmall cell lung cancer (NSCLC), the threonine(790)-methionine(790) (T790M) point mutation of EGFR kinase is one of the leading causes of acquired resistance to the first generation tyrosine kinase inhibitors (TKIs), such as gefitinib and erloti
Autor:
John E. Tellew, Fang-Tsao Hong, Larry E. Overman, Guillaume Bélanger, Bruce N. Rogers, William C. Trenkle
Publikováno v:
The Journal of Organic Chemistry. 67:7880-7883
The construction of triazacyclopenta[cd]pentalene diesters 6 by the reaction of dihydropyrrole alpha-ketoesters 3 with acylated hydrazines was evaluated further as a potential central strategic step in the total syntheses of complex guanidine alkaloi