Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Ann M. Janssen"'
Autor:
Jimmy Kong, Theunis C. Goosen, Kimberly O. Cameron, Samit Kumar Bhattacharya, Suvi T. M. Orr, Dilinie P. Fernando, Peter Cornelius, Eunsun Lee, Meihua Tu, Stefanus J. Steyn, David Austen Perry, Laura Michael, Jana Polivkova, Ann M. Janssen, Margaret Jackson, Jeffrey T. Kohrt, Ruduan Wang, Sylvie Perez, Hirokazu Ueno, Kimberly Lapham, Dawn Kelly-Sullivan, Victoria Bagdasarian, Roger Swartz, Ingrid A. Stock, Yingxin Zhang, Ryan Jones, Erasga Noe Ouano, Kim F. McClure, Wenhua Jiao, Daniel W. Kung, Guoqiang Wang, Hua Gao, Sam Varma
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5410-5414
The optimization for selectivity and central receptor occupancy for a series of spirocyclic azetidine-piperidine inverse agonists of the ghrelin receptor is described. Decreased mAChR muscarinic M2 binding was achieved by use of a chiral indane in pl
Autor:
Joseph S. Warmus, Markus Boehm, David W. Piotrowski, Terri Hinchey, Joanne Buxton, Janice E. Chin, Ann M. Janssen, Kentaro Futatsugi, Allyn T. Londregan, Philip A. Carpino, Nicole S. Roush
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1407-1411
Optimization of a high-throughput screening hit led to the discovery of a new series of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as highly potent agonists of TGR5. This novel chemotype was rapidly developed through iterative combinatorial li
Autor:
Martin B. Brenner, Joseph S. Warmus, Jeffrey S. Dubins, Liuqing Wei, Janice E. Chin, Nicole S. Roush, David Hepworth, Angela Wolford, Mei Li, Sophie Y. Lavergne, Sandra M. Jennings, Wenhua Jiao, Kevin B. Bahnck, Denise Gautreau, David W. Piotrowski, Joanne Buxton, John R. Hadcock, Matthew F. Sammons, Declan Flynn, Michael Herr, Benjamin D. Stevens, Steven B. Coffey, Kentaro Futatsugi, Michael John Munchhof, Jian Wang, Terri Hinchey, Suvi T. M. Orr, Gregory Storer, Angel Guzman-Perez, Bryan Li, Ann M. Janssen
Publikováno v:
MedChemComm. 4:205-210
Reported herein is a medicinal chemistry effort towards the identification of orally available TGR5 agonist 12, which served as a dog tool compound for studies to increase confidence in this mechanism. With the challenge of striking the balance of TG
Autor:
Joseph S. Warmus, Steven B. Coffey, John R. Hadcock, Liuqing Wei, Kevin Daniel Freeman-Cook, Martin B. Brenner, Kentaro Futatsugi, Suvi T. M. Orr, Nicole S. Roush, Angela Wolford, David W. Piotrowski, David Hepworth, Joanne Buxton, Sophie Y. Lavergne, Michael Herr, Gregory Storer, Janice E. Chin, Jian Wang, Ann M. Janssen, Terri Hinchey, Raman Sharma, Allyn T. Londregan, Amit S. Kalgutkar, Sandra M. Jennings, Wenhua Jiao, Declan Flynn
Publikováno v:
ACS Medicinal Chemistry Letters. 4:63-68
Takeda G-protein-coupled receptor 5 (TGR5) represents an exciting biological target for the potential treatment of diabetes and metabolic syndrome. A new class of high-throughput screening (HTS)-derived tetrahydropyrido[4,3-d]pyrimidine amide TGR5 ag
Autor:
Jeffrey E. Campbell, Robin Roof, Peter A. Boxer, Johnson Paul D, Ann M. Janssen, Jamie Singer, Jacob Bradley Schwarz, Nicole S. Roush, Leonard T. Meltzer, Chad L. Stoner, Michael William Wilson, Lisa H. Gold, Shelley R. Graham, Susan Hurst, Ti-Zhi Su, Leonard W. Cooke
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2409-2412
The synthesis and SAR of tolylamines with 5-HT6 receptor antagonist activity is presented. The amine, core aromatic, peripheral aromatic, and ether linker moieties of HTS hit 1 were modulated and the effect on potency at 5-HT6 examined. Tolylpiperidi
Autor:
Ann M. Janssen, Jason W. Armstrong, James V. Peterson, Richard A. Gerren, Richard A. Stanton, Steven D. Hamilton
Publikováno v:
Laboratory Robotics and Automation. 8:287-294
Laboratory automation for many years has contributed to increased productivity in analytical laboratories. Now automation is enabling biotechnology and pharmaceutical discovery research to progress more quickly and efficiently, encouraging researcher
Autor:
Duanzhi Wen, Sidney V. Suggs, Devarajan Karunagaran, Naili Liu, Rod L. Cupples, Yi Luo, Ann M. Janssen, Noa Ben-Baruch, David B. Trollinger, Victoria L. Jacobsen, Shi-Yuan Meng, Hsieng S. Lu, Sylvia Hu, David Chang, Weining Yang, Donna Yanigahara, Raymond A. Koski, Yosef Yarden
Publikováno v:
Molecular and Cellular Biology. 14:1909-1919
We used molecular cloning and functional analyses to extend the family of Neu differentiation factors (NDFs) and to explore the biochemical activity of different NDF isoforms. Exhaustive cloning revealed the existence of six distinct fibroblastic pro