Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Janice E. Chin"'
Autor:
Anna Pakula, Janelle M. Spinazzola, Louis M. Kunkel, James Conner, Jeffrey J. Widrick, Janice E. Chin, Matthias Lambert, Jane Owens
Publikováno v:
Molecular therapy : the journal of the American Society of Gene Therapy. 29(3)
Duchenne muscular dystrophy (DMD) is a severe genetic disorder caused by mutations in the DMD gene. Absence of dystrophin protein leads to progressive degradation of skeletal and cardiac function and leads to premature death. Over the years, zebrafis
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:
Melissa L. Gillaspy, Diane M. Hargrove, Mary E. Lame, Paul Da Silva Jardine, Dennis O. Scott, Catherine E. Trebino, Yingxin Zhang, Kimberly O. Cameron, Richard L. Elliott, Kelly A. Martin, Janice E. Chin, Elena E. Beretta, Swick Andrew Gordon, Jeffrey S. Dubins, Janet A. LaFlamme, Dexue Sun, Tristan S. Maurer, Nancy A. Nardone, Amit S. Kalgutkar, Jeremy A. Bartlett, Robert M. Oliver, Yue Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6797-6801
We describe the design, synthesis, and structure-activity relationships of triazolobenzodiazepinone CCK1 receptor agonists. Analogs in this series demonstrate potent agonist activity as measured by in vitro and in vivo assays for CCK1 agonism. Our ef
Autor:
Gina M. Ward, Janice D. Wagner, John R. Hadcock, Janice E. Chin, Bruce Auerbach, Kylie Kavanagh, Li Zhang, H. James Harwood
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 335:103-113
Cannabinoid-1 (CB(1)) receptor antagonists exhibit pharmacological properties favorable to treatment of obesity, caused by both centrally mediated effects on appetite and peripherally mediated effects on energy metabolism. However, the relative contr
Autor:
David Christopher Ebner, Paula M. Loria, David Hepworth, Edward L. Conn, Janice E. Chin, Lucy Rogers, Kevin J. Filipski, Philip A. Carpino, Shawn Cabral, Maria A. Vanvolkenburg, Lisa D. Norquay, John R. Hadcock, Aaron C. Smith, Kimberly O. Cameron, Markus Boehm, Esther C.Y. Lee, Denise Gautreau, Martin B. Brenner, Michelle Morin, Peter C. Bonnette, Alan M. Mathiowetz
Publikováno v:
ACS medicinal chemistry letters. 4(11)
Orphan G protein-coupled receptors (oGPCRs) are a class of integral membrane proteins for which endogenous ligands or transmitters have not yet been discovered. Transgenic animal technologies have uncovered potential roles for many of these oGPCRs, p
Publikováno v:
Molecular Endocrinology. 8:51-58
Chinese hamster ovary (CHO) cells were transfected with a cDNA encoding protein kinase C alpha (PKC) and a cell line (CHO-PKC alpha) expressing approximately 7-fold greater amounts of PKC as the parental cells were isolated. Activation of PKC by 12-O
Publikováno v:
Current opinion in drug discoverydevelopment. 9(5)
The peptide galanin is primarily expressed in the central nervous system (CNS) and it is active in a range of models of behavior. The identification of three galanin receptors, whose distribution of expression is distinct but overlapping, is evidence
Autor:
Y Sugie, T Inagaki, Janice E. Chin, K A Dekker, Carolyn B. Levy, D A Perry, Jeffrey S. Dubins, R K McPherson, Janice C. Parker, P V Perry, B Hulin, Judith L. Treadway, K Tachikawa, K M Andrews
Publikováno v:
Diabetes. 49(12)
Peptidic glucagon antagonists have been shown to lower blood glucose levels in diabetic models (1-3), but attempts to identify small molecular weight glucagon receptor-binding antagonists have met with little success. Skyrin, a fungal bisanthroquinon