Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Todd W. Shearer"'
Autor:
Tony Y. Wang, Chiara Piubelli, Lee T. Schaller, Pierette Banker, Stefano Tacconi, Paula Selley, Todd W. Shearer, Robert A. Reid, Federico Faggioni, Daniel J. Price, Richard F. Cox, Shawn P. Williams, David H. Drewry, Michela Tessari, Richard G. Buckholz, Patrick R. Maloney, Paul R. Reid, Brian D. Thompson, Xi Liang, Jeffery L. Smith, Octerloney B. McDonald, Ilaria Sartori
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1958-1963
Hypothalamic CAMKK2 represents a potential mechanism for chemically affecting satiety and promoting weight loss in clinically obese patients. Single-digit nanomolar inhibitors of CAMKK2 were identified in three related ATP-competitive series. Limited
Autor:
Stephen A. Stimpson, Todd W. Shearer, Fritz Kramer, Ying Shen, Marc K. Hellerstein, Chelsea King, Po-yin Anne Wong, Mahalakshmi Shankaran, Alan J. Russell, Philip Stewart Turnbull, William J. Evans, Lisa G. Clifton, Scott M. Turner
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 310:E405-E417
Biomarkers of muscle protein synthesis rate could provide early data demonstrating anabolic efficacy for treating muscle-wasting conditions. Androgenic therapies have been shown to increase muscle mass primarily by increasing the rate of muscle prote
Autor:
Stephen A. Stimpson, Lisa G. Clifton, Richard V. Clark, Marc K. Hellerstein, Katja Remlinger, Todd W. Shearer, Scott M. Turner, Michael S. Leonard, James C. Poole, William J. Evans
Publikováno v:
Journal of Cachexia, Sarcopenia and Muscle
Background We recently validated in cross-sectional studies a new method to determine total body creatine pool size and skeletal muscle mass based on D3-creatine dilution from an oral dose and detection of urinary creatinine enrichment by isotope rat
Autor:
Adam Ashe, Thomas B. Stanley, Todd W Shearer, Craig D. Wagner, John C. Ulrich, Lisa M. Leesnitzer, Barry G. Shearer, Raymond V. Merrihew, Robert W. Wiethe, James M. Way, Robert X. Xu, Andrew N. Billin, Timothy M. Willson, Michael R. Jeune
Publikováno v:
Journal of Medicinal Chemistry. 53:1857-1861
4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide 3 (GSK3787) was identified as a potent and selective ligand for PPARdelta with good pharmacokinetic properties. A detailed binding study using mass spectral analysis confirmed cova
Autor:
Susan P Weaver, Sarva M. Tadepalli, Channa K Jayawickreme, Lihong Chen, George R. Szewczyk, Maite de los Frailes, Mythily Vimal, Brian Budzik, Thomas J. Rimele, Sean Ross, Susan Armour, David Moncol, Don L. Anderson, Francisco Javier Colilla, Michael R. Jeune, David D. Wisnoski, Karen A. Evans, Ralph A. Rivero, Zibin B Chen, J. David Becherer, Todd W Shearer, Jian Jin, Robert J. Griffin
Publikováno v:
Journal of Medicinal Chemistry. 52:7962-7965
A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5 G-protein coupled receptor is described. Subsequent optimization resulted in the rapid identifi
Autor:
Christie Schulte, Curt D. Haffner, J. Chuck Poole, Eric E. Boros, John C. Ulrich, David J. Cowan, Tiffany Carpenter, Eugene L. Stewart, J. Darren Stuart, Frank Preugschat, David N. Deaton, Tara Renae Rheault, Todd W. Shearer, Barry G. Shearer, J. David Becherer, Michael R. Jeune, Istvan Kaldor, Lisa M. Shewchuk, Terrence L. Smalley
Publikováno v:
Journal of medicinal chemistry. 58(17)
Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure-activity relationships (SAR) of the 4-, 6-, and 8-substituents of the quinoline ring resulted in the identification of ap
Autor:
John C. Ulrich, Petrov Kimberly, Tiffany Carpenter, David J. Cowan, J. Darren Stuart, J. David Becherer, Eugene L. Stewart, Frank Preugschat, David N. Deaton, W. Wallace Harrington, Yu Guo, Naphtali Milliken, Barry G. Shearer, Michael R. Jeune, Istvan Kaldor, Terrence L. Smalley, Curt D. Haffner, Brad R. Henke, Rodolfo Cadilla, Todd W. Shearer, Eric E. Boros, Christie Schulte
Publikováno v:
Journal of medicinal chemistry. 58(8)
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in
Autor:
Stephen A. Stimpson, Fritz Kramer, Marc K. Hellerstein, Mahalakshmi Shankaran, Alan J. Russell, Andrew N. Billin, William J. Evans, Todd W. Shearer, Scott Turner
Publikováno v:
The FASEB Journal. 29
Autor:
Scott Turner, Fritz Kramer, Marc K. Hellerstein, William J. Evans, Mahalakshmi Shankaran, Alan J. Russell, Stephen A. Stimpson, Andrew N. Billin, Todd W. Shearer
Publikováno v:
The FASEB Journal. 29
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 320:258-265
This study was designed to evaluate the signaling pathways coupling adenosine A1 receptors and extracellular signal-regulated kinase (ERK) 1 and 2 in human trabecular meshwork (HTM) cells. Studies were conducted using cultures of primary HTM cells an