Zobrazeno 1 - 10
of 26
pro vyhledávání: '"David B Duignan"'
Autor:
Dawn M George, Raymond J Huntley, Kevin Cusack, David B Duignan, Michael Hoemann, Jacqueline Loud, Regina Mario, Terry Melim, Kelly Mullen, Gagandeep Somal, Lu Wang, Jeremy J Edmunds
Publikováno v:
PLoS ONE, Vol 13, Iss 9, p e0203567 (2018)
The ability to restrict low molecular weight compounds to the gastrointestinal (GI) tract may enable an enhanced therapeutic index for molecular targets known to be associated with systemic toxicity. Using a triazolopyrazine CSF1R inhibitor scaffold,
Externí odkaz:
https://doaj.org/article/f9e4d7a1ef864cb18c1b355c36fdb091
Autor:
Kathy Sarris, Philip J. Hajduk, Ihle David C, Diana L. Donnelly-Roberts, Arthur Gomtsyan, Christian Goess, David B. Duignan, Danying Song, Chaohong Sun, Andrea Mcclure, Adrian D. Hobson, Robert H. Stoffel, Anil Vasudevan, John A. Mankovich, Sanjay C. Panchal, A. Chris Krueger, Steven L. Swann, Kenneth M. Comess, Andrew M. Petros, Wilson Noel S, Jill M. Wetter, Paul G. Richardson, Kenton L. Longenecker, Paul M. Jung, Vincent S. Stoll, Amanda W. Dombrowski, Suzanne Mathieu, Justin D. Dietrich, Philip B. Cox
Publikováno v:
Journal of Medicinal Chemistry. 64:417-429
Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and MAPK signaling pathways. The development of biologic drugs that inhibit TNFα has led to
Autor:
Sami Osman, Christian Goess, Xiazi Qiu, David B. Duignan, Qin C. Ji, John P. Savaryn, Gary J. Jenkins
Publikováno v:
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 1180
LC/MS quantification of leukotoxin (LTX) and leukotoxin diol (LTXdiol) in plasma has been previously reported, however large sample volumes are required for achieving stated assay Lower Limit of Quantification (LLOQ). Reported here is a fit-for-purpo
Autor:
Anshul Gupta, Jennifer L. Liras, Stephen Fowler, W. George Lai, Jane R. Kenny, Jonathan A. Phillips, Jinping Gan, Niresh Hariparsad, David B. Duignan, Wen Li Kelly Chen
Publikováno v:
Lab on a chip. 20(3)
Over the last decade, progress has been made on the development of microphysiological systems (MPS) for absorption, distribution, metabolism, and excretion (ADME) applications. Central to this progress has been proof of concept data generated by acad
Autor:
Douglas A. Keller, Brian R. Berridge, Ananthsrinivas Chakilam, Yvonne Will, Monicah A. Otieno, Kristin M. Fabre, David B. Duignan, Yvonne P. Dragan, Lorna Ewart, Terry R. Van Vleet, Danilo A. Tagle, Claire G. Jeong, Jinping Gan, Peggy Guzzie-Peck, Jonathan A. Phillips, Jeetu Eswaraka, Sonia M. de Morais, David E. Watson, Radhakrishna Sura, William R Proctor
Publikováno v:
Experimental Biology and Medicine. 242:1579-1585
Tissue chips are poised to deliver a paradigm shift in drug discovery. By emulating human physiology, these chips have the potential to increase the predictive power of preclinical modeling, which in turn will move the pharmaceutical industry closer
Autor:
Wilson Noel S, Gagandeep Somal, Michael Z. Hoemann, Don Konopacki, Maria A. Argiriadi, Anil Vasudevan, David B. Duignan, Bruce Clapham, David Banach, Phil B. Cox, Andrew Burchat, David J. Calderwood
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5562-5567
A series of furano[3,2-d]pyrimidine Syk inhibitors were synthesized and optimized for their enzyme potency and selectivity versus other kinases. In addition, ADME properties were assessed and compounds were prepared with optimized profiles for in viv
Autor:
Kevin P. Cusack, David B. Duignan, Jacqueline Loud, Michael Z. Hoemann, Lu Wang, Kelly D. Mullen, Regina Mario, Jeremy J. Edmunds, Dawn M. George, Gagandeep Somal, Raymond Huntley, Terry Melim
Publikováno v:
PLoS ONE, Vol 13, Iss 9, p e0203567 (2018)
PLoS ONE
PLoS ONE
The ability to restrict low molecular weight compounds to the gastrointestinal (GI) tract may enable an enhanced therapeutic index for molecular targets known to be associated with systemic toxicity. Using a triazolopyrazine CSF1R inhibitor scaffold,
Autor:
Youngjae Kim, Michelle Hart, Gary Gintant, Christopher M. Harris, Patricia N. Banfor, Jason A. Segreti, Scott W Mittelstadt, Peter Bousquet, David B. Duignan
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 359(1)
Inhibition of the sphingosine-1-phosphate (S1P)-catabolizing enzyme S1P lyase (S1PL) elevates the native ligand of S1P receptors and provides an alternative mechanism for immune suppression to synthetic S1P receptor agonists. S1PL inhibition is repor
Autor:
Jing Chen, Spiros Liras, Manthena V.S. Varma, Judith L. Treadway, Martha L. Minich, Laurel Sweet, John D. Knafels, Karen Atkinson, Nahor Haddish-Berhane, Angel Guzman-Perez, Benjamin D. Stevens, Alan Robertson, Sharad B. Murdande, David B. Duignan, Mark Ammirati, Timothy P. Rolph, William J. Zavadoski, Christopher S. Jones, Patricia Bourassa, Jeffrey A. Pfefferkorn, John Litchfield, Lili Yao, Kevin J. Filipski, Margit MacDougall, Levenia Baker, John C. Pettersen, Theresa D’Aquila, Ayman El-Kattan, Bo Feng, Francis Bourbonais, Meihua Tu, Robert J. Aiello, Gary Erik Aspnes, Jianwei Bian, David R. Derksen, Paul DaSilva-Jardine, Beijing Tan, James A. Landro, Over Cabrera, Rachel E. Kosa, Hud Lawrence Risley, Shenping Liu, Amanda L. Lapworth, Nicole Barucci
Publikováno v:
Journal of Medicinal Chemistry. 55:1318-1333
Glucokinase is a key regulator of glucose homeostasis, and small molecule allosteric activators of this enzyme represent a promising opportunity for the treatment of type 2 diabetes. Systemically acting glucokinase activators (liver and pancreas) hav
Publikováno v:
Molecular Pharmaceutics. 6:1180-1189
As sandwich cultured (SC) hepatocytes can repolarize to form bile canalicular networks, allowing active excretion of compounds in a vectorial manner, the model has been widely used for assessing the transporter related complexity of ADME/tox issues.