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    Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes

    Sep 28, 2017

    R. Ian Storer, Andy Pike, Nigel A. Swain, Aristos J. Alexandrou, Bruce M. Bechle, David C. Blakemore, Alan D. Brown, Neil A. Castle, Matthew S. Corbett, Neil J. Flanagan, David Fengas, M. Scott Johnson, Lyn H. Jones, Brian E. Marron, C. Elizabeth Payne, David Printzenhoff, David J. Rawson, Colin R. Rose, Thomas Ryckmans, Jianmin Sun, Jonathan W. Theile, Rubben Torella, Elaine Tseng, Joseph S. Warmus

     

    Discovery of N-Substituted 7-Azaindoles as PIM1 Kinase Inhibitors – Part I

    Sep 18, 2017

    Claude Barberis, Neil Moorcroft, Chris Arendt, Mikhail Levit, Sandra Moreno-Mazza, Joseph Batchelor, Ingrid Mechin, Tahir Majid

    Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4- yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7

    Jul 17, 2017

    Nigel Alan Swain, Dave Batchelor, Serge Beaudoin, Bruce M. Bechle, Paul A Bradley, Alan D Brown, Bruce Brown, Ken J Butcher, Richard P Butt, Mark L Chapman, Stephen Denton, David Ellis, Sebastien Galan, Stephen M Gaulier, Ben S Greener, Marcel J. de Groot, Mel S Glossop, Ian K Gurrell, Jo Hannam, Matthew S Johnson, Zhixin Lin, Christopher J Markworth, Brian E Marron, David S Millan, Shoko Nakagawa, Andy Pike, David Printzenhoff, David J Rawson, Sarah J Ransley, Steven M Reister, Kosuke Sasaki, R Ian Storer, Paul Anthony Stupple, and Christopher W West

    Ion-pulling simulations provide insights into the mechanisms of channel opening of the skeletal muscle ryanodine receptor

    Jun 05, 2017

    David D. Mowrey, Le Xu, Yingwu Mei, Daniel A. Pasek, Gerhard Meissner, and Nikolay V. Dokholyan

     

    The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

    Apr 26, 2017

    D. C. Pryde, N. A. Swain, P. A. Stupple, C. W. West, B. Marron, C. J. Markworth, D. Printzenhoff, Z. Lin, P. J. Cox, R. Suzuki, S. McMurray, G. J. Waldron, C. E. Payne, J. S. Warmus and M. L. Chapman

    The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels

    Aug 31, 2016

    Jonathan W. Theile, Matthew D. Fuller, and Mark L. Chapman

    Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells

    Aug 24, 2016

    Zhixin Lin, Sonia Santos, Karen Padilla, David Printzenhoff, Neil A. Castle

    Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

    Apr 06, 2016

    Aristos J. Alexandrou, Adam R. Brown, Mark L. Chapman, Mark Estacion, Jamie Turner, Malgorzata A. Mis, Anna Wilbrey, Elizabeth C. Payne, Alex Gutteridge, Peter J. Cox, Rachel Doyle, David Printzenhoff, Zhixin Lin, Brian E. Marron, Christopher West, Nigel A. Swain, R. Ian Storer, Paul Stupple, Neil A. Castle, James A. Hounshell, Mirko Rivara, Andrew Randall, Sulayman D. Dib-Hajj, Douglas Krafte, Stephen G. Waxman, Manoj K. Patel, Richard P. Butt, Edward B. Stevens

    APOL1 kidney disease risk variants cause cytotoxicity by depleting cellular potassium and inducing stress-activated protein kinases

    Nov 21, 2015

    Opeyemi A. Olabisi, Jia-Yue Zhang, Lynn VerPlank, Nathan Zahler, Salvatore DiBartolo III, John F. Heneghan, Johannes S. Schlöndorff, Jung Hee Suh, Paul Yan, Seth L. Alper, David J. Friedman, and Martin R. Pollak

    Validation of ion channel targets

    Nov 05, 2015

    Aaron C Gerlach and Brett M Antonio