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G4941K substitution in the pore-lining S6 helix of the skeletal muscle ryanodine receptor increases RyR1 sensitivity to cytosolic and luminal Ca2+
Le Xu, David D. Mowrey, Venkat R. Chirasani, Ying Wang, Daniel A. Pasek, Nikolay V. Dokholyan, and Gerhard Meissner
12.18.2017
GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability
Alexandre J C Loucif, Pierre-Philippe Saintot, Jia Liu, Brett M Antonio, Shannon G Zellmer, Katrina Yoger, Emma L Veale, Anna Wilbrey, Kiyoyuki Omoto, Lishuang Cao, Alex Gutteridge, Neil A Castle, Edward B Stevens, Alistair Matie
11.19.2017
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes
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, …
09.28.2017
Discovery of N-Substituted 7-Azaindoles as PIM1 Kinase Inhibitors – Part I
Claude Barberis, Neil Moorcroft, Chris Arendt, Mikhail Levit, Sandra Moreno-Mazza, Joseph Batchelor, Ingrid Mechin, Tahir Majid
09.18.2017
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
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 …
07.17.2017
Ion-pulling simulations provide insights into the mechanisms of channel opening of the skeletal muscle ryanodine receptor
David D. Mowrey, Le Xu, Yingwu Mei, Daniel A. Pasek, Gerhard Meissner, and Nikolay V. Dokholyan
06.05.2017
The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics
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
04.26.2017
The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels
Jonathan W. Theile, Matthew D. Fuller, and Mark L. Chapman
08.31.2016
Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells
Zhixin Lin, Sonia Santos, Karen Padilla, David Printzenhoff, Neil A. Castle
08.24.2016
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release
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, …
04.06.2016
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