TRPA1 ankyrin repeat six interacts with a small molecule inhibitor chemotype
Wei Chou Tseng, David C. Pryde, Katrina E. Yoger, Karen M. Padilla, Brett M. Antonio, Seungil Han, Veerabahu Shanmugasundaram, and Aaron C. Gerlach
View Articlep62-Dependent Phase Separation of Patient-Derived KEAP1 Mutations and NRF2
E. W. Cloer, P. F. Siesser, E. M. Cousins, D. Goldfarb, D. D. Mowrey, J. S. Harrison, S. J. Weir, N. V. Dokholyan, M. B. Majora
View ArticlePF-06526290 can both enhance and inhibit conduction through voltage-gated sodium channels
Lingxin Wang, Shannon G Zellmer, David M Printzenhoff and Neil A Castle
View ArticleA comprehensive Approach to Identifying Repurposed Drugs to Treat SCN8A Epilepsy
Talia A. Atkin, Chani M. Maher, Aaron C. Gerlach, Bryant C. Gay, Brett M. Antonio, Sonia C. Santos, Karen M. Padilla, JulieAnn Rader, Douglas S. Krafte, Matthew A. Fox, Gregory R. Stewart, Slavé Petrovski, Orrin Devinsky, Matthew Might, Steven Petrou, David B. Goldstein
View ArticleDiscovery and in Vitro Optimization of 3‐Sulfamoylbenzamides as ROMK Inhibitors
Matthew F. Sammons, Sujay V. Kharade, Kevin J. Filipski, Markus Boehm, Aaron C. Smith, Andre Shavnya, Dilinie P. Fernando, Matthew S. Dowling, Philip A. Carpino, Neil A. Castle, Shannon G. Zellmer, Brett M. Antonio, James R. Gosset, Anthony Carlo, and Jerod S. Denton
View ArticleG4941K 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
View ArticleGI-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
View ArticleHighly 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, Jonathan W. Theile, Rubben Torella, Elaine Tseng, Joseph S. Warmus
View ArticleDiscovery 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
View ArticleDiscovery 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 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
View Article