Zobrazeno 1 - 10
of 14
pro vyhledávání: '"David, Printzenhoff"'
Publikováno v:
PLoS ONE, Vol 11, Iss 8, p e0161450 (2016)
The voltage dependent sodium channel Nav1.9, is expressed preferentially in peripheral sensory neurons and has been linked to human genetic pain disorders, which makes it target of interest for the development of new pain therapeutics. However, chara
Externí odkaz:
https://doaj.org/article/0a4e951432894c9b88aeb7972ad455b8
Autor:
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 A 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
Publikováno v:
PLoS ONE, Vol 11, Iss 4, p e0152405 (2016)
Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7 contribution to nociceptive signalling has been hampered by a lack of selective inhibitors. H
Externí odkaz:
https://doaj.org/article/b9af198893454af186b55747950a6251
Autor:
Jianmin Sun, Thomas Ryckmans, David Fengas, Colin R. Rose, M. Scott Johnson, Matthew Corbett, David James Rawson, Nigel Alan Swain, Joseph S. Warmus, Lyn H. Jones, Brian E. Marron, Aristos J. Alexandrou, David Printzenhoff, C. Elizabeth Payne, Bruce M. Bechle, Rubben Torella, Neil A. Castle, Jonathan W. Theile, Elaine Tseng, David C. Blakemore, Andrew Pike, R. Ian Storer, Neil J. Flanagan, Alan Daniel Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4805-4811
The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed. Extensive in vitro pharmacology and ADME profiling followed by in vivo preclinical PK and efficac
Autor:
David C. Pryde, Brian E. Marron, Peter J. Cox, C. J. Markworth, Joseph S. Warmus, Christopher William West, David Printzenhoff, S. McMurray, Stupple Paul Anthony, Zhixin Lin, Nigel Alan Swain, Mark L. Chapman, C. E. Payne, Ryoichi Suzuki, Gareth Waldron
Publikováno v:
MedChemComm. 8:1255-1267
In this article, we describe the discovery of an aryl ether series of potent and selective Nav1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Nav cha
Publikováno v:
British Journal of Pharmacology. 172:4905-4918
Background and purpose Aryl sulfonamide Nav 1.3 or Nav 1.7 voltage-gated sodium (Nav ) channel inhibitors interact with the Domain 4 voltage sensor domain (D4 VSD). During studies to better understand the structure-activity relationship of this inter
Autor:
Rosemarie Roeloffs, Anthony W Bannon, Adam R. Brown, Alexandre J.C. Loucif, Aristos J. Alexandrou, Anthony J. Kirkup, Mathew D Fuller, Gillian Stockbridge, Edward B. Stevens, David Printzenhoff, Praveen Anand, Steve England, Claire Elizabeth Payne, Uma Anand, Peter J. Bungay, Aaron C. Gerlach, Mark L. Chapman, Kemp Mark Ian, John H. Mahoney, Rebecca L. Prime, Jonathon W Theile, Brett M Antonio, Richard P. Butt, Sharan K. Bagal
Publikováno v:
British Journal of Pharmacology. 172:2654-2670
Background and Purpose NaV1.8 ion channels have been highlighted as important molecular targets for the design of low MW blockers for the treatment of chronic pain. Here, we describe the effects of PF-01247324, a new generation, selective, orally bio
Autor:
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
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(21)
The discovery and selection of a highly potent and selective Na
Autor:
Bruce M. Bechle, Stephen Martin Denton, Sebastien Galan, David James Rawson, Marcel J. de Groot, Brian E. Marron, Matthew S Johnson, Jo Hannam, Shoko Nakagawa, Dave Batchelor, Nigel Alan Swain, Steven M Reister, David Ellis, Mark L. Chapman, David Printzenhoff, Sarah J Ransley, Beaudoin Serge, David S. Millan, Christopher W. West, Kenneth John Butcher, R. Ian Storer, Stephen M Gaulier, Stupple Paul Anthony, Andrew Pike, Alan Daniel Brown, Christopher John Markworth, Bruce Brown, Zhixin Lin, Sasaki Kosuke, Paul A. Bradley, Ian Gurrell, Richard P. Butt, Mel Glossop, Ben S. Greener
Publikováno v:
Journal of medicinal chemistry. 60(16)
A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cyto
Autor:
Edward B. Stevens, Zhixin Lin, Anna Wilbrey, Stephen G. Waxman, Peter J. Cox, Sulayman D. Dib-Hajj, Mark L. Chapman, Malgorzata A. Mis, Christopher William West, R. Ian Storer, Stupple Paul Anthony, Elizabeth C. Payne, Manoj K. Patel, David Printzenhoff, Andrew D. Randall, James A. Hounshell, Douglas S. Krafte, Jamie Turner, Nigel Alan Swain, Aristos J. Alexandrou, Richard P. Butt, Adam R. Brown, Mark Estacion, Brian E. Marron, Alex Gutteridge, Neil A. Castle, Rachel Doyle, Mirko Rivara
Publikováno v:
PLoS ONE, Vol 11, Iss 4, p e0152405 (2016)
PLoS ONE
PLoS ONE
Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7 contribution to nociceptive signalling has been hampered by a lack of selective inhibitors. H
Autor:
Brett Antonio, Christopher Silvia, Alan D. Wickenden, Shannon G. Zellmer, Neil A. Castle, David Printzenhoff
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 12:107-122
Voltage dependent sodium channels are widely recognized as valuable targets for the development of therapeutic interventions for neuroexcitatory disorders such as epilepsy and pain as well as cardiac arrhythmias. An ongoing challenge for sodium chann