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Ion Channels as Targets in Drug Discovery

Gary Stephens, Edwards Stevens (2024) Springer 

DOI: 10.1007/978-3-031-52197-3


Spontaneous activity in peripheral sensory nerves: a systematic review

Choi, Dongchana; Goodwin, Georgea; Stevens, Edward B.b; Soliman, Nadiac; Namer, Barbarad,e; Denk, Franziskaa,* (2023) PAIN 

DOI: 10.1097/j.pain.0000000000003115

New aryl and acylsulfonamides as state-dependent inhibitors of Nav1.3

Nace Zidar a., Tihomir Tomaˇsiˇc., Danijel Kikelj., Martina Durcik., Jan Tytgat., Steve Peigneur., Marc Rogers., Alexander Haworth., and Robert W. Kirby. (2023) New aryl and acylsulfonamides as state-dependent inhibitors of Nav1.3 voltage-gated sodium channel. European Journal of Medicinal Chemistry, 2023.


Time Is a Critical Factor When Evaluating Oligonucleotide Therapeutics in Human Ether-a-Go-Go-Related Gene Assays

Yusheng Qu., Robert Kirby., Richard Davies., Ayesha Jinat., Stefano Stabilini., Bin Wu., Longchuan Yu., BaoXi Gao., and Hugo M. Vargas. (2023). Time Is a Critical Factor When Evaluating Oligonucleotide Therapeutics in Human Ether-a-Go-Go-Related Gene Assays. Nucleic Acid Therapeutics. Nucleic Acid Therapeutics, 2022.

Development of ASIC1a ligand-gated ion channel drug screening assays across multiple automated patch clamp platforms

Ridley, J., Manyweathers, S., Tang, R., Goetze, T., Becker, N., Kirby, R., Obergrussberger, A., & Rogers, M. (2022). Development of ASIC1a ligand-gated ion channel drug screening assays across multiple automated patch clamp platforms. Frontiers in Molecular Neuroscience.  Frontiers in Molecular Neuroscience, 2022.


Ion Channel Discovery – Partnering to Access Specialized Expertise

Stevens, E. B and Wright, P. D Future Drug Discovery, 2020. Many thanks to Future Drug Discovery for publishing the article.

A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm

Bradley J. Ridder, Derek J. Leishman, Matthew Bridgland-Taylor, Mohammadreza Samieegohar, Xiaomei Han, Wendy W. Wu, Aaron Randolph, Phu Tran, Jiansong Sheng, Timm Danker, Anders Lindqvist, Daniel Konrad, Simon Hebeisen, Liudmila Polonchuk, Evgenia Gissinger, Muthukrishnan Renganathan, Bryan Koci, Haiyang Wei, Jingsong Fan, Paul Levesque, Jae Kwagh, John Imredy, Jin Zhai, Marc Rogers, Edward Humphries, Robert Kirby, Sonja Stoelzle-Feix, Nina Brinkwirth, Maria  Giustina Rotordam, Nadine Becker, Søren Friis, Markus Rapedius, Tom A. Goetze, Tim Strassmaier, George Okeyo, James Kramer, Yuri Kuryshev, Caiyun Wu, Herbert Himmel, Gary R. Mirams, David G. Strauss, Rémi Bardenet, Zhihua Lia. Toxicology and Applied Pharmacology, 394: 114961

Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells

Kramer, J.; Himmel, H. M.; Lindqvist, A.; Stoelzle-Feix, S.; Chaudhary, K. W.; Li, D.; Bohme, G. A.; Bridgland-Taylor, M.; Hebeisen, S.; Fan, J.;  Renganathan, M.;  Imredy, J.; Humphries, E. S. A.; Brinkwirth, N.; Strassmaier, T.; Ohtsuki, A.; Danker, T.; Vanoye, C.; Polonchuk, L.; Fermini, B.; Beck Pierson, J.;  Gintant, G. Scientific Reports, 2020, 10; 5627


Ion channel drug discovery and modern medicine

Rogers, M.  MedNous, November-December 2019. Article published in the November-December 2019 edition of ‘MedNous’, a publication of Evernow Publishing Ltd.

The role of Nav1.7 in human nociceptors: insights from human induced pluripotent stem cell-derived sensory neurons of erythromelalgia patients

Meents, J.E.; Bressan, E.; Sontag, S.; Foerster, A.; Hautvast, P.; Rösseler, C.; Hampl, M.; Schüler, H.; Goetzke, R.; Le TKC.; Kleggetveit, I.P.; Le Cann, K.; Kerth, C.; Rush, A.M.; Rogers, M.; Kohl, Z.; Schmelz, M.; Wagner, W.; Jørum, E.; Namer, B.; Winner, B.; Zenke, M.; Lampert, A. PAIN, March 22, 2019.


Recent advances in targeting ion channels to treat chronic pain

Stevens, E.B.; Stephens, G.J.  British Journal of Pharmacology. 2018, 175 (12), 2133-2137


Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels

Zidar, N.; Žula, A.; Tomašič, T.; Rogers, M.; Kirby, RW.; Tytgat, J.; Peigneur, S.; Kikelj, D.; Ilaš, J.; Mašič LP.  European Journal of Medicinal Chemistry. 2017, 139, 232-241


Characterization of Endogenous Sodium Channels in the ND7-23 Neuroblastoma Cell Line: Implications for Use as a Heterologous Ion Channel Expression System Suitable for Automated Patch Clamp Screening

Rogers, M.; Zidar, N.; Kikelj, D.; Kirby, R.W.  Assay and Drug Development Technologies. 2016, 14 (2),109-130 


Novel K+ Channel Targets in Atrial Fibrillation Drug Development – Where Are We? 

El-Haou, S.; Ford, J.; Milnes, J.  Journal of Cardiovascular Pharmacology. 2015, 66 (5), 412-431 

Atrial‐like cardiomyocytes from human pluripotent stem cells are a robust preclinical model for assessing atrial‐selective pharmacology 

Devalla, H.D.; Schwach, V.; Ford, J.W.; Milnes, J.T.; El‐Haou, S.; Jackson, C.; Gkatzis, K.; Elliott, D.A.; de Sousa Lopes, S.M.C.; Mummery, C.L.; Verkerk, A.O.; Passier, R.  EMBO Molecular Medicine 2015. 7 (4), 394-410

Synthesis and biological evaluation of piperazine derivatives as novel isoform selective voltage-gated sodium (Nav) 1.3 channel modulators 

Jukič, M.; Frlan, R.; Chan, F.; Kirby, R.W.; Madge, D.J.; Tytgat, J.; Peigneur, S.; Anderluh, M.; Kikelj, D.  Medicinal Chemistry Research. , 24 (6), 2366-2380

Open access to the KCNQ channel: Retigabine and second generation M-current openers

Chapter 10 in: Cox B & Gosling M (Eds.) Ion Channel Drug Discovery. Krupp, J.; Rush, A.M.; Swahn, B.; Main M. Royal Society of Chemistry Publishing. 2015, 238-257


Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels 

Peigneur, S.; Žula, A.; Zidar, N.; Chan-Porter, F.; Kirby, R.; Madge, D.; Ilaš, J.; Kikelj, D.; Tytgat, J.  Marine Drugs. 2014, 12(4), 2132-43


Human Electrophysiological and Pharmacological Properties of XEN-D0101: A Novel Atrial-Selective Kv1.5/IKur Inhibitor

Ford J.; Milnes J.; Wettwer E.; Christ T.; Rogers M.; Sutton K.; Madge D.; Virag L.; Jost N.; Horvath Z.; Matschke K.; Varro A.; Ravens, U.  Journal of Cardiovascular Pharmacology. 2013, 61 (5), 408-415

Novel state-dependent voltage-gated sodium channel modulators, based on marine alkaloids from Agelas sponges 

Hodnik, Ž.; Tomašić, T.; Mašič L.P.; Chan, F.; Kirby, R.W.; Madge D.J.; Kikelj, D.  European Journal of Medicinal Chemistry. 2013, 70, 154-64

Ligand- and structure-based virtual screening for clathrodin-derived human voltage-gated sodium channel modulators 

Tomašić, T.; Hartzoulakis. B.; Zidar. N.; Chan, F.; Kirby R.W.; Madge, D.J.; Peigneur, S.; Tytgat, J.; Kikelj, D.  Journal of Chemical Information and Modelling. 2013, 53 (12), 3223-32


Recent advances in electrophysiology-based screening technology and the impact upon ion channel discovery research 

Southan, A.P.; Clark, G.  Methods in Molecular Biology. 2009, 565, 187-208

Voltage-clamp and current-clamp recordings from mammalian DRG neurons

Cummins, T.R.; Rush, A.M.; Estacion, M.; Dib-Hajj, S.D.; Waxman, S.G. Nature Protocols. 2009, 4, 1103-12


Multiple sodium channels and their roles in electrogenesis within dorsal root ganglion neurons

Rush, A.M.; Cummins, T.R.;  Waxman, S.G. Journal of Physiology. 2007, 579, 1-14 


The role of sodium channels in neuropathic pain

Rogers, M.; Tang L.; Madge, D.; Stevens E.  Seminars in cell and developmental biology. 2006, 17 (5), 571-581

A single sodium channel mutation produces hyper- or hypoexcitability in different types of neurons

Rush, A.M.; Dib-Hajj, S.D.; Liu, S.; Cummins T.R.; Black, J.A.; Waxman, S.G. Proceedings of the National Academy of Science USA. 2006, 103, 8245-50

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