Publications - Sophion

Wnts control membrane potential in mammalian cancer cells

Author(s): Jonathan Ashmore, Hervør Olsen, Naja Sørensen, Christopher Thrasivoulou, Aamir Ahmed

Voltage-Gated Ion Channels in Cancer Cell Proliferation

Author(s): Vidhya R. Rao 1 , Mathew Perez-Neut 1, Simon Kaja 2 and Saverio Gentile 1,*

Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel NaV1.1 Provide Novel Leads for Development of Antiepileptic Drugs

Author(s): Chun Yuen Chow, Yanni K.-Y. Chin, Andrew A. Walker, Shaodong Guo, Linda V. Blomster, Micaiah J. Ward, Volker Herzig, Darin R. Rokyta, and Glenn F. King

Using automated patch clamp electrophysiology platforms in pain-related ion channel research: insights from industry and academia

Author(s): Damian Bell, Mark Dallas

The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6+/− mice

Author(s): Nadia Lybøl von Schoubye, Kristen Frederiksen Uffe Kristiansen, Anders Victor Petersend, Nils Ole Dalby, Morten Grunnet, Henrik Sinda Jensen, Thomas Jespersen, Vikaas S. Sohale, Jean-François Perrier

The Snake with the Scorpion’s Sting: Novel Three-Finger Toxin Sodium Channel Activators from the Venom of the Long-Glanded Blue Coral Snake

Author(s): Daryl C. Yang 1,2,†, Jennifer R. Deuis 3,†, Daniel Dashevsky 2,†, James Dobson 2,†, Timothy N. W. Jackson 2, Andreas Brust 3, Bing Xie 4, Ivan Koludarov 2, Jordan Debono 2, Iwan Hendrikx 2, Wayne C. Hodgson 1, Peter Josh 5, Amanda Nouwens 5, Gregory J. Baillie 3, Timothy J. C. Bruxner 3, Paul F. Alewood 3, Kelvin Kok Peng Lim 6, Nathaniel Frank 7, Irina Vetter 3,8,* and Bryan G. Fry 2,*

The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis

Author(s): Vinayak Singh†, Stefano Donini‡, Angela Pacitto§, Claudia SalaΔ, Ruben C. HartkoornΔ, Neeraj DharΔ, Gyorgy Keri⊥, David B. Ascher§, Guillaume Mondésert#, Anthony VocatΔ, Andréanne LupienΔ, Raphael SommerΔ, Hélène Vermet#, Sophie Lagrange#, Joe Buechler⊗, Digby F. Warner†, John D. McKinneyΔ, Janos Pato⊥, Stewart T. ColeΔ, Tom L. Blundell§, Menico Rizzi‡, and Valerie Mizrahi*†

The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6

Author(s): Mathilde R. Israel, Panumart Thongyoo, Jennifer R. Deuis, David J. Craik, Irina Vetter, Thomas Durek

The development of automated patch clamp assays for canonical transient receptor potential channels TRPC3, 6, and 7

Author(s): McPate M, Bhalay G, Beckett M, Fairbrother S, Gosling M, Groot-Kormelink PJ, Lane R, Kent T, Van Diepen MT, Tranter P, Verkuyl JM.

Termination of Vernakalant-Resistant Atrial Fibrillation by Inhibition of Small-Conductance Ca2+-Activated K+ Channels in Pigs

Journal: Circulation: Arrhythmia and Electrophysiology
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Author(s): Jonas Goldin Diness, Lasse Skibsbye, Rafel Simó-Vicens, Joana Larupa Santos, Pia Lundegaard, Carlotta Citerni, Daniel Rafael Peter Sauter, Sofia Hammami Bomholtz, Jesper Hastrup Svendsen, Søren-Peter Olesen, Ulrik S. Sørensen, Thomas Jespersen, Morten Grunnet, Bo Hjorth Bentzen

Synthesis of Pseudellone Analogs and Characterization as Novel T-type Calcium Channel Blockers

Author(s): Dan Wang, Pratik Neupane, Lotten Ragnarsson, Robert J. Capon and Richard J. Lewis

Synthesis and Biological Evaluation of Novel Olean-28,13?- lactams as Potential Anti-prostate Cancer Agents

Author(s): Yong Ai†‡, Yang Hu†, Fenghua Kang†‡, Yisheng Lai†‡, Yanju Jia†, Zhangjian Huang*†‡, Sixun Peng†‡, Hui Ji*†, Jide Tian§, and Yihua Zhang*†‡

Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors

Author(s): Daowei Huang, Lei Huang, Qingwei Zhang, Jianqi Li a

Synthesis and Biological Evaluation of Five‐Atom‐Linker‐Based Arylpiperazine Derivatives with an Atypical Antipsychotic Profile

Author(s): Chunhui Wu, Yu Wang, Feipu Yang, Wenqiang Shi, Zhen Wang, Ling He, Yang He, Jingshan Shen

Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect

Author(s): Mingshuo Xu, Yu Wang, Feipu Yang, Chunhui Wu, Zhen Wang, Bin Ye, Xiangrui Jiang, Qingjie Zhao, JianfengLi, Yongjian Liu, Junchi Zhang, Guanghui Tian, Yang He, Jingshan Shen, Hualiang Jiang

Study of TRP Channels by Automated Patch Clamp Systems

Author(s): Morten Sunesen, Rasmus B Jacobsen

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain

Author(s): Steven J. McKerrall, Teresa Nguyen, Kwong Wah Lai, Philippe Bergeron, Lunbin Deng, Antonio Di Pasquale, Jae H. Chang, Jun Chen, Tania Chernov-Rogan, David H. Hackos, Jonathan Maher, Daniel F. Ortwine, Jodie Pang, Jian Payandeh, William R. Proctor, Shannon D. Shields, Jennifer Vogt, Pengfei Ji, Wenfeng Liu, Elisa Ballini, Lilia Schumann, Glauco Tarozzo, Girish Bankar, Sultan Chowdhury, Abid Hasan, J. P. Johnson Jr., Kuldip Khakh, Sophia Lin, Charles J. Cohen, Christoph M. Dehnhardt, Brian S. Safina, Daniel P. Sutherlin

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Author(s): Fang Zhu, Yujie Wang, Qian Du, Wenxiang Ge, Zhanhui Li, Xu Wang, Chunyan Fu, Lusong Luo, Sheng Tian, Haikuo Ma, Jiyue Zheng, Yi Zhang, Xiaotian Sun, Sudan He, Xiaohu Zhang

Simultaneous assessment of compound activity on cardiac Nav1.5 peak and late currents in an automated patch clamp platform

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Donglin Guo & Stephen Jenkinson

Selective Nav1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

Author(s): Girish Bankar, Samuel J. Goodchild, Sarah Howard, Karen Nelkenbrecher, Matthew Waldbrook, Michelle Dourado, Noah G. Shuart, Sophia Lin, Clint Young, Zhiwei Xie, Kuldip Khakh, Elaine Chang, Luis E. Sojo, Andrea Lindgren, Sultan Chowdhury, Shannon Decker, Michael Grimwood, Jean-Christophe Andrez, Christoph M. Dehnhardt, Jodie Pang, Jae H. Chang, Brian S. Safina, Daniel P. Sutherlin, James P. Johnson, Jr., David H. Hackos, C. Lee Robinette, and Charles J. Cohen

Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator

Author(s): Jun-ichi Okada1,2,*, Takashi Yoshinaga3, Junko Kurokawa4, Takumi Washio1,2, Tetsushi Furukawa4, Kohei Sawada3, Seiryo Sugiura1,2 and Toshiaki Hisada1,2

Screening strategies for the discovery of ion channel monoclonal antibodies

Author(s): Caroline S. Colley, Elizabeth England, John E. Linley, Trevor C. I. Wilkinson

Scaffold Hopping Toward Agomelatine: Novel 3, 4-Dihydroisoquinoline Compounds as Potential Antidepressant Agents

Author(s): Yang Yang, Wei Ang, Haiyue Long, Ying Chang, Zicheng Li, Liangxue Zhou, Tao Yang, Yong Deng & Youfu Luo

Role of High-Throughput Electrophysiology in Drug Discovery

Author(s): Chang Liu, Tianbo Li, and Jun Chen

Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr–/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator

Author(s): Brandon S. Martin 1), Gabriel Martinez-Botella 2), Carlos M. Loya 2), Francesco G. Salituro 2), Albert J. Robichaud 2), Molly M. Huntsman 3), Mike A. Ackley 2), James J. Doherty 2),* and Joshua G. Corbin 1)

Rational engineering defines a molecular switch that is essential for activity of spider-venom peptides against the analgesics target Nav1.7

Author(s): Julie K Klint, Yanni K. Y. Chin, and Mehdi Mobli

QPatch: the past, present and future of automated patch clamp

Author(s): Chris Mathes

QPatch: the missing link between HTS and ion channel drug discovery.

Journal: Combinatorial Chemistry & High Throughput Screening
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Author(s): Chris Mathes*,1, Søren Friis 2, Michael Finley 3 and Yi Liu 3

Positive allosteric modulators of α7 nicotinic acetylcholine receptors affect neither the function of other ligand- and voltage-gated ion channels and acetylcholinesterase, nor β-amyloid content

Journal: The International Journal of Biochemistry & Cell Biology
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Author(s): Hugo R. Ariasa, Federica Ravazzinib, Katarzyna M. Targowska-Dudac, Agnieszka A. Kaczord, e, Dominik Feuerbachf, Juan C. Boffig, Piotr Draczkowskid, Dirk Montagh, Brandon M. Browni, Ana Belén Elgoyheng, Krzysztof Jozwiakc, Giulia Puiab

Porphyrin derivatives as potent and selective blockers of neuronal Kv1 channels

Author(s): D. Daly a), A. Al-Sabi b), G. K. Kinsella c), K. Nolan a) and J. O. Dolly b)

Physiological modulators of Kv3.1 channels adjust firing patterns of auditory brainstem neurons

Author(s): Maile Reed Brown 1), Lynda El-Hassar 1), Yalan Zhang 1), Giuseppe Alvaro 2), Charles H Large 2), and Leonard K. Kaczmarek 3)

Pharmacological screening technologies for venom peptide discovery

Author(s): Prashanth JR(1, Hasaballah N(1, Vetter I(2

Pharmacological characterisation of the highly Nav1.7 selective spider venom peptide Pn3a

Author(s): Jennifer R. Deuis, Zoltan Dekan, Joshua S. Wingerd, Jennifer J. Smith, Nehan R. Munasinghe, Rebecca F. Bhola 2), Wendy L. Imlach, Volker Herzig, David A. Armstrong, K. Johan Rosengren, Frank Bosmans, Stephen G. Waxman, Sulayman D. Dib-Hajj, Pierre Escoubas, Michael S. Minett, Macdonald J. Christie, Glenn F. King, Paul F. Alewood, Richard J. Lewis, John N. Wood & Irina Vetter

pH-dependent inhibition of K2P3.1 prolongs atrial refractoriness in whole hearts

Author(s): Mark A. Skarsfeldt, Thomas A. Jepps, Sofia H. Bomholtz, Lea Abildgaard, Ulrik S. Sørensen, Emilie Gregers, Jesper H. Svendsen

Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation

Author(s): Santoshi Billakota, J. Michael Andresen, Bryant C. Gay, Gregory R. Stewart, Nikolai B. Fedorov, Aaron C. Gerlach, Orrin Devinsky

Patch clamping by numbers

Author(s): Claire Wood 1, Gareth J. Waldron* 1, Christine Williams 2, Gareth J. Waldron 2

Patch clamp electrophysiology steps up a gear

Author(s): Derek J. Trezise

NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions

Author(s): Nausch B, Rode F, Jørgensen S, Nardi A, Korsgaard MP, Hougaard C, Bonev AD, Brown WD, Dyhring T, Strøbæk D, Olesen SP, Christophersen P, Grunnet M, Nelson MT, Rønn LC.

Novel Chitohexaose Analog Protects Young and Aged mice from CLP Induced Polymicrobial Sepsis

Author(s): Pragnya Das, Santosh K. Panda, Beamon Agarwal, Sumita Behera, Syed M. Ali, Mark E. Pulse, Joseph S. Solomkin, Steven M. Opal, Vineet Bhandari & Suchismita Acharya

New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1

Author(s): Nichole Coleman, Brandon M. Brown, Aida Oliván-Viguera, Vikrant Singh, Marilyn M. Olmstead, Marta Sofia Valero, Ralf Köhler and Heike Wulff

Multiple sodium channel isoforms mediate the pathological effects of Pacific ciguatoxin-1

Author(s): Marco C. Inserra, Mathilde R. Israel, Ashlee Caldwell, Joel Castro, Jennifer R. Deuis, Andrea M. Harrington, Angelo Keramidas, Sonia Garcia-Caraballo, Jessica Maddern, Andelain Erickson, Luke Grundy, Grigori Y. Rychkov, Katharina Zimmermann, Richard J. Lewis, Stuart M. Brierley & Irina Vetter

Modulation of P2X3 and P2X2/3 Receptors by Monoclonal Antibodies

Author(s): Anatoly Shcherbatko‡12, Davide Foletti‡1, Kris Poulsen‡1, Pavel Strop‡, Guoyun Zhu‡, Adela Hasa-Moreno‡, Jody Melton Witt‡, Carole Loo‡, Stellanie Krimm‡, Ariel Pios‡, Jessica Yu‡, Colleen Brown‡, John K. Lee§, Robert Stroud¶, Arvind Rajpal‡ and David Shelton‡

MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes

Author(s): James Kramer 1*, Carlos A. Obejero-Paz 1*, Glenn Myatt 2, Yuri A. Kuryshev 1, Andrew Bruening-Wright 1, Joseph S. Verducci 3 & Arthur M. Brown 1

Mashiningan improves opioid-induced constipation in rats by activating cystic fibrosis transmembrane conductance regulator chloride channel

Journal: Journal of Pharmacology and Experimental Therapeutics
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Author(s): Yumi Harada, Seiichi Iizuka, Yayoi Saegusa, Sachiko Mogami, Naoki Fujitsuka and Tomohisa Hattori

Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach

Journal: Bioorganic & Medicinal Chemistry Letters
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Author(s): Johan Kajanus, Ingemar Jacobson, Annika Åstrand (b., Roine I. Olsson, Ulrik Gran, Annika Björe, Ola Fjellström (a., Öjvind Davidsson, Hans Emtenäs, Anders Dahlén, Boel Löfberg, Zhong-Qing Yuan, Johan Sundell, Johan Cassel, Jonna Gyll, Tommy Iliefski, Ågot Högberg, Emma Lindhardt, Jesper Malmberg

Ion channel screening technologies today

Author(s): Georg C. Terstappen

Intracellular Calcium Mobilization in Response to Ion Channel Regulators via a Calcium-Induced Calcium Release Mechanism

Journal: The Journal of Pharmacology and Experimental Therapeutics
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Author(s): Terry Petrou, Hervør L. Olsen, Christopher Thrasivoulou, John R. Masters, Jonathan F. Ashmore, and Aamir Ahmed

Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor

Author(s): M. Flinspach, Q. Xu, A. D. Piekarz, R. Fellows, R. Hagan, A. Gibbs, Y. Liu, R. A. Neff, J. Freedman, W. A. Eckert, M. Zhou, R. Bonesteel, M. W. Pennington, K. A. Eddinger, T. L. Yaksh, M. Hunter, R. V. Swanson & A. D. Wickenden

Inhibitory effects of cannabidiol on voltage-dependent sodium currents

Author(s): Mohammad-Reza Ghovanloo, Noah Gregory Shuart, Janette Mezeyova, Richard A Dean, Peter C Ruben and Samuel J Goodchild

Inhibition of the potassium channel KCa3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury

Journal: Volume 795, 15 January 2017, Pages 1–7
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Author(s): Roland G.W. Staala, Tanzilya Khayrullinaa, Hong Zhanga, Scott Davisb, Shaun M. Fallona, Manuel Cajinac, Megan E. Nattinic, Andrew Hub, Hua Zhouc, Suresh Babu Podac, Stevin Zorna, Gamini Chandrasenac, Elena Dalea, Brian Campbella, Lars Christian Biilmann Rønnd, Gordon Munrod, Thomas Mӧllera

Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp

Author(s): Sören J. Wacker, Dr. Wiktor Jurkowski, Dr. Katie J. Simmons, Prof. Dr. Colin W. G. Fishwick, Prof. Dr. A. Peter Johnson, Dr. David Madge, Prof. Dr. Erik Lindahl, Dr. Jean‐Francois Rolland, Prof. Dr. Bert L. de Groot

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel

Author(s): Pamela A. Haile, Linda N. Casillas, Michael J. Bury, John F. Mehlmann, Robert Singhaus, Jr., Adam K. Charnley, Terry V. Hughes, Michael P. DeMartino, Gren Z. Wang, Joseph J. Romano, Xiaoyang Dong, Nikolay V. Plotnikov, Ami S. Lakdawala, Maire A. Convery, Bartholomew J. Votta, David B. Lipshutz, Biva M. Desai, Barbara Swift, Carol A. Capriotti, Scott B. Berger, Mukesh K. Mahajan, Michael A. Reilly, Elizabeth J. Rivera, Helen H. Sun, Rakesh Nagilla, Carol LePage, Michael T. Ouellette, Rachel D. Totoritis, Brian T. Donovan, Barry S. Brown†, Khuram W. Chaudhary†, Peter J. Gough, John Bertin, and Robert W. Marquis

Identification and Electrophysiological Evaluation of 2-Methylbenzamide Derivatives as Nav1.1 Modulators

Author(s): François Crestey§, Kristen Frederiksen§, Henrik S. Jensen§, Kim Dekermendjian§, Peter H. Larsen§, Jesper F. Bastlund§, Dunguo Lu†, Henry Liu†, Charles R. Yang†, Morten Grunnet*§, and Niels Svenstrup*§

Identification and Characterization of ProTx-III [μ-TRTX-Tp1a], a New Voltage-Gated Sodium Channel Inhibitor from Venom of the Tarantula Thrixopelma pruriens

Author(s): Fernanda C. Cardoso, Zoltan Dekan, K. Johan Rosengren, Andelain Erickson, Irina Vetter, Jennifer R. Deuis, Volker Herzig, Paul F. Alewood, Glenn F. King, and Richard J. Lewis

High-Throughput Screening of Nav1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument

Author(s): Chris Chambers, Ian Witton, Cathryn Adams, Luke Marrington and Juha Kammonen

High-Throughput Screen of GluK1 Receptor Identifies Selective Inhibitors with a Variety of Kinetic Profiles Using Fluorescence and Electrophysiology Assays

Author(s): Kelli Solly 1), Rebecca Klein 2), Michael Rudd 3), M. Katharine Holloway 4), Eric N. Johnson 1),*, Darrell Henze 2), Michael F. A. Finley 1)

High-throughput electrophysiology: An emerging paradigm for ion-channel screening and physiology

Author(s): John Dunlop, Mark Bowlby, Ravikumar Peri, Dmytro Vasilyev & Robert Arias

High throughput physiological screening of iPSC-derived cardiomyocytes for drug development

Journal: Biochimica et Biophysica Acta (BBA) - Molecular Cell Research
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Author(s): Juan C. del Álamo a), Derek Lemonsb, c), Ricardo Serrano a), Alex Savchenkob, c, e), Fabio Cerignoli d), Rolf Bodmer c), Mark Mercolab, c, e)

GABA-A a17B3y2 on QPatch

Author(s): Hervor L Olsen, M Knirke Jensen

Functional Studies of Sodium Channels: From Target to Compound Identification

Journal: Wiley Online Library DOI: 10.1002/cpph.14
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Author(s): Daniel Bertrand 1), Bruno Biton 2), Thomas Licher 3), Jean-Marie Chambard 2), Christophe Lanneau 2), Michel Partiseti 2), Isabel A. Lefevre 2)

From identification to functional characterization of cyriotoxin-1a, an antinociceptive toxin from the spider Cyriopagopus schioedtei.

Author(s): Gonçalves TC, Benoit E, Kurz M, Lucarain L, Fouconnier S, Combemale S, Jaquillard L, Schombert B, Chambard JM, Boukaiba R, Hessler G, Bohme A, Bialy L, Hourcade S, Béroud R, De Waard M, Servent D, Partiseti M

Extracellular K+ Dampens T Cell Functions: Implications for Immune Suppression in the Tumor Microenvironment

Author(s): Seow Theng Ong, Aik Seng Ng, Xuan Rui Ng, Zhong Zhuang, Brandon Han Siang Wong, Praseetha Prasannan, Yee Jiun Kok, Xuezhi Bi, Heesung Shim, Heike Wulff, Kanianthara George Chandy, and Navin Kumar Verma

Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel NaV1.7 Inhibition

Author(s): Hue N. T. Tran, Poanna Tran, Jennifer R. Deuis, Akello J. Agwa, Alan H. Zhang, Irina Vetter and Christina I. Schroeder

Engineering Highly Potent and Selective Microproteins Against Nav1.7 Sodium Channel for Treatment of Pain

Author(s): Anatoly Shcherbatko1, Andrea Rossi1, Davide Foletti2, Guoyun Zhu1, Oren Bogin3, Meritxell Galindo-Casas1, Mathias Rickert4, Adela Hasa-Moreno1, Victor Bartevitch5, Andreas Crameri6, Alexander R. Steiner7, Robert Henningsen7, Avinash Gill8, Jaume Pons1, David L. Shelton1, Arvind Rajpal9 and Pavel Strop1*

Electrophysiological and Pharmacological Characterization of Human Inwardly Rectifying Kir2.1 Channels on an Automated Patch-Clamp Platform

Author(s): Camille Sanson, Brigitte Schombert, Bruno Filoche-Romme, Michel Partiseti and G. Andrees Bohme

Eleclazine exhibits enhanced selectivity for long QT syndrome type 3–associated late Na+ current

Author(s): Nesrine El-Bizri, Cheng Xie, Lynda Liu, James Limberis, Michael Krause, Ryoko Hirakawa, Steven Nguyen, Dennis R. Tabuena, Luiz Belardinelli, Kristopher M.Kahlig

Efficient Enzymatic Ligation of Inhibitor Cystine Knot Spider Venom Peptides: Using Sortase A To Form Double-Knottins That Probe Voltage-Gated Sodium Channel NaV1.7

Author(s): Agwa AJ, Blomster LV, Craik DJ, King GF, Schroeder CI.

Effect of antiarrhythmic drugs on small conductance calcium – activated potassium channels

Author(s): Rafel Simó-Vicensa, Daniel R.P. Sauter, Morten Grunnet, Jonas G. Diness, Bo H. Bentzen

Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis

Author(s): Ana Guardia, Jessica Baiget, Mónica Cacho, Arancha Pérez, Montserrat Ortega-Guerra, Winston Nxumalo, Setshaba D. Khanye, Joaquín Rullas, Fátima Ortega, Elena Jiménez, Esther Pérez-Herrán, María Teresa Fraile-Gabaldón, Jorge Esquivias, Raquel Fernández, Esther Porras-De Francisco, Lourdes Encinas, Marta Alonso, Ilaria Giordano, Cristina Rivero, Juan Miguel-Siles, Javier G. Osende, Katrina A. Badiola, Peter J. Rutledge , Matthew H. Todd, Modesto Remuiñán, and Carlos Alemparte

Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide are Potent TMEM16A Antagonists that Fully Bronchodilate Airway

Author(s): Kent Miner, Katja Labitzke, Benxian Liu, Paul Wang, Kathryn Henckels, Kevin Gaida, Robin Elliott, Jian Jeffrey Chen, Longbin Liu, Anh Leith, Esther Trueblood, Kelly Hensley, Xing-Zhong Xia, Oliver Homann, Brian Bennett, Mike Fiorino, John Whoriskey, Gang Yu, Sabine Escobar, Min Wong, Teresa L. Born, Alison Budelsky, Mike Comeau, Dirk Smith, Jonathan Phillips, James A. Johnston, Joe McGivern, Kerstin Weikl, David Powers, Karl Kunzelmann, Deanna Mohn, Andreas Hochheimer, John K. Sullivan

Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination

Author(s): Bandita Bagchi, Ahmed Al-Sabi, Seshu Kaza, Dimitri Scholz, Valerie B. O’Leary, J. Oliver Dolly, Saak V. Ovsepian

Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination

Author(s): Bandita Bagchi, Ahmed Al-Sabi, Seshu Kaza, Dimitri Scholz, Valerie B. O'Leary, J. Oliver Dolly , Saak V. Ovsepian

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Author(s): Jeff A. Zablocki*†, Elfatih Elzein†, Xiaofen Li†, Dmitry O. Koltun†, Eric Q. Parkhill†, Tetsuya Kobayashi†, Ruben Martinez†, Britton Corkey†, Haibo Jiang†, Thao Perry†, Rao Kalla†, Gregory T. Notte†, Oliver Saunders†, Michael Graupe†, Yafan Lu†, Chandru Venkataramani†, Juan Guerrero†, Jason Perry⊥, Mark Osier§, Robert Strickley∥,Gongxin Liu#, Wei-Qun Wang#, Lufei Hu#, Xiao-Jun Li#, Nesrine El-Bizri#, Ryoko Hirakawa#, Kris Kahlig#, Cheng Xie#, Cindy Hong Li#, Arvinder K. Dhalla#, Sridharan Rajamani#, Nevena Mollova‡, Daniel Soohoo‡, Eve-Irene Lepist‡, Bernard Murray‡, Gerry Rhodes‡, Luiz Belardinelli#, and Manoj C. Desai†

Discovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.

Author(s): Panayiotis A. Procopiou , Niall A. Anderson, John Barrett, Tim N. Barrett, Matthew H. J. Crawford, Brendan J. Fallon, Ashley P. Hancock, Joelle Le, Seble Lemma, Richard P. Marshall, Josie Morrell, John M. Pritchard, James E. Rowedder, Paula Saklatvala, Robert J. Slack, Steven L. Sollis, Colin J. Suckling, Lee R. Thorp, Giovanni Vitulli, and Simon J. F. Macdonald

Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain

Journal: Bioorganic & Medicinal Chemistry Letters
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Author(s): Mark J.Wall, Nalin L.Subasinghe, Michael P.Winters. Mary Lou Lubin, Michael F.A. Finley, Ning Qin Michael, R. Brandt, Michael P.Neeper, Craig R. Schneider, Raymond W.Colburn, Christopher M. Flores, Zhihua Sui

Discovery and mode of action of a novel analgesic β-toxin from the African spider Ceratogyrus darlingi

Author(s): Silmara R. Sousa, Joshua S. Wingerd, Andreas Brust, Christopher Bladen, Lotten Ragnarsson, Volker Herzig, Jennifer R. Deuis, Sebastien Dutertre, Irina Vetter, Gerald W. Zamponi, Glenn F. King, Paul F. Alewood, Richard J. Lewis

Discovery and electrophysiological characterization of SKF-32802; a novel hERG agonist found through a large-scale structural similarity search

Author(s): Brian T. Donovan, Deepak Bandyopadhyay,, Chaya Duraiswami, Christopher J. Nixon, Claire Y. Townsend, Stan F. Martens

Direct evidence for high affinity blockade of NaV1.6 channel subtype by huwentoxin-IV spider peptide, using multiscale functional approaches

Author(s): Tânia C. Gonçalves, Rachid Boukaiba, Jordi Molgób, Muriel Amar, Michel Partiseti, Denis Servent, Evelyne Benoit

Differential Free Intracellular Calcium Release by Class II Antiarrhythmics in Cancer Cell Lines

Journal: The Journal of Pharmacology and Experimental Therapeutics
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Author(s): Reyes-Corral M, Sørensen NM, Thrasivoulou C, Dasgupta P, Ashmore JF 1, Ahmed A

Development of the 1,2,4-triazole-based anticonvulsant drug candidates acting on the voltage-gated sodium channels. Insights from in-vivo, in-vitro, and in-silico studies

Author(s): Barbara Kaproń, Jarogniew J. Łuszczki, Anita Płazińska, Agata Siwek, Tadeusz Karcz, Anna Gryboś, Gabriel Nowak, Anna Makuch-Kocka, Katarzyna Walczak, Ewa Langner, Karolina Szalast, Sebastian Marciniak, Magdalena Paczkowska, Judyta Cielecka-Piontek, Lukasz M.Ciesla, Tomasz Plech

Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems

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Developing Molecular Pharmacology of BK Channels for Therapeutic Benefit

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Comprehensive in vitro cardiac safety assessment using human stem cell technology: Overview of CSAHi HEART initiative

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Takasuna K1, Asakura K2, Araki S3, Ando H4, Kazusa K5, Kitaguchi T6, Kunimatsu T7, Suzuki S8, Miyamoto N9.

Co-expression of β Subunits with the Voltage-Gated Sodium Channel NaV1.7: the Importance of Subunit Association and Phosphorylation and Their Effects on Channel Pharmacology and Biophysics

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Characterization of Potassium Channel Modulators with QPatch™ Automated Patch-Clamp Technology: System Characteristics and Performance To cite this article:

Author(s): Jonatan Kutchinsky, Søren Friis, Margit Asmild, Rafael Taboryski, Simon Pedersen, Ras K. Vestergaard, Rasmus B. Jacobsen, Karen Krzywkowski, Rikke L. Schrøder, Trine Ljungstrøm, Nathalie Hélix, Claus B. Sørensen, Morten Bech, and Niels J. Willumsen

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Characterization of compounds on nicotinic acetylcholine receptor alpha7 channels using higher throughput electrophysiology

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Cell volume and membrane stretch independently control K+ channel activity

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Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells: An In-Vitro Model to Predict Cardiac Effects of Drugs

Journal: Journal of Biomedical Science and Engineering
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Author(s): Romain Sube, Eric A. Ertel

Cardiac sodium channel antagonism – Translation of preclinical in vitro assays to clinical QRS prolongation

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Stephen Jenkinson, Asser Bassyouni, Jason Cordes, Bernard Fermini, Donglin Guo, David M.Potter, David S.Ramirez, Jill Steidl-Nichols, Sunny Sun, ToddWisialowski

Cardiac safety assessment with motion field imaging analysis of human iPS cell-derived cardiomyocytes is improved by an integrated evaluation with cardiac ion channel profiling

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Biological Profiling of Coleoptericins and Coleoptericin-Like Antimicrobial Peptides from the Invasive Harlequin Ladybird Harmonia axyridis

Journal: Advances in Experimental Medicine and Biology
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Author(s): Rolf Hirsch, Jochen Wiesner, Alexander Marker, Armin Bauer, Peter E. Hammann, Andreas Vilcinskas

Benzothiophenes as Potent Analgesics Against Neuropathic Pain

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Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels

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Author(s): Mads P.G. Korsgaard, Dorte Strøbæk and Palle Christophersen

Automated Patch Clamping Using the QPatch

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Automated Electrophysiology: High Throughput of Art

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Automated and manual patch clamp data of human induced pluripotent stem cell-derived dopaminergic neurons

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Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium

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An Official American Thoracic Society Workshop Report: Translational Research in Rare Respiratory Diseases

Author(s): Kristof AS, Petrof BJ, Hamid Q, Kolb M, Landry JS, MacKenzie A, McCormack FX, Murawski IJ, Moss J, Rauch F, Rosas IO, Shapiro AJ, Smith BM, Thomas DY, Trapnell BC, Young LR, Zariwala MA

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality

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A Small Molecule Induces Oligodendrogenesis Leading to Myelin Sheath Repair

Journal: Journal of Clinical Endocrinology & Metabolic Disorders
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Author(s): Steven H Nye, James G Yarger

A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo

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A novel substituted aminoquinoline selectively targets voltage-sensitive sodium channel isoforms and NMDA receptor subtypes and alleviates chronic inflammatory and neuropathic pain

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A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons

Journal: The Journal of Pharmacological and Experimental Therapeutics
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Author(s): Marcelo D. Rosato-Siri, Erika Zambello, Chiara Mutinelli, Nicoletta Garbati, Roberto Benedetti, Laura Aldegheri, Francesca Graziani, Caterina Virginio, Giuseppe Alvaro and Charles H. Large

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A dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a P2X7 antagonist clinical candidate

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