Validation and optimization of novel high-throughput assays for human epithelial sodium channels

Journal of Biomolecular Screening

Volumn 20, Issue 2, 2015, Pages 242-253

  Chen, Mao Xiang ^a,c   Gatfield, Kelly ^a,c   Ward, Emma ^a,c   Downie, David ^a,c   Sneddon, Helen F ^a,c   Walsh, Stacey ^b,c   Powell, Andrew J ^a,c   Laine, Dramane ^b,c   Carr, Michael ^b,c   Trezise, Derek ^a,c  

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (United States)

^c Essen BioScience Ltd   (United Kingdom)

Author keywords

channel; epithelial; FLIPR; IonWorks; sodium

Indexed keywords

EPITHELIAL SODIUM CHANNEL; EPITHELIAL SODIUM CHANNEL ALPHA; EPITHELIAL SODIUM CHANNEL BETA; EPITHELIAL SODIUM CHANNEL BLOCKING AGENT; EPITHELIAL SODIUM CHANNEL GAMMA; UNCLASSIFIED DRUG; EPITHELIAL SODIUM CHANNEL STIMULATING AGENT; MOLECULAR LIBRARY;

ARTICLE; BACMAM VIRUS; CELL MEMBRANE POTENTIAL; CONTROLLED STUDY; ELECTROPHYSIOLOGY; GENE MUTATION; HEK293 CELL LINE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; LIDDLE SYNDROME; LUNG ALVEOLUS EPITHELIUM; PRIORITY JOURNAL; PROCESS OPTIMIZATION; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN MOTIF; TOXICITY; TURNOVER TIME; VALIDATION PROCESS; VIRUS; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; EPITHELIUM CELL; GENE EXPRESSION; GENETICS; MEMBRANE POTENTIAL; METABOLISM; MOLECULAR LIBRARY; PATCH CLAMP TECHNIQUE; PROCEDURES; RESPIRATORY TRACT MUCOSA; STANDARDS;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; EPITHELIAL CELLS; EPITHELIAL SODIUM CHANNEL AGONISTS; EPITHELIAL SODIUM CHANNEL BLOCKERS; EPITHELIAL SODIUM CHANNELS; GENE EXPRESSION; HEK293 CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MEMBRANE POTENTIALS; PATCH-CLAMP TECHNIQUES; RESPIRATORY MUCOSA; SMALL MOLECULE LIBRARIES;

EID: 84921523862     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057114552399     Document Type: Article

References (34)

1. Garty H., Palmer L. G. Epithelial Sodium Channels: Function, Structure, and Regulation. Physiol. Rev. 1997 ; 77: 359-396
2. Rossier B. C., Pradervand S., Schild L., et al. Epithelial Sodium Channel and the Control of Sodium Balance: Interaction between Genetic and Environmental Factors. Annu. Rev. Physiol. 2002 ; 64: 877-897
3. Schild L. The Epithelial Sodium Channel: From Molecule to Disease. Rev. Physiol. Biochem. Pharmacol. 2004 ; 151: 93-107
4. Kellenberger S., Schild L. Epithelial Sodium Channel/Degenerin Family of Ion Channels: A Variety of Functions for a Shared Structure. Physiol. Rev. 2002 ; 82: 735-767
5. Matalon S., O'Brodovich H. Sodium Channels in Alveolar Epithelial Cells: Molecular Characterization, Biophysical Properties, and Physiological Significance. Annu. Rev. Physiol. 1999 ; 61: 627-661
6. Canessa C. M., Schild L., Buell G., et al. Amiloride-Sensitive Epithelial Na+ Channel Is Made of Three Homologous Subunits. Nature. 1994 ; 367: 463-467
7. Jasti J., Furukawa H., Gonzales E. B., et al. Structure of Acid-Sensing Ion Channel 1 at 1.9 A Resolution and Low pH. Nature. 2007 ; 449: 316-323
8. Stockand J. D., Staruschenko A., Pochynyuk O., et al. Insight toward Epithelial Na+ Channel Mechanism Revealed by the Acid-Sensing Ion Channel 1 Structure. IUBMB Life. 2008 ; 60: 620-628
9. Eaton D. C., Malik B., Bao H. F., et al. Regulation of Epithelial Sodium Channel Trafficking by Ubiquitination. Proc. Am. Thorac. Soc. 2010 ; 7: 54-64
10. Hanwell D., Ishikawa T., Saleki R., et al. Trafficking and Cell Surface Stability of the Epithelial Na+ Channel Expressed in Epithelial Madin-Darby Canine Kidney Cells. J. Biol. Chem. 2002 ; 277: 9772-9779
11. Lu C., Pribanic S., Debonneville A., et al. The PY Motif of ENaC, Mutated in Liddle Syndrome, Regulates Channel Internalization, Sorting and Mobilization from Subapical Pool. Traffic. 2007 ; 8: 1246-1264
12. Abriel H. J., Loffing J. F., Rebhun J. H., et al. Defective Regulation of the Epithelial Na+ Channel by Nedd4 in Liddle's Syndrome. J. Clin. Invest. 1999 ; 103: 667-673
13. Schild L. The Epithelia Sodium Channel and the Control of Sodium Balance. Biochim. Biophys. Acta. 2010 ; 1802: 1159-1165
14. Rauh R., Diakov A., Tzschoppe A., et al. A Mutation of the Epithelial Sodium Channel Associated with Atypical Cystic Fibrosis Increases Channel Open Probability and Reduces Na+ Self Inhibition. J. Physiol. 2010 ; 588: 1211-1225
15. Hirsh A. J., Molino B. F., Zhang J., et al. Design, Synthesis, and Structure-Activity Relationships of Novel 2-Substituted Pyrazinoylguanidine Epithelial Sodium Channel Blockers: Drugs for Cystic Fibrosis and Chronic Bronchitis. J. Med. Chem. 2006 ; 49: 4098-4115
16. Hirsh A. J., Zhang J., Zamurs A., et al. Pharmacological Properties of N-(3,5-diamino-6-chloropyrazine-2-carbonyl)-N′-4-[4-(2,3-dihydroxypropoxy)phenyl]butyl-guanidine methanesulfonate (552-02), a Novel Epithelial Sodium Channel Blocker with Potential Clinical Efficacy for Cystic Fibrosis Lung Disease. J. Pharmacol. Exp. Ther. 2008 ; 325: 77-88
17. Hunt T., Atherton-Watson H. C., Axford J., et al. Discovery of a Novel Chemotype of Potent Human ENaC Blockers Using a Bioisostere Approach. Part 1: Quaternary Amines. Bioorg. Med. Chem. Lett. 2012 ; 22: 929-932
18. Hunt T., Atherton-Watson H. C., Collingwood S. P., et al. Discovery of a Novel Chemotype of Potent Human ENaC Blockers Using a Bioisostere Approach. Part 2: α-Branched Quaternary Amines. Bioorg. Med. Chem. Lett. 2012 ; 22: 2877-2879
19. Clark K. L., Hughes S. A., Bulsara P., et al. Pharmacological Characterization of a Novel ENaCα siRNA (GSK2225745) with Potential for the Treatment of Cystic Fibrosis. Mol. Ther. Nucl. Acids. 2013 ; 15: e65
20. Collingwood S. P., Smith N. Pyrazine Derivatives as Epithelial Sodium Channel Blocker. 2007 ;:
21. Condreay J., Witherspoon S., Clay W., et al. Transient and Stable Gene Expression in Mammalian Cells Transduced with a Recombinant Baculovirus Vector. Proc. Natl. Acad. Sci. U. S. A. 1999 ; 96: 127-132
22. Shroeder K., Neagle B., Trezise D. J., et al. Ionworks HT: A New High-Throughput Electrophysiology Measurement Platform. J. Biomol. Screen. 2003 ; 8: 1-14
23. Finkel A., Wittel A., Yang N., et al. Population Patch Clamp Improves Data Consistency and Success Rates in the Measurement of Ionic Currents. J. Biomol. Screen. 2006 ; 11: 488-496
24. John V. H., Dale T. J, Hollands E. C., et al. Novel 384-Well Population Patch Clamp Electrophysiology Assays for Ca2+-Activated K+ Channels. J. Biomol. Screen. 2007 ; 12: 50-60
25. Dale T. J., Townsend C., Hollands E. C., et al. Population Patch Clamp Electrophysiology: A Breakthrough Technology for Ion Channel Screening. Mol. Biosyst. 2007 ; 3: 714-722
26. Hollands E. C., Dale T. J., Baxter A. W., et al. Population Patch-Clamp Electrophysiology Analysis of Recombinant GABAA alpha1beta3gamma2 Channels Expressed in HEK-293 Cells. J. Biomol. Screen. 2009 ; 14: 769-780
27. Li H., Sheppard D. N., Hug M. J. Transepithelial Electrical Measurements with the Ussing Chamber. J. Cyst. Fibros. 2004 ;: 123-126
28. Jiang X., Ingbar D. H., O'Grady S. M. Adrenergic Regulation of Ion Transport across Adult Alveolar Epithelial Cells: Effects on Cl-Channel Activation and Transport Function in Cultures with an Apical Air Interface. J. Membr. Biol. 2001 ; 181: 195-204
29. Chraïbi A., Horisberger J. D. Na Self Inhibition of Human Epithelial Na Channel: Temperature Dependence and Effect of Extracellular Proteases. J. Gen. Physiol. 2002 ; 120: 133-145
30. Knight K. K., Olson D. R., Zhou R., et al. Liddle's Syndrome Mutations Increase Na+ Transport through Dual Effects on Epithelial Na+ Channel Surface Expression and Proteolytic Cleavage. Proc. Natl. Acad. Sci. U. S. A. 2006 ; 103: 2805-2808
31. Clare J. J., Chen M. X., Downie D. L., et al. Use of Planar Array Electrophysiology for the Development of Robust Ion Channel Cell Lines. Comb. Chem. High Throughput Screen. 2009 ; 12: 96-106
32. Kashlan O. B., Sheng S., Kleyman T. R. On the Interaction between Amiloride and Its Putative Alpha-Subunit Epithelial Na+ Channel Binding Site. J. Biol. Chem. 2005 ; 280: 26206-26215
33. Chraïbi A., Vallet V., Firsov D., et al. Protease Modulation of the Activity of the Epithelial Sodium Channel Expressed in Xenopus Oocytes. Gen. Physiol. 1998 ; 111: 127-138
34. Jovov B., Berdiev B. K., Fuller C. M., et al. The Serine Protease Trypsin Cleaves C Termini of Beta-and Gamma-Subunits of Epithelial Na+ Channels. J. Biol. Chem. 2002 ; 277: 4134-4140