201
Views
9
CrossRef citations to date
0
Altmetric
Reviews

Advances in functional assays for high-throughput screening of ion channels targets

(Associate Director) , , &
Pages 995-1006 | Published online: 05 Sep 2010

Bibliography

  • Wickenden A. K+ channels as therapeutic drug targets. Pharmacol Ther 2002;5:157-82
  • Drews J. Drug discover: a historical perspective. Science 2000;287:1960-4
  • Venter C, Adams MD, Myers EW, The sequence of human genome. Science 2001;291:1304-51
  • Davies NP, Hanna MG. The skeletal muscle channelopathies: distinct entities and overlapping syndromes. Curr Opin Neurol 2003;16:559-68
  • Mulley JC, Scheffer IE, Petrou S, Berkovic SF. Channelopathies as a genetic cause of epilepsy. Curr Opin Neurol 2003;16:171-6
  • Pietrobon D. Calcium channels and channelopathies of the central nervous system. Mol Neurobiol 2002;25:31-50
  • Kullmann DM. The neuronal channelopathies. Brain 2002;125:1177-95
  • Hubner CA, Jentsch TJ. Ion channel diseases. Hum Mol Genet 2002;11:2435-45
  • Abt M, Lim Y, Sacks J, A sequential approach for identifying lead compounds in large chemical databases. Stat Sci 2001;16:154-68
  • Dai GE, Haedo RJ, Warren VA, A high-throughput assay for evaluating state dependence and subtype selectivity of CaV2 calcium channel inhibitors. Assay Drug Dev Technol 2008;6(2):195-212
  • Mattheakis LC, Sayvchenko A. Assay technologies for screening ion channel targets. Curr Opin Drug Discov Devel 2001;1:124-34
  • Rudiger R, Mongillo M, Rizzuto R, Pozzan T. Looking forward to see calcium. Nat Rev Mol Cell Biol 2003;4:579-86
  • Brini M, Marsault R, Bastianutto C, Transfected Aequorin in the measurement of cytosolic Ca2+ concentration([Ca2+]C). J Biol Chem 1995;270:9896-903
  • Maeda A, Nishimura S, Kameda K, Generation of cell transfectants expressing cardiac calcium ion channel and calcium indicator protein aequorin. Anal Biochem 1996;242:31-9
  • Stables J, Mattheakis LC, Chang R, Rees S. Recombinant aequorin as reporter of changes in intracellular calcium in mammalian cells. Methods Enzymol 2000;327:456-71
  • Nayak TK, Harinath S, Nama S, Inhibition of human two pore domain K+ channel TREK1 by local anesthetic Lidocaine: negative cooperativity and half-of-sites saturation kinetics. Mol Pharmacol 2009;76:903-17
  • Triggle D. Voltage gated ion channels as drug targets, John Wiley & Sons, 2006
  • Diwan JJ, Paliwal R, Kaftan E, Bawa R. Amitochondrial protein fraction catalyzing transport of the K+ analog Tl+. FEBS Lett 1990;273:215-18
  • Weaver CD, Harden D, Dworetzky SI, A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modultaors in mammalian cells. J Biomol Screen 2004;9:671-7
  • Bartschat DK, Blaustein MP. Potassium channels in isolated presynaptic nerve terminals from Rat Brain. J Physiol 1985;361:419-40
  • Scott CW, Wilkins DE, Trivedi S, Crankshaw DJ. A medium-throughput functional assay of KCNQ2 potassium channels using rubidium efflux and atomic absorption spectroscopy. Anal Biochem 2003;319:251-7
  • Trivedi S, Dekermendjian K, Julien R, Cellular HTS assays for pharmacological characterization of NaV1.7 modulators. Assay Drug Dev Technol 2007;6(2):167-79
  • Terstappen GC. Functional analysis of native and recombinant ion channels using high-capacity nonradioactive rubidium efflux assay. Anal Biochem 1999;272:149-55
  • Gill S, Gill R, Wicks D, Liang D. A cell based Rb flux assa of the KV1.3 potassium channel. Assay Drug Dev Technol 2007;5(3):373-80
  • Sorota S, Zhang X, Margulis M, Characterization of a hERG screen using the ionworks HTS: comparison of a hERG rubidium efflux screen. Assay Drug Dev Technol 2005;3(1):47-57
  • Wang K, Mcllvain B, Tseng E, Validation of an atomic absorption rubidium ion efflux assa for KCNQ/M channels using Io channel reader 8000. Assay Drug Dev Technol 2004;2(5):525-34
  • Jow F, Tseng E, Maddox T, Rb efflux through functional activation of cardiac KCNQ/minK chanels by the Benzodiazepine R-L3 (L-364,373). Assay Drug Dev Technol 2006;4:443-50
  • Rezazadeh S, Hesketh JC, Fedida D. Rb flux through hERG channels affects the potency of channel blocking drugs: correlation with data obtained using a high throughput Rb efflux assay. J Biomol screen 2004;9(7):588-97
  • Foster CD, Speakman MJ, Fujii K, Brading AF. The effects of cromakalim on the detrusor muscle of human and pig urinary bladder. Br J Pharmacol 1989;97:281-91
  • Baxter DF, Kirk M, Garcia AF, A novel membrane potential-sensitive fluorescent dye improves cell-based assays for ion channels. J Biomol Screen 2002;7:79-85
  • Minta A, Tsien RY. Fluorescent indicators for cytosolic sodium. J Biol Chem 1989;264:19449-57
  • Wolff C, Fuks B, Chatelain P. Comparative study of membrane potential-sensitive fluorescent probes and their use in ion channel screening assays. J Biomol Screen 2003;8:533-43
  • Gonzalez JE, Tsien RY. Improved indicators of cell membrane potential that use fluorescence resonance energy transfer. Chem Biol 1997;4:269-77
  • Gonzalez JE, Oades K, Leychkis Y, Cellbased assays and instrumentation for screening ion-channel targets. Drug Discov Today 1999;4:431-9
  • Huang CJ, Harootunian A, Maher MP, Characterization of voltage-gated sodium channel blockers by electrical stimulation and fluorescence detection of membrane potential. Nat Biotechnol 2006;24:439-46
  • Dunlop J, Bowlby M, Peri R, High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiology. Nat Rev Drug Discov 2008;7:358-68
  • Farrea C, Georgea M, Brüggemanna A, Fertig N. Ion channel screening – automated patch clamp on the rise. Drug Discov Today Technol 2008;5(1):e23-8
  • Xia X, Maliski EG, Gallant P, Rogers D. Classification of kinase inhibitors using a bayesian model. J Med Chem 2004;47:4463-70
  • Ghose AK, Viswanadhan VN, Wendoloski J. Prediction of hydrophobic (lipophilic) properties of small organic molecules using fragmental methods: an analysis of ALOGP and CLOGP methods. J Phys Chem 1998;102:3762-72
  • Rogers D, Brown RD, Hahn M. Using extended-connectivity fingerprints with Laplacian-modified Bayesian analysis in high-throughput screening follow-up. J Biomol Screen 2005;10:682-6

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.