A medium-throughput functional assay of KCNQ2 potassium channels using rubidium efflux and atomic absorption spectrometry

Analytical Biochemistry

Volumn 319, Issue 2, 2003, Pages 251-257

  Scott, Clay W ^a   Wilkins, Deidre E ^a   Trivedi, Shephali ^a   Crankshaw, Denis J ^b  

^a ASTRAZENECA   (United Kingdom)

^b MCMASTER UNIVERSITY   (Canada)

Author keywords

Atomic absorption spectrometry; K+ channel; KCNQ2; Kv7.2; Rubidium flux

Indexed keywords

ATOMIC ABSORPTION SPECTROMETRY; ATOMS; CELL CULTURE; POTASSIUM; RUBIDIUM; TEA;

96-WELL MICROTITER PLATE; ATOMIC ABSORPTION SPECTROMETERS; HETEROLOGOUS EXPRESSION; KCNQ2; KV7.2; NEUROTRANSMITTER RELEASE; PHARMACOLOGICAL PROFILES; VOLTAGE-GATED POTASSIUM CHANNELS;

ABSORPTION SPECTROSCOPY;

LINOPIRDINE; MEMBRANE PROTEIN; POTASSIUM ION; RETIGABINE; RUBIDIUM ION; VOLTAGE GATED POTASSIUM CHANNEL;

ARTICLE; ATOMIC ABSORPTION SPECTROMETRY; BIOACCUMULATION; CATION TRANSPORT; CELL MEMBRANE DEPOLARIZATION; CELL MEMBRANE TRANSPORT; CELLULAR DISTRIBUTION; CONTROLLED STUDY; EMBRYO; HETEROLOGOUS EXPRESSION; HUMAN; HUMAN CELL; INHIBITION KINETICS; NEUROTRANSMITTER RELEASE; PHARMACOLOGICAL BLOCKING; PHARMACOLOGICAL STIMULATION; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN STABILITY;

EID: 0037829355     PISSN: 00032697     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0003-2697(03)00328-2     Document Type: Article

References (33)

1. Coghlan M.J., Carroll W.A., Gopalakrishnan M. Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress. J. Med. Chem. 44:2001;1627-1653.
2. Shieh C., Coghlan M., Sullivan J.P., Gopalakrishnan M. Potassium channels: molecular defects, diseases, and therapeutic opportunities. Pharmacol. Rev. 52:2000;557-593.
3. Catterall W.A., Chandy K.G., Gutman G.A. The IUPHAR Compendium of Voltage-gated Ion Channels. 2002;IUPHAR Media, Leeds.
4. Whiteaker K.L., Gopalakrishnan S.M., Groebe D., Shieh C.C., Warrior U., Burns D.J., Coghlan M.J., Scott V.E., Gopalakrishnan M. Validation of FLIPR membrane potential dye for high throughput screening of potassium channel modulators. J. Biomol. Screen. 6:2001;305-312.
5. Tang W., Kang J., Wu X., Rampe D., Wang L., Shen H., Li Z., Dunnington D., Garyantes T. Development and evaluation of high throughput functional assay methods for HERG potassium channel. J. Biomol. Screen. 6:2001;325-331.
6. Falconer M., Smith F., Surah-Narwal S., Congrave G., Liu Z., Hayter P., Ciaramella G., Keighley W., Haddock P., Waldron G., Sewing A. High-throughput screening for ion channel modulators. J. Biomol. Screen. 7:2002;460-465.
7. Bartschat D.K., Blaustein M.P. Calcium-activated potassium channels in isolated presynaptic nerve terminals from rat brain. J. Physiol. 361:1985;441-457.
8. Bartschat D.K., Blaustein M.P. Potassium channels in isolated presynaptic nerve terminals from rat brain. J. Physiol. 361:1985;419-440.
9. Cheng C.S., Alderman D., Kwash J., Dessaint J., Patel R., Lescoe M.K., Kinrade M.B., Yu W. A high-throughput HERG potassium channel function assay: an old assay with a new look. Drug Dev. Indus. Pharm. 28:2002;177-191.
10. Terstappen G.C. Functional analysis of native and recombinant ion channels using a high-capacity nonradioactive rubidium efflux assay. Anal. Biochem. 272:1999;149-155.
11. Tinel N., Lauritzen I., Chouabe C., Lazdunski M., Borsotto M. The kcnq2 potassium channel - splice variants, functional and developmental expression - brain localization and comparison with kcnq3. FEBS Lett. 438:1998;171-176.
12. Schroeder B.C., Kubisch C., Stein V., Jentsch T.J. Moderate loss of function of cyclic-AMP-modulated KCNQ2/KCNQ3 K+ channels causes epilepsy. Nature. 396:1998;687-690.
13. Yang W.P., Levesque P.C., Little W.A., Conder M.L., Ramakrishnan P., Neubauer M.G., Blanar M.A. Functional expression of two kvlqt1-related potassium channels responsible for an inherited idiopathic epilepsy. J. Biol. Chem. 273:1998;19419-19423.
14. Jow F., Wang K.W. Cloning and functional expression of rKCNQ2 K+ channel from rat brain. Mol. Brain Res. 80:2000;269-278.
15. Smith J.S., Iannotti C.A., Dargis P., Christian E.P., Aiyar J. Differential expression of KCNQ2 splice variants: Implications to M current function during neuronal development. J. Neurosci. 21:2001;1096-1103.
16. Wang H.S., Pan Z.M., Shi W.M., Brown B.S., Wymore R.S., Cohen I.S., Dixon J.E., McKinnon D. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 282:1998;1890-1893.
17. Biervert C., Schroeder B.C., Kubisch C., Berkovic S.F., Propping P., Jentsch T.J., Steinlein O.K. A potassium channel mutation in neonatal human epilepsy. Science. 279:1998;403-406.
18. Singh N.A., Charlier C., Stauffer D., Dupont B.R., Leach R.J., Melis R., Ronen G.M., Bjerre I., Quattlebaum T., Murphy J.V., Mcharg M.L., Gagnon D., Rosales T.O., Peiffer A., Anderson V.E., Leppert M. A novel potassium channel gene, kcnq2, is mutated in an inherited epilepsy of newborns. Nat. Genet. 18:1998;25-29.
19. Charlier C., Singh N.A., Ryan S.G., Lewis T.B., Reus B.E., Leach R.J., Leppert M. A pore mutation in a novel kqt-like potassium channel gene in an idiopathic epilepsy family. Nat. Genet. 18:1998;53-55.
20. Cooper E.C., Aldape K.D., Abosch A., Barbaro N.M., Berger M.S., Peacock W.S., Jan Y.N., Jan L.Y. Colocalization and coassembly of two human brain M-type potassium channel subunits that are mutated in epilepsy. Proc. Natl. Acad. Sci. USA. 97:2000;4914-4919.
21. Shapiro M.S., Roche J.P., Kaftan E.J., Cruzblanca H., Mackie K., Hille B. Reconstitution of muscarinic modulation of the KCNQ2/KCNQ3 K+ channels that underlie the neuronal M current. J. Neurosci. 20:2000;1710-1721.
22. Wang H.S., McKinnon D. Potassium currents in rat prevertebral and paravertebral sympathetic neurones: control of firing properties. J. Physiol. 485:1995;319-335.
23. Motulsky H.J., Ransnas L.A. Fitting curves to data using nonlinear regression: a practical and nonmathematical review. FASEB J. 1:1987;365-374.
24. Zhang J.H., Chung T.D.Y., Oldenburg K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J. Biomol. Screen. 4:1999;67-73.
25. Hadley J.K., Noda M., Selyanko A.A., Wood I.C., Abogadie F.C., Brown D.A. Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels. Br. J. Pharmacol. 129:2000;413-415.
26. Rundfeldt C. The new anticonvulsant retigabine (D-23129) acts as an opener of k+ channels in neuronal cells. Eur. J. Pharmacol. 336:1997;243-249.
27. Rundfeldt C. Characterization of the K+ channel opening effect of the anticonvulsant retigabine in PC12 cells. Epilepsy Res. 35:1999;99-107.
28. Tatulian L., Delmas P., Abogadie F.C., Brown D.A. Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine. J. Neurosci. 21:2001;5535-5545.
29. Main M.J., Cryan J.E., Dupere J.R.B., Cox B., Clare J.J., Burbidge S.A. Modulation of KCNQ2/3 potassium channels by the novel anticonvulsant retigabine. Mol. Pharmacol. 58:2000;253-262.
30. Rundfeldt C., Netzer R. The novel anticonvulsant retigabine activates M-currents in Chinese hamster ovary-cells transfected with human KCNQ2/3 subunits. Neurosci. Lett. 282:2000;73-76.
31. Wickenden A.D., Yu W.F., Zou A., Jegla T., Wagoner P.K. Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol. Pharmacol. 58:2000;591-600.
32. Malayev A.A., Nelson D.J., Philipson L.H. Mechanism of clofilium block of the human Kv1.5 delayed rectifier potassium channel. Mol. Pharmacol. 47:1995;198-205.
33. Attali B., Romey G., Honore E., Schmid-Alliana A., Mattei M.G., Lesage F., Ricard P., Barhanin J., Lazdunski M. Cloning, functional expression, and regulation of two K+ channels in human T lymphocytes. J. Biol. Chem. 267:1992;8650-8657.