High-throughput technologies for studying potassium channels - Progresses and challenges

Drug Discovery Today: TARGETS

Volumn 3, Issue 1, 2004, Pages 32-38

  Xu, Jia ^a   Chen, Ying ^b   Li, Min ^b  

^a AVIVA Biosciences Corporation   (United States)

^b JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

POTASSIUM CHANNEL;

CELLULAR DISTRIBUTION; DRUG INDUSTRY; DRUG TARGETING; ELECTROPHYSIOLOGY; FLUORESCENCE; GENOMICS; HIGH THROUGHPUT SCREENING; HUMAN; IMPEDANCE; ION CURRENT; MEDICAL RESEARCH; NONHUMAN; PROTEIN STRUCTURE; REVIEW; SPECTROSCOPY; STRUCTURE ANALYSIS; VOLTAGE CLAMP;

EID: 10044275839     PISSN: 17418372     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1741-8372(04)02394-1     Document Type: Review

References (39)

1. Hopkins A.L., Groom C.R. The druggable genome. Nat. Rev. Drug Discov. 1:2002;727-730
2. Drews J. Drug discovery: a historical perspective. Science. 287:2000;1960-1964
3. Chen, Y. and Li, M. www.molecularinteraction.org
4. Jan L.Y., Jan Y.N. Cloned potassium channels from eukaryotes and prokaryotes. Annu. Rev. Neurosci. 20:1997;91-123
5. Jan L.Y., Jan Y.N. Structural elements involved in specific K+ channel functions. Annu. Rev. Physiol. 54:1992;537-555
6. Li M., et al. Specification of subunit assembly by the hydrophilic amino-terminal domain of the Shaker potassium channel. Science. 257:1992;1225-1230
7. Coetzee W.A., et al. Molecular diversity of K+ channels. Ann. N. Y. Acad. Sci. 868:1999;233-285
8. Ford J.W., et al. Potassium channels: gene family, therapeutic relevance, high-throughput screening technologies and drug discovery. Prog. Drug Res. 58:2002;133-168
9. Curran M.E. Potassium ion channels and human disease: phenotypes to drug targets? Curr. Opin. Biotechnol. 9:1998;565-572
10. Sanguinetti M.C., et al. Spectrum of HERG K+-channel dysfunction in an inherited cardiac arrhythmia. Proc. Natl. Acad. Sci. U. S. A. 93:1996;2208-2212
11. Derst C., et al. Mutations in the ROMK gene in antenatal Bartter syndrome are associated with impaired K+ channel function. Biochem. Biophys. Res. Commun. 230:1997;641-645
12. Mu D., et al. Genomic amplification and oncogenic properties of the KCNK9 potassium channel gene. Cancer Cell. 3:2003;297-302
13. Schmalhofer W.A., et al. Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties. Biochemistry. 41:2002;7781-7794
14. Miao S., et al. Benzamide derivatives as blockers of Kv1.3 ion channel. Bioorg. Med. Chem. Lett. 13:2003;1161-1164
15. Cai Y.C., Douglass J. In vivo and in vitro phosphorylation of the T lymphocyte type n (Kv1.3) potassium channel. J. Biol. Chem. 268:1993;23720-23727
16. Koster J.C., et al. Hyperinsulinism induced by targeted suppression of beta cell KATP channels. Proc. Natl. Acad. Sci. U. S. A. 99:2002;16992-16997
17. De Ponti F., et al. QT-interval prolongation by non-cardiac drugs: lessons to be learned from recent experience. Eur. J. Clin. Pharmacol. 56:2000;1-18
18. Antzelevitch C., Shimizu W. Cellular mechanisms underlying the long QT syndrome. Curr. Opin. Cardiol. 17:2002;43-51
19. Woosley, R.L. and Singh, S.N. (2000) Arrhythmia Treatment and Therapy: Evaluation of Clinical Trial Evidence, Dekker, New York
20. Xu J., et al. Ion-channel assay technologies: quo vadis? Drug Discov. Today. 6:2001;1278-1287
21. Worley, J.F. 3rd and Main, M.J. (2002) An industrial perspective on utilizing functional ion channel assays for high throughput screening, Receptors Channels 8, 269-282
22. Kostyuk P.G., et al. Effect of internal fluoride and phosphate on membrane currents during intracellular dialysis of nerve cells. Nature. 257:1975;691-693
23. Kostyuk P.G., et al. Asymmetrical displacement currents in nerve cell membrane and effect of internal fluoride. Nature. 267:1977;70-72
24. Lorenson M.Y., et al. Calcium release from pituitary secretory granules: modulation by thiols, disulfides, and dihydropyridine calcium channel blockers. Endocrinology. 126:1990;2671-2678
25. Romani A., Scarpa A. Hormonal control of Mg2+ transport in the heart. Nature. 346:1990;841-844
26. Simons T.J. Calcium-dependent zinc efflux in human red blood cells. J. Membr. Biol. 123:1991;73-82
27. 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
28. Tang W., et al. Development and evaluation of high throughput functional assay methods for HERG potassium channel. J. Biomol. Screen. 6:2001;325-331
29. Tang W., et al. Functional expression of a vertebrate inwardly rectifying K+ channel in yeast. Mol. Biol. Cell. 6:1995;1231-1240
30. Han X., Wang E. Ion-channel sensing of ferricyanide anion based on a supported bilayer lipid membrane. Anal. Sci. 17:2001;1171-1174
31. Chadwick C.C., et al. Identification of a specific radioligand for the cardiac rapidly activating delayed rectifier K+ channel. Circ. Res. 72:1993;707-714
32. Papadatos G.A., et al. Slowed conduction and ventricular tachycardia after targeted disruption of the cardiac sodium channel gene Scn5a. Proc. Natl. Acad. Sci. U. S. A. 99:2002;6210-6215
33. Guyton and Authur (1991) Textbook of Medical Physiology (8th edn), W.B. Saunders
34. Doyle D.A., et al. The structure of the potassium channel: molecular basis of K+ conduction and selectivity. Science. 280:1998;69-77
35. Li M., et al. Assembly of potassium channels. Ann. N. Y. Acad. Sci. 707:1993;51-59
36. Xu J., et al. Assembly of voltage-gated potassium channels. Conserved hydrophilic motifs determine subfamily-specific interactions between the alpha- subunits. J. Biol. Chem. 270:1995;24761-24768
37. Loo T.W., Clarke D.M. Correction of defective protein kinesis of human P-glycoprotein mutants by substrates and modulators. J. Biol. Chem. 272:1997;709-712
38. Ficker E., et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J. Biol. Chem. 277:2002;4989-4998
39. Sanguinetti M.C., et al. A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell. 81:1995;299-307