Application of PatchXpress planar patch clamp technology to the screening of new drug candidates for cardiac KCNQ1/KCNE1 (IKs) activity

Assay and Drug Development Technologies

Volumn 5, Issue 5, 2007, Pages 617-628

  Trepakova, Elena S ^a   Malik, Manish G ^a   Imredy, John P ^a   Penniman, Jacob R ^a   Dech, Spencer J ^a   Salata, Joseph J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

POTASSIUM CHANNEL KCNQ1; CARDIOVASCULAR AGENT; KCNE1 PROTEIN, HUMAN; KCNH1 PROTEIN, HUMAN; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG; VOLTAGE GATED POTASSIUM CHANNEL;

ANIMAL CELL; ARTICLE; CELL STRAIN HEK293; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG SCREENING; ELECTROPHYSIOLOGY; EMBRYO; FEMALE; GENETIC CODE; HEART CONTRACTION; HEART MUSCLE CELL; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; NONHUMAN; PATCH CLAMP; PROTEIN EXPRESSION; VALIDATION PROCESS; ANIMAL; CELL LINE; CHEMISTRY; CHO CELL; CRICETULUS; DRUG EFFECT; GUINEA PIG; HAMSTER; IN VITRO STUDY; INSTRUMENTATION; STATISTICAL ANALYSIS;

ANIMALS; CARDIOVASCULAR AGENTS; CELL LINE; CHEMISTRY, PHARMACEUTICAL; CHO CELLS; CRICETINAE; CRICETULUS; DATA INTERPRETATION, STATISTICAL; DRUG EVALUATION, PRECLINICAL; ELECTROPHYSIOLOGY; ETHER-A-GO-GO POTASSIUM CHANNELS; GUINEA PIGS; HUMANS; KCNQ1 POTASSIUM CHANNEL; MYOCYTES, CARDIAC; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNELS, VOLTAGE-GATED;

EID: 35348959556     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2007.091     Document Type: Article

References (35)

1. Kr potassium channel. Cell 1995;81:299-307.
2. International Conference on Harmonization; S7B guidance on nonclinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals. Notice. Fed Regist 2005 October 20;70:61133-61134.
3. Ks potassium channel. Nature 1996;384:80-83.
4. Ks cardiac potassium current. Nature 1996;384:78-80.
5. + current is composed of two currents in guinea pig atrial cells. Am J Physiol 1991;260:393-399.
6. Ks contributes to the longer action potential of the M cell. Circ Res 1995;76:351-365.
7. Suzuki A, Bosnjak ZJ, Kwok WM: The effects of isoflurane on the cardiac slowly activating delayed-rectifier potassium channel in guinea pig ventricular myocytes. Anesth Analg 2003;96:1308-1315.
8. Tsuji Y, Opthof T, Kamiya K, Yasui K, Liu W, Lu Z, Kodama I: Pacing-induced heart failure causes a reduction of delayed rectifier potassium currents along with decreases in calcium and transient outward currents in rabbit ventricle. Cardiovasc Res 2000;48:300-309.
9. Ks to canine ventricular repolarization: key role for beta-adrenergic receptor stimulation. Circulation 2003;107:2753-2760.
10. Ks in human ventricular muscle. Circulation 2005;112:1392-1399.
11. Roden DM, Lazzara R, Rosen M, Schwartz PJ, Towbin J, Vincent GM: Multiple mechanisms in the long-QT syndrome. Current knowledge, gaps, and future directions. The SADS Foundation Task Force on LQTS. Circulation 1996;94:1996-2012.
12. Wang Q, Curran ME, Splawski I, Burn TC, Millholland JM, VanRaay TJ, et al.: Positional cloning of a novel potassium channel gene: KVLQT1 mutations cause cardiac arrhythmias. Nat Genet 1996;12:17-23.
13. + current, on repolarization in human and guinea pig ventricular myocytes. Cardiovasc Res 1998;38:441-450.
14. Finley MR, Li Y, Hua F, Lillich J, Mitchell KE, Ganta S, et al.: Expression and coassociation of ERG1, KCNQ1, and KCNE1 potassium channel proteins in horse heart. Am J Physiol Heart Circ Physiol 2002;283:H126-H138.
15. Shimizu W, Antzelevitch C: Cellular basis for the ECG features of the LQT1 form of the long-QT syndrome: effects of beta-adrenergic agonists and antagonists and sodium channel blockers on transmural dispersion of repolarization and torsades de pointes. Circulation 1998;98:2314-2322.
16. Ks: potential for antiarrhythmic therapy. Curr Med Chem 2004;11:29-44.
17. Kurokawa J, Chen L, Kass RS: Requirement of subunit expression for cAMP-mediated regulation of a heart potassium channel. Proc Natl Acad Sci U S A 2003;100:2122-2127.
18. +-current by dofetilide. Circ Res 1993;72:75-83.
19. Ks blockade reduces dispersion of repolarization in heart failure. Heart Rhythm 2005;2:731-738.
20. Tao H, Santa Ana D, Guia A, Huang M, Ligutti J, Walker G, et al.: Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol 2004;2:497-506.
21. Zheng W, Spencer RH, Kiss L: High throughput assay technologies for ion channel drug discovery. Assay Drug Dev Technol 2004;2:543-552.
22. Mathes C: QPatch: the past, present and future of automated patch clamp. Expert Opin Ther Targets 2006;10:319-327.
23. Dubin AE, Nasser N, Rohrbacher J, Hermans AN, Marrannes R, Grantham C, et al.: Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp. J Biomol Screen 2005;10:168-181.
24. Guo L, Guthrie H: Automated electrophysiology in the preclinical evaluation of drugs for potential QT prolongation. J Pharmacol Toxicol Methods 2005;52:123-135.
25. Ly JQ, Shyy G, Misner DL: Assessing hERG channel inhibition using PatchXpress. J Assoc Lab Automation 2005;10:225-230.
26. Imredy JP, Irving WD, Clouse HK, Salata JJ: Electrophysiological and pharmacological characterization of a cell line stably expressing hKCNQ1 and hKCNE1 potassium channels [abstract]. Biophys J 2004;86:A98.
27. Salata JJ, Jurkiewicz NK, Wallace AA, Stupienski RF, Guinosso PJ, Lynch JJ: Cardiac electrophysiological actions of the histamine H-1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ Res 1995;76:110-119.
28. Yu SP, Kerchner GA: Endogenous voltage-gated potassium channels in human embryonic kidney (HEK293) cells. J Neurosci Res 1998;52:612-617.
29. Zhu GY, Zhang Y, Xu HX, Jiang C: Identification of endogenous outward currents in the human embryonic kidney (HEK 293) cell line. J Neurosci Methods 1998;81:73-83.
30. Fermini B, Jurkiewicz NK, Jow B, Guinosso PJ, Baskin EP, Lynch JJ, et al.: Use-dependent effects of the class-III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization - block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol 1995;26:259-271.
31. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ: Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 1981;391:85-100.
32. Ks. Am J Physiol Heart Circ Physiol 1996;40:H2477-H2489.
33. Trepakova ES, Dech SJ, Salata JJ: Flunarizine is a highly potent inhibitor of cardiac hERG potassium current. J Cardiovasc Pharmacol 2006;47:211-220.
34. + current in single canine cardiac Purkinje-cells. Am J Physiol 1992;262:H1197-H1207.
35. Ks channel complex inhibits drug block-novel mechanism underlying variable antiarrhythmic drug actions. Circulation 2003;108:132-134.