Kinetics of drug interaction with the Kv11.1 potassium channel

Molecular Pharmacology

Volumn 85, Issue 5, 2014, Pages 769-776

  Hill, Adam P ^a,b   Perrin, Mark J ^c   Heide, Juliane ^a,b   Campbell, Terence J ^a,b   Mann, Stefan A ^a,b   Vandenberg, Jamie I ^a,b  

^a VICTOR CHANG CARDIAC RESEARCH INSTITUTE   (Australia)

^b UNIVERSITY OF NEW SOUTH WALES   (Australia)

^c BARWON HEALTH   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

CLOZAPINE; POTASSIUM CHANNEL KV11.1; UNCLASSIFIED DRUG; VOLTAGE GATED POTASSIUM CHANNEL;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; DRUG DIFFUSION; DRUG PROTEIN BINDING; FEMALE; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; CELLS, CULTURED; CHO CELLS; CLOZAPINE; CRICETINAE; CRICETULUS; DRUG INTERACTIONS; ETHER-A-GO-GO POTASSIUM CHANNELS; KINETICS; MEMBRANE POTENTIALS; POTASSIUM CHANNEL BLOCKERS;

EID: 84897433375     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.114.091835     Document Type: Article

References (31)

1. Brennan T, Fink M, and Rodriguez B (2009) Multiscale modelling of drug-induced effects on cardiac electrophysiological activity. Eur J Pharm Sci 36:62-77.
2. Carmeliet E (1992) Voltage-and time-dependent block of the delayed K+ current in cardiac myocytes by dofetilide. J Pharmacol Exp Ther 262:809-817.
3. Colquhoun D, Dowsland KA, Beato M, and Plested AJR (2004) How to impose microscopic reversibility in complex reaction mechanisms. Biophys J 86:3510-3518.
4. Di Veroli GY, Davies MR, Zhang H, Abi-Gerges N, and Boyett MR (2013a) hERG inhibitors with similar potency but different binding kinetics do not pose the same proarrhythmic risk: Implications for drug safety assessment. J Cardiovasc Electrophysiol DOI: 10.1111/jce.12289 [published ahead of print].
5. Di Veroli GY, Davies MR, Zhang H, Abi-Gerges N, and Boyett MR (2013b) Highthroughput screening of drug-binding dynamics to HERG improves early drug safety assessment. Am J Physiol Heart Circ Physiol 304:H104-H117.
6. Ficker E, Jarolimek W, Kiehn J, Baumann A, and Brown AM (1998) Molecular determinants of dofetilide block of HERG K+ channels. Circ Res 82:386-395.
7. Hille B (2001) Classical mechanisms of block, in Ionic Channels of excitable membranes, 3rd ed, pp 503-537, Sinauer Associates, Inc., Sunderland, MA.
8. Kamiya K, Niwa R, Morishima M, Honjo H, and Sanguinetti MC (2008) Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci 108:301-307.
9. Kirsch GE, Trepakova ES, Brimecombe JC, Sidach SS, Erickson HD, Kochan MC, Shyjka LM, Lacerda AE, and Brown AM (2004) Variability in the measurement of hERG potassium channel inhibition: effects of temperature and stimulus pattern. J Pharmacol Toxicol Methods 50:93-101.
10. Lee SY, Kim YJ, Kim KT, Choe H, and Jo SH (2006) Blockade of HERG human K1 channels and IKr of guinea-pig cardiomyocytes by the antipsychotic drug clozapine. Br J Pharmacol 148:499-509 Wiley Online Library.
11. Lieberman JA, Stroup TS, McEvoy JP, Swartz MS, Rosenheck RA, Perkins DO, Keefe RS, Davis SM, Davis CE, and Lebowitz BD et al.; Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE) Investigators (2005) Effectiveness of antipsychotic drugs in patients with chronic schizophrenia. N Engl J Med 353: 1209-1223 Mass Medical Soc.
12. Lu Y, Mahaut-Smith MP, Varghese A, Huang CL, Kemp PR, and Vandenberg JI (2001) Effects of premature stimulation on HERG K(+) channels. J Physiol 537: 843-851.
13. Milnes JT, Crociani O, Arcangeli A, Hancox JC, and Witchel HJ (2003) Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652. Br J Pharmacol 139:887-898.
14. Milnes JT, Witchel HJ, Leaney JL, Leishman DJ, and Hancox JC (2010) Investigating dynamic protocol-dependence of hERG potassium channel inhibition at 37 degrees C: Cisapride versus dofetilide. J Pharmacol Toxicol Methods 61: 178-191.
15. Mitcheson JS, Chen J, and Sanguinetti MC (2000) Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate. J Gen Physiol 115:229-240.
16. Olofsson J, Pihl J, Sinclair J, Sahlin E, Karlsson M, and Orwar O (2004) A microfluidics approach to the problem of creating separate solution environments accessible from macroscopic volumes. Anal Chem 76:4968-4976.
17. Paul AA, Witchel HJ, and Hancox JC (2002) Inhibition of the current of heterologously expressed HERG potassium channels by flecainide and comparison with quinidine, propafenone and lignocaine. Br J Pharmacol 136:717-729.
18. Perrin MJ, Kuchel PW, Campbell TJ, and Vandenberg JI (2008) Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels. Mol Pharmacol 74:1443-1452.
19. Ray WA, Chung CP, Murray KT, Hall K, and Stein CM (2009) Atypical antipsychotic drugs and the risk of sudden cardiac death. N Engl J Med 360:225-235.
20. Redfern WS, Carlsson L, Davis AS, Lynch WG, MacKenzie I, Palethorpe S, Siegl PKS, Strang I, Sullivan AT, and Wallis R et al. (2003) Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development. Cardiovasc Res 58:32-45.
21. Roden DM and Hoffman BF (1985) Action potential prolongation and induction of abnormal automaticity by low quinidine concentrations in canine Purkinje fibers. Relationship to potassium and cycle length. Circ Res 56: 857-867.
22. Roden DM (2004) Drug-induced prolongation of the QT interval. N Engl J Med 350: 1013-1022.
23. Saiz J, Gomis-Tena J, Monserrat M, Ferrero JM, Jr, Cardona K, and Chorro J (2011) Effects of the antiarrhythmic drug dofetilide on transmural dispersion of repolarization in ventriculum. A computer modeling study. IEEE Trans Biomed Eng 58:43-53.
24. Sanguinetti MC, Jiang C, Curran ME, and Keating MT (1995) A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell 81:299-307.
25. Smith PL, Baukrowitz T, and Yellen G (1996) The inward rectification mechanism of the HERG cardiac potassium channel. Nature 379:833-836.
26. Vandenberg JI, Perry MD, Perrin MJ, Mann SA, Ke Y, and Hill AP (2012) hERG K(+) channels: structure, function, and clinical significance. Physiol Rev 92: 1393-1478.
27. Vandenberg JI, Varghese A, Lu Y, Bursill JA, Mahaut-Smith MP, and Huang CL-H (2006) Temperature dependence of human ether-a-go-go-related gene K+ currents. Am J Physiol Cell Physiol 291:C165-C175.
28. Walker BD, Singleton CB, Bursill JA, Wyse KR, Valenzuela SM, Qiu MR, Breit SN, and Campbell TJ (1999) Inhibition of the human ether-a-go-go-related gene (HERG) potassium channel by cisapride: affinity for open and inactivated states. Br J Pharmacol 128:444-450.
29. Weerapura M, Hébert TE, and Nattel S (2002) Dofetilide block involves interactions with open and inactivated states of HERG channels. Pflugers Arch 443:520-531.
30. Witchel HJ, Dempsey CE, Sessions RB, PerryM, Milnes JT, Hancox JC, andMitcheson JS (2004) The low-potency, voltage-dependent HERG blocker propafenone-molecular determinants and drug trapping. Mol Pharmacol 66:1201-1212.
31. Zhou Q, Zygmunt AC, Cordeiro JM, Siso-Nadal F, Miller RE, Buzzard GT, and Fox JJ (2009) Identification of Ikr kinetics and drug binding in native myocytes. Ann Biomed Eng 37:1294-1309.