High affinity HERG K + channel blockade by the antiarrhythmic agent dronedarone: Resistance to mutations of the S6 residues Y652 and F656

Biochemical and Biophysical Research Communications

Volumn 325, Issue 3, 2004, Pages 883-891

  Ridley, John M ^a   Milnes, James T ^a   Witchel, Harry J ^a   Hancox, Jules C ^a  

^a SCHOOL OF MEDICAL SCIENCES   (United Kingdom)

Author keywords

Acquired long QT syndrome; Amiodarone; Antiarrhythmic; Delayed rectifier; Dronedarone; F656; F656A; Human ether a go go related gene; I Kr; Long QT syndrome; Potassium channel; QT prolongation; Y652; Y652A

Indexed keywords

ALANINE; AMINO ACID; AMIODARONE; ANTIARRHYTHMIC AGENT; AROMATIC AMINO ACID; DRONEDARONE; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL HERG; POTASSIUM ION;

ARTICLE; BINDING AFFINITY; CELL LINE; CELL MEMBRANE DEPOLARIZATION; CHANNEL GATING; CONTROLLED STUDY; DRUG POTENCY; HUMAN; HUMAN CELL; IC 50; INHIBITION KINETICS; MAMMAL CELL; MEASUREMENT; MUTAGENESIS; MUTATION; PRIORITY JOURNAL; TEMPERATURE; WILD TYPE;

AMINO ACID SUBSTITUTION; AMIODARONE; ANTI-ARRHYTHMIA AGENTS; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG RESISTANCE; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; ION CHANNEL GATING; KIDNEY; MEMBRANE POTENTIALS; MUTAGENESIS, SITE-DIRECTED; POTASSIUM CHANNELS, VOLTAGE-GATED; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

MAMMALIA;

EID: 8444244427     PISSN: 0006291X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bbrc.2004.10.127     Document Type: Article

References (29)

1. Kr potassium channel Cell 81 1995 299 307
2. M.C. Trudeau, J.W. Warmke, B. Ganetzky, and G.A. Robertson HERG, a human inward rectifier in the voltage-gated potassium channel family Science 269 1995 92 95
3. + channels: friend and foe Trends Pharmacol. Sci. 22 2001 240 246
4. J.S. Mitcheson, and M.D. Perry Molecular determinants of high-affinity drug binding to HERG channels Curr. Opin. Drug Discov. Dev. 6 2003 667 674
5. J.S. Mitcheson, J. Chen, and M.C. Sanguinetti Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate J. Gen. Physiol. 115 2000 229 240
6. J.P. Lees-Miller, Y. Duan, G.Q. Teng, and H.J. Duff Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites Mol. Pharmacol. 57 2000 367 374
7. J.S. Mitcheson, J. Chen, M. Lin, C. Culberson, and M.C. Sanguinetti A structural basis for drug-induced long QT syndrome Proc. Natl. Acad. Sci. USA 97 2000 12329 12333
8. J. Chen, G. Seebohm, and M.C. Sanguinetti Position of aromatic residues in the S6 domain, not inactivation, dictates cisapride sensitivity of HERG and eag potassium channels Proc. Natl. Acad. Sci. USA 99 2002 12461 12466
9. J.A. Sanchez-Chapula, T. Ferrer, R.A. Navarro-Polanco, and M.C. Sanguinetti Voltage-dependent profile of human ether-a-go-go-related gene channel block is influenced by a single residue in the S6 transmembrane domain Mol. Pharmacol. 63 2003 1051 1058
10. + channels by vesnarinone Mol. Pharmacol. 60 2001 244 253
11. I. Kodama, K. Kamiya, and J. Toyama Cellular electropharmacology of amiodarone Cardiovasc. Res. 35 1997 13 29
12. S.A. Doggrell Amiodarone-waxed and waned and waxed again Expert Opin. Pharmacother. 2 2001 1877 1890
13. S.A. Doggrell, and J.C. Hancox Dronedarone: an amiodarone analogue Expert Opin. Invest. Drugs 13 2004 415 426
14. A. Varro, J. Takacs, M. Nemeth, O. Hala, L. Virag, N. Iost, B. Balati, M. Agoston, A. Vereckei, G. Pastor, M. Delbruyere, P. Gautier, D. Nisato, and J.G. Papp Electrophysiological effects of dronedarone (SR 33589), a noniodinated amiodarone derivative in the canine heart: comparison with amiodarone Br. J. Pharmacol. 133 2001 625 634
15. P. Gautier, E. Guillemare, A. Marion, J.P. Bertrand, Y. Tourneur, and D. Nisato Electrophysiologic characterization of dronedarone in Guinea pig ventricular cells J. Cardiovasc. Pharmacol. 41 2003 191 202
16. + current, HERG and KvLQT1/minK potassium channels Br. J. Pharmacol. 140 2003 996 1002
17. S.S. Po, D.W. Wang, I.C. Yang, J.P.J. Johnson, L. Nie, and P.B. Bennett Modulation of HERG potassium channels by extracellular magnesium and quinidine J. Cardiovasc. Pharmacol. 33 1999 181 185
18. M. Weerapura, S. Nattel, D. Chartier, R. Caballero, and T.E. Hebert A comparison of currents carried by HERG, with and without coexpression of MiRP1, and the native rapid delayed rectifier current. Is MiRP1 the missing link? J. Physiol. 540 2002 15 27
19. J.T. Milnes, O. Crociani, A. Arcangeli, J.C. Hancox, and H.J. Witchel Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652 Br. J. Pharmacol. 139 2003 887 898
20. Z. Zhou, Q. Gong, B. Ye, Z. Fan, J.C. Makielski, G.A. Robertson, and C.T. January Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature Biophys. J. 74 1998 230 241
21. + channel J. Mol. Cell. Cardiol. 36 2004 701 705
22. J.T. Milnes, C.E. Dempsey, J.M. Ridley, O. Crociani, A. Arcangeli, J.C. Hancox, and H.J. Witchel Preferential closed channel blockade of HERG potassium currents by chemically synthesised BeKm-1 scorpion toxin FEBS Lett. 547 2003 20 26
23. + current and prolongation of the guinea-pig ventricular action potential by 4-aminopyridine J. Physiol. 549 2003 667 672
24. J. Kiehn, D. Thomas, C.A. Karle, W. Schols, and W. Kubler Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels Naunyn Schmiedebergs Arch. Pharmacol. 359 1999 212 219
25. + channels J. Pharmacol. Sci. 95 2004 311 319
26. + channels expressed in mammalian cell lines and Xenopus oocytes J. Pharmacol. Toxicol. Methods 48 2002 65 80
27. P. Gautier, E. Guillemare, L. Djandjighian, A. Marion, J. Planchenault, C. Bernhart, J.M. Herbert, and D. Nisato In vivo and in vitro characterization of the novel antiarrhythmic agent SSR149744C: electrophysiological, anti-adrenergic, and anti-angiotensin II effects J. Cardiovasc. Pharmacol. 44 2004 244 257
28. o and C-type inactivation FEBS Lett. 417 1997 43 47
29. M. Perry, M.J. De Groot, R. Helliwell, D. Leishman, M. Tristani-Firouzi, M.C. Sanguinetti, and J. Mitcheson Structural determinants of HERG channel block by clofilium and ibutilide Mol. Pharmacol. 66 2004 240 249