Dissociation of E-4031 from the HERG channel caused by mutations of an amino acid results in greater block at high stimulation frequency

Cardiovascular Research

Volumn 57, Issue 3, 2003, Pages 651-659

  Ishii, Kuniaki ^a   Nagai, Mirei ^a   Takahashi, Masahiro ^a   Endoh, Masao ^a  

^a YAMAGATA UNIVERSITY   (Japan)

Author keywords

Antiarrhythmic agents; Arrhythmia (mechanisms); K channel; Long QT syndrome

Indexed keywords

1 [2 (6 METHYL 2 PYRIDYL)ETHYL] 4 (4 METHYLSULFONYLAMINOBENZOYL)PIPERIDINE; 1' (6 CYANO 1,2,3,4 TETRAHYDRO 2 NAPHTHYL) 3,4 DIHYDRO 6 METHANESULFONAMIDOSPIRO[2H 1 BENZOPYRAN 2,4' PIPERIDIN] 4 OL; DOFETILIDE; ISOLEUCINE; PHENYLALANINE; POTASSIUM CHANNEL; QUINIDINE; SULFONE DERIVATIVE;

ARTICLE; BINDING SITE; CONTROLLED STUDY; DISSOCIATION; DRUG EFFECT; GENE MUTATION; MICROELECTRODE; MOLECULAR BIOLOGY; NONHUMAN; OOCYTE; PRIORITY JOURNAL; STIMULATION; VOLTAGE CLAMP; WILD TYPE; XENOPUS;

ANIMALS; ANTI-ARRHYTHMIA AGENTS; CATION TRANSPORT PROTEINS; DOSE-RESPONSE RELATIONSHIP, DRUG; ETHER-A-GO-GO POTASSIUM CHANNELS; ISOLEUCINE; LONG QT SYNDROME; MUTAGENESIS, SITE-DIRECTED; OOCYTES; PATCH-CLAMP TECHNIQUES; PHENETHYLAMINES; PIPERIDINES; POINT MUTATION; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PYRIDINES; SULFONAMIDES; XENOPUS;

EID: 0037371557     PISSN: 00086363     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0008-6363(02)00774-5     Document Type: Article

References (26)

1. Gwilt M., Arrowsmith J.E., Blackburn K.J., et al. UK-68,798: a novel, potent and highly selective class III antiarrhythmic agent which blocks potassium channels in cardiac cells. J Pharmacol Exp Ther. 256:1991;318-324.
2. + current. Differential sensitivity to block by class III antiarrhythmic agents. J Gen Physiol. 96:1990;195-215.
3. Lynch J.J. Jr., Wallace A.A., Stupienski R.F., et al. Cardiac electrophysiologic and antiarrhythmic actions of two long-acting spirobenzopyran piperidine class III agents, L-702,958 and L-706,000 [MK-499]. J Pharmacol Exp Ther. 269:1994;541-554.
4. Kr potassium channel. Cell. 81:1995;299-307.
5. Trudeau M.C., Warmke J.W., Ganetzky B., Robertson G.A. HERG, a human inward rectifier in the voltage-gated potassium channel family. Science. 269:1995;92-95.
6. Roden D.M. Current status of class III antiarrhythmic drug therapy. Am J Cardiol. 72:1993;44B-49B.
7. k blocking drug, UK-68,798: potent in guinea pig but no effect in rat myocardium. J Cardiovasc Pharmacol. 16:1990;401-410.
8. Hondeghem L.M., Snyders D.J. Class III antiarrhythmic agents have a lot of potential but a long way to go. Reduced effectiveness and dangers of reverse use dependence. Circulation. 81:1990;686-690.
9. + current by dofetilide. Circ Res. 72:1993;75-83.
10. Mitcheson J.S., Chen J., Sanguinetti M.C. Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate. J Gen Physiol. 115:2000;229-240.
11. Herzberg I.M., Trudeau M.C., Robertson G.A. Transfer of rapid inactivation and sensitivity to the class III antiarrhythmic drug E-4031 from HERG to M-eag channels. J Physiol (Lond). 511:1998;3-14.
12. + channels. Circ Res. 82:1998;386-395.
13. Lees-Miller J.P., Duan Y., Teng G.Q., Duff H.J. Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites. Mol Pharmacol. 57:2000;367-374.
14. Mitcheson J.S., Chen J., Lin M., Culberson C., Sanguinetti M.C. A structural basis for drug-induced long QT syndrome. Proc Natl Acad Sci USA. 97:2000;12329-12333.
15. Ishii K., Kondo K., Takahashi M., Kimura M., Endoh M. An amino acid residue whose change by mutation affects drug binding to the HERG channel. FEBS Lett. 506:2001;191-195.
16. + channel determined by construction of multimeric cDNAs. Neuron. 9:1992;861-871.
17. + channel, rat Kv1.4, has two potential domains that could produce rapid inactivation. J Biol Chem. 272:1997;19333-19338.
18. Wang J., Trudeau M.C., Zappia A.M., Robertson G.A. Regulation of deactivation by an amino terminal domain in human ether-a-go-go-related gene potassium channels. J Gen Physiol. 112:1998;637-647.
19. + current in cardiac myocytes by dofetilide. J Pharmacol Exp Ther. 262:1992;809-817.
20. + current in rabbit ventricular myocytes. Cardiovasc Drugs Ther. 7:1993;599-604.
21. Kiehn J., Lacerda A.E., Wible B., Brown A.M. Molecular physiology and pharmacology of HERG. Single-channel currents and block by dofetilide. Circulation. 94:1996;2572-2579.
22. Snyders D.J., Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol Pharmacol. 49:1996;949-955.
23. Kr) in AT-1 cells. Concentration-, time-, voltage-, and use-dependent effects. Circulation. 91:1995;1799-1806.
24. + channel. Open-channel block by methanesulfonanilides. Circ Res. 78:1996;499-503.
25. + channels: evidence for a trap door mechanism of activation gating. J Gen Physiol. 109:1997;527-535.
26. + conduction and selectivity. Science. 280:1998;69-77.