Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: Involvement of S6 sites

Molecular Pharmacology

Volumn 57, Issue 2, 2000, Pages 367-374

  Lees Miller, James P ^a   Duan, Yanjun ^a   Teng, Guo Qi ^a   Duff, Henry J ^a  

^a UNIVERSITY OF CALGARY   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOPYRIDINE; DOFETILIDE; PHENYLALANINE; QUINIDINE; TETRYLAMMONIUM;

ALLOSTERISM; AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; DRUG PROTEIN BINDING; GENE EXPRESSION REGULATION; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; XENOPUS;

AMINO ACID MOTIFS; AMINO ACID SUBSTITUTION; ANIMALS; ANTI-ARRHYTHMIA AGENTS; BINDING SITES; CATION TRANSPORT PROTEINS; ETHER-A-GO-GO POTASSIUM CHANNELS; MODELS, BIOLOGICAL; MUTATION; OOCYTES; PHENETHYLAMINES; PHENYLALANINE; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; QUINIDINE; RECOMBINANT PROTEINS; SULFONAMIDES; TETRAETHYLAMMONIUM; XENOPUS LAEVIS;

EID: 0033952902     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. 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.
2. CAST Investigators Preliminary Report: Effect of encainide and flecainide on mortality in a randomized trial of arrhythmia suppression after myocardial infarction. Cardiac Arrhythmias Suppression Trial (CAST). N Engl J Med (1989) 321:406-412.
3. Choi KL, Mossman C, Aube J and Yellen G (1993) The internal quaternary ammonium receptor site of shaker potassium channels. Neuron 10:533-541.
4. Curran ME, Splawski I, Timothy KW, Vincent GM, Green ED and Keating MT (1995) A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome. Cell 80:795-803.
5. Diamond (1996) Antiarrhythmic trials: Danish investigations of arrhythmias and mortality on dofetilde. Lancet 348:1597-1598.
6. Doyle DA, Cabrai JM, Pfuetzner RA, Kuo A, Gulbis JM, Cohen SL, Chait BT and MacKinnon R (1998) The Structure of the potassium channel: molecular basis of K+ conduction and selectivity. Science (Wash DC) 280:69-77.
7. + channels. Circ Res 82:386-395.
8. Herzberg IM, Trudeau MC and Robertson GA (1998) Transfer of rapid inactivation and sensitivity to the class III antiarrhythmic drug E-4031 from HERG to M-eag channels. J Physiol (Lond) 511:3-14.
9. Ho SN, Hunt HD, Horton RM, Pullen JK and Pease LR (1989) Site-directed mutagenesis by overlap extension using the polymerase chain reaction. Gene 77:51-59.
10. Hockerman, Johnson BD, Scheuer T and Catterall WA (1995) Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels. J Biol Chem 270:22119-22122.
11. Jurkiewicz NK and Sanguinetti MC (1993) Rate-dependent prolongation of cardiac action potentials by a methanesulfonanilide Class III antiarrhythmic agent: Specific block of rapidly activating delayed rectifier K current by dofetilide. Circ Res 72:75-83.
12. Kiehn J, Lacerda AE, Wible B and Brown AM (1996) Molecular physiology and pharmacology of HERG. Single-channel currents and block by dofetilide. Circulation 94:2572-2579.
13. Lees-Miller JP, Kondo C, Duff HJ and Wang L (1997) Electrophysiological characterization of an alternatively processed ERG K+ channel in mouse and human hearts. Circ Res 81:719-726.
14. + channel. Neuron 19:175-184.
15. McPhee JC, Ragsdale DS, Scheurer T and Catterall WA (1995) A critical role for transmembrane segment IVS6 of the sodium channel α subumt in fast inactivation. J Biol Chem 270:12025-12034.
16. Minor DL Jr, Masseling SJ, Jan YN and Jan LY (1999) Transmembrane structure of an inwardly rectifying potassium channel. Cell 96:879-891.
17. Peterson BZ, Tanada TN and Catterall WA (1996) Molecular determinants of high affinity dihydropyridine binding in L-type calcium channels. J Biol Chem 271: 5293-5296.
18. + channels by local anesthetics. Science (Wash DC) 265:1724-1728.
19. 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.
20. Shi W, Wang HS, Pan Z, Wymore E, Cohen I, McKinnon D and Dixon J (1998) Cloning of a mammalian elk potassium channel gene and EAG mRNA distribution in rat sympathetic ganglia. J Physiol (Lond) 511:675-682.
21. Shi W, Wymore RS, Wang HS, Pan Z, Cohen IS, McKinnon D and Dixon JE (1997) Identification of two nervous system-specific members of the erg potassium channel gene family. J Neurosci 17:9423-9432.
22. + channels. Biophys J 67:2316-2325.
23. Smith PL, Baukrowitz T and Yellen G (1996) The inward rectification mechanism of the HERG cardiac potassium channel. Nature (Lond) 379:833-835.
24. Snyders DJ and Chaudhary A (1996) High affinity open channel block by dofetilide of HERG expressed in human cell line. Mol Pharmacol 49:949-955.
25. Spector PS, Curran ME, Keating MT and Sanguinetti MC (1996a) Class III antiarrhythmic drugs block HERG, a human cardiac delayed rectifier K+ channel. Open-channel block by methanesulfonanilides. Circ Res 78:499-503.
26. Spector PS, Curran ME, Zou A, Keating MT and Sanguinetti MC (1996b) Fast inactivation causes rectification of the IKr channel. J Gen Physiol 107:611-619.
27. Splawski I, Shen J, Timothy KW, Vincent GM, Lehmann MH and Keating MT (1998) Genomic structure of three long QT syndrome genes: KVLQT1, HERG, and KCNE1. Genomics 51:86-97.
28. Sword Investigators (1996) Sword trial of sotalol. Lancet 348:827-828.
29. Wang L and Duff HJ (1996) Identification and characteristics of delayed rectifier K+ current in fetal mouse ventricular myocytes. Am J Physiol 270:H2088-H2093.
30. Wang S, Liu S, Morales MJ, Strauss HC and Rasmusson RL (1997) A quantitative analysis of the activation and inactivation kinetics of HERG expressed in Xenopus oocytes. J Physiol (Lond) 502:45-60.
31. Warmke JW and Ganetzky B (1994) A family of potassium channel genes related to EAG in Drosophila and mammals. Proc Natl Acad Sci USA 91:3438-3442.
32. + channel: Role of S6 in antiarrhythmic drug binding. Circ Res 78:1105-1114.
33. Zhang H, ZhuB, Yao JA and Tseng GN (1998) Differential effects of S6 mutations on binding of quinidine and 4-aminopyridine to rat isoforms of Kv 1.4: Common site but different factors in determining blockers binding affinity. J Pharmacol Exp Ther 287:332-343.
34. Zou A, Xu QP and Sanguinetti MC (1998) A mutation in the pore region of HERG K+ channels expressed in Xeriopus oocytes reduces rectification by shifting the voltage dependence of inactivation. J Physiol (Lond) 509:129-137.