Molecular analysis of a binding site for quinidine in a human cardiac delayed rectifier K+ channel: Role of S6 in antiarrhythmic drug binding

Circulation Research

Volumn 78, Issue 6, 1996, Pages 1105-1114

  Yeola, Sarita W ^a   Rich, Tom C ^a   Uebele, Vic N ^a   Tamkun, Michael M ^a   Snyders, Dirk J ^a  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

antiarrhythmic agents; drug binding sites; K+ channels; quinidine; structure function analysis

Indexed keywords

ANTIARRHYTHMIC AGENT; MESSENGER RNA; POTASSIUM CHANNEL; POTASSIUM ION; QUINIDINE; TETRYLAMMONIUM;

AMINO ACID SUBSTITUTION; ARTICLE; CALCIUM CELL LEVEL; CHANNEL GATING; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG BINDING SITE; DRUG MECHANISM; GENE MUTATION; HEART ARRHYTHMIA; HUMAN; HUMAN CELL; L CELL; MOLECULAR BIOLOGY; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS;

EID: 0029976743     PISSN: 00097330     EISSN: None     Source Type: Journal    
DOI: 10.1161/01.RES.78.6.1105     Document Type: Article

References (37)

1. Snyders DJ, Knoth KM, Roberds SL, Tamkun MM. Time-, voltage-, and state-dependent block by quinidine of a cloned human cardiac potassium channel. Mol Pharmacol. 1992;41:322-330.
2. + channel protein in explanted cardiac tissue. J Clin Invest. 1995;96:282-292.
3. + current similar to Kv1.5 cloned channel currents. Circ Res. 1993;73:1061-1076.
4. + channel current. Circ Res. 1993;73:210-216.
5. Cobbe SM. Incidence and risks associated with atrial fibrillation. Pacing Clin Electrophysiol. 1994;17:1005-1010.
6. Armstrong CM. Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons. J Gen Physiol. 1971;58: 413-437.
7. Choi KL, Mossman C, Aube J, Yellen G. The internal quaternary ammonium receptor site of Shaker potassium channels. Neuron. 1993;10:533-541.
8. Chandy KG, Gutman GA. Voltage-gated potassium channel genes. In: Peroutka SJ, ed. Handbook of Receptors and Channels. Boca Raton, Fla: CRC Press; 1994:1-71.
9. Dougerthy DA. Cation-π interactions in chemistry and biology: a new view of benzene, Phe, Tyr and Trp. Science. 1996;271:163-168.
10. Aiyar J, Nguyen AN, Chandy KG, Grissmer S. The P-region and S6 of Kv3.1 contribute to the formation of the ion conduction pathway. Biophys J. 1994;67:2261-2264.
11. Yamagishi T, Ishii K, Taira N. Absence of effects of class III antiarrhythmic agents on cloned cardiac K channels. Jpn J Pharmacol. 1993;61:371-373.
12. + channel currents by quinidine. Circ Res. 1993;73:351-359.
13. Snyders DJ, Tamkun MM, Bennett PB. A rapidly activating and slowly inactivating potassium channel cloned from human heart: functional analysis after stable mammalian cell culture expression. J Gen Physiol. 1993;101:513-543.
14. 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.
15. + channel. Science. 1996; 271:653-656.
16. Valenzuela C, Delpon E, Tamkun MM, Tamargo J, Snyders DJ. Stereoselective block of a human cardiac potassium channel (Kv1.5) by bupivacaine enantiomers. Biophys J. 1995;69:418-427.
17. + channel comprises part of the pore. Nature. 1994;367:179-182.
18. Snyders DJ, Yeola SW. Determinants of antiarrhythmic drug action: electrostatic and hydrophobic components of block of the human cardiac hKv1.5 channel. Circ Res. 1995;77:575-583.
19. + channel. Science. 1991;251:939-942.
20. + channels. Biophys J. 1994;67:2316-2325.
21. Woodhull AM. Ionic blockade of sodium channels in nerve. J Gen Physiol. 1973;61:687-708.
22. + channel subfamily does not prevent expression of currents with wild-type characteristics. FEBS Lett. 1994;340:104-108.
23. + channel behaves like an open-channel blocker. Neuron. 1991;7: 743-753.
24. + channel. Nature. 1991;353:86-90.
25. Hille B. Ionic Channels of Excitable Membranes. 2nd ed. Sunderland, Mass: Sinauer Associates; 1991.
26. Uebele VN, England SK, Chaudhary AC, Tamkun MM, Snyders DJ. Functional differences in Kv1.5 currents expressed in mammalian cell lines are due to the presence of endogenous Kvβ2.1 subunits. J Biol Chem. 1996;271:2406-2412.
27. + channel. Biophys J. 1995;68:448-458.
28. + channels. Science. 1991;251:942-944.
29. + channels by local anesthetics. Science. 1994;265:1724-1728.
30. Snyders DJ, Hondeghem LM. Effects of quinidine on the sodium current of ventricular guinea pig myocytes: evidence for a drug-associated rested state with altered kinetics. Circ Res. 1990;66: 565-579.
31. + channels by a quaternary ammonium ion: catalysis by a transition-intermediate state? J Physiol (Lond). 1993;471:319-341.
32. O'Leary ME, Horn R. Internal block of human heart sodium channels by symmetrical tetra-alkylammoniums. J Gen Physiol. 1994;104:507-522.
33. + channel cloned from human heart. Mol Pharmacol. 1993;44:1240-1245.
34. Yang T, Prakash C, Roden DM, Snyders DJ. Mechanism of block of a human cardiac potassium channel by terfenadine racemate and its enantiomers. Br J Pharmacol. 1995;115:267-274.
35. Wang Z, Fermini B, Nattel S. Effects of flecainide, quinidine, and 4-aminopyridine on transient outward and ultrarapid delayed rectifier currents in human atrial myocytes. J Pharmacol Exp Ther. 1995;272:184-196.
36. Snyders DJ, Rich TC, Mays DJ, Tamkun MM, Yeola SW. Involvement of S6 in voltage-dependent deactivation gating of hKv1.5 potassium channels. Biophys J. 1996;70:A144. Abstract.
37. Franqueza L, Delpón E, Gay P, Snyders DJ, Tamargo J, Valenzuela C. Molecular determinants for stereoselective bupivacaine binding in hKv1.5 channels. Biophys J. 1996;70:A400. Abstract.