Molecular determinants of Kv1.5 channel block by diphenyl phosphine oxide-1

Journal of Molecular and Cellular Cardiology

Volumn 48, Issue 6, 2010, Pages 1111-1120

  Du, Yi mei ^a   Zhang, Xiao xian ^a   Tu, Dan na ^a   Zhao, Ning ^a   Liu, Yan jie ^b   Xiao, Hua ^a   Sanguinetti, Michael C ^c   Zou, Anruo ^a   Liao, Yu hua ^a  

^a UNION HOSPITAL   (China)

^b HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

^c UNIVERSITY OF UTAH SCHOOL OF MEDICINE   (United States)

Author keywords

Atrial fibrillation; Diphenyl phosphine oxide 1; Kv1.5; Potassium channels; Ultra rapid delayed rectifier; Voltage clamp

Indexed keywords

2' (4 METHOXYPHENYLACETAMIDOMETHYL) N [2 (3 PYRIDYL)ETHYL] 2 BIPHENYLCARBOXAMIDE; ALANINE; DIPHENYLPHOSPHINE OXIDE 1; ISOLEUCINE; LEUCINE; MUTANT PROTEIN; PHOSPHINE OXIDE DERIVATIVE; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL KV1.5; THREONINE; UNCLASSIFIED DRUG; VALINE;

ANIMAL CELL; ARTICLE; BINDING SITE; CHANNEL GATING; CONTROLLED STUDY; DRUG PROTEIN BINDING; FEMALE; IC 50; MICROELECTRODE; MOLECULAR BIOLOGY; MOLECULAR MECHANICS; MUTAGENESIS; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; VOLTAGE CLAMP; WILD TYPE; XENOPUS LAEVIS;

ANIMALS; ATRIAL FIBRILLATION; COMPUTER SIMULATION; ELECTROPHYSIOLOGY; HUMANS; INHIBITORY CONCENTRATION 50; ISOLEUCINE; KV1.5 POTASSIUM CHANNEL; LEUCINE; OOCYTES; PATCH-CLAMP TECHNIQUES; PHOSPHINES; PROTEIN BINDING; THREONINE; XENOPUS LAEVIS;

XENOPUS LAEVIS;

EID: 77952668656     PISSN: 00222828     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.yjmcc.2010.02.010     Document Type: Article

References (29)

1. Choudhury A., Lip G.Y. Antiarrhythmic drugs in atrial fibrillation: an overview of new agents, their mechanisms of action and potential clinical utility. Expert Opin Investig Drugs 2004, 13:841-855.
2. + channel current. Circ Res 1993, 73:210-216.
3. Peukert S., Brendel J., Pirard B., Bruggemann A., Below P., Kleemann H.W., et al. Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5. J Med Chem 2003, 46:486-498.
4. Amos G.J., Wettwer E., Metzger F., Li Q., Himmel H.M., Ravens U. Differences between outward currents of human atrial and subepicardial ventricular myocytes. J Physiol 1996, 491(Pt 1):31-50.
5. Nattel S., Carlsson L. Innovative approaches to anti-arrhythmic drug therapy. Nat Rev Drug Discov 2006, 5:1034-1049.
6. Trotter B.W., Nanda K.K., Kett N.R., Regan C.P., Lynch J.J., Stump G.L., et al. Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation. J Med Chem 2006, 49:6954-6957.
7. Kur): rationale, pharmacology and evidence for potential therapeutic value. J Cardiovasc Pharmacol 2008, 52:105-120.
8. + channels. J Biol Chem 2004, 279:394-400.
9. Decher N., Kumar P., Gonzalez T., Pirard B., Sanguinetti M.C. Binding site of a novel Kv1.5 blocker: a "foot in the door" against atrial fibrillation. Mol Pharmacol 2006, 70:1204-1211.
10. Arechiga I.A., Barrio-Echavarria G.F., Rodriguez-Menchaca A.A., Moreno-Galindo E.G., Decher N., Tristani-Firouzi M., et al. Kv1.5 open channel block by the antiarrhythmic drug disopyramide: molecular determinants of block. J Pharmacol Sci 2008, 108:49-55.
11. Strutz-Seebohm N., Gutcher I., Decher N., Steinmeyer K., Lang F., Seebohm G. Comparison of potent Kv1.5 potassium channel inhibitors reveals the molecular basis for blocking kinetics and binding mode. Cell Physiol Biochem 2007, 20:791-800.
12. Kur blocker (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide. J Pharmacol Exp Ther 2005, 315:1362-1367.
13. Kur blocker, (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide, in rat and nonhuman primate. J Pharmacol Exp Ther 2006, 316:727-732.
14. + channels and ultrarapidly activating delayed rectifier potassium current. J Pharmacol Exp Ther 2006, 317:1054-1063.
15. Karczewski J., Kiss L., Kane S.A., Koblan K.S., Lynch R.J., Spencer R.H. High-throughput analysis of drug binding interactions for the human cardiac channel, Kv1.5. Biochem Pharmacol 2009, 77:177-185.
16. Wang X., Liao Y., Zou A., Li L., Tu D. Blockade action of ketanserin and increasing effect of potassium ion on Kv1.3 channels expressed in Xenopus oocytes. Pharmacol Res 2007, 56:148-154.
17. Tu D.N., Liao Y.H., Zou A.R., Du Y.M., Run Q., Wang X.P., et al. Electropharmacological properties of telmisartan in blocking hKv1.5 and HERG potassium channels expressed on Xenopus laevis oocytes. Acta Pharmacol Sin 2008, 29:913-922.
18. Du Y., Zhang S., Wu H., Zou A., Lei M., Cheng L., et al. Glycyrretinic acid blocks cardiac sodium channels expressed in Xenopus oocytes. J Ethnopharmacol 2009, 125:318-323.
19. + channel block. J Biol Chem 2002, 277:23587-23595.
20. Decher N., Kumar P., Gonzalez T., Renigunta V., Sanguinetti M.C. Structural basis for competition between drug binding and Kvbeta 1.3 accessory subunit-induced N-type inactivation of Kv1.5 channels. Mol Pharmacol 2005, 68:995-1005.
21. Eldstrom J., Wang Z., Xu H., Pourrier M., Ezrin A., Gibson K., et al. The molecular basis of high-affinity binding of the antiarrhythmic compound vernakalant (RSD1235) to Kv1.5 channels. Mol Pharmacol 2007, 72:1522-1534.
22. + channel. Role of S6 in antiarrhythmic drug binding. Circ Res 1996, 78:1105-1114.
23. Franqueza L., Longobardo M., Vicente J., Delpon E., Tamkun M.M., Tamargo J., et al. Molecular determinants of stereoselective bupivacaine block of hKv1.5 channels. Circ Res 1997, 81:1053-1064.
24. Caballero R., Moreno I., Gonzalez T., Valenzuela C., Tamargo J., Delpon E. Putative binding sites for benzocaine on a human cardiac cloned channel (Kv1.5). Cardiovasc Res 2002, 56:104-117.
25. Ander M., Luzhkov V.B., Aqvist J. Ligand binding to the voltage-gated Kv1.5 potassium channel in the open state-docking and computer simulations of a homology model. Biophys J 2008, 94:820-831.
26. + channel. Science 2005, 309:897-903.
27. Kamiya K., Niwa R., Mitcheson J.S., Sanguinetti M.C. Molecular determinants of HERG channel block. Mol Pharmacol 2006, 69:1709-1716.
28. Leicher T., Bahring R., Isbrandt D., Pongs O. Coexpression of the KCNA3B gene product with Kv1.5 leads to a novel A-type potassium channel. J Biol Chem 1998, 273:35095-35101.
29. Decher N., Gonzalez T., Streit A.K., Sachse F.B., Renigunta V., Soom M., et al. Structural determinants of Kvbeta1.3-induced channel inactivation: a hairpin modulated by PIP(2). EMBO J 2008, 27:3164-3174.