Block effect of capsaicin on hERG potassium currents is enhanced by S6 mutation at Y652

European Journal of Pharmacology

Volumn 630, Issue 1-3, 2010, Pages 1-9

  Xing, Junlian ^a   Ma, Jihua ^a   Zhang, Peihua ^a   Fan, Xinrong ^a  

^a WUHAN UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

Author keywords

Capsaicin; HERG; K+ channel; Voltage clamp

Indexed keywords

ALANINE; CAPSAICIN; PHENYLALANINE; POTASSIUM CHANNEL HERG; POTASSIUM ION; PROTEIN S6; TYROSINE;

ANIMAL CELL; ARTICLE; CHANNEL GATING; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG SENSITIVITY; FEMALE; GENE MUTATION; IC 50; INHIBITION KINETICS; MICROELECTRODE; MOLECULAR MECHANICS; NONHUMAN; OOCYTE; POTASSIUM CURRENT; PRIORITY JOURNAL; PROTEIN EXPRESSION; STEADY STATE; VOLTAGE CLAMP; WILD TYPE; XENOPUS;

ALANINE; AMINO ACID SUBSTITUTION; ANIMALS; CAPSAICIN; DOSE-RESPONSE RELATIONSHIP, DRUG; ETHER-A-GO-GO POTASSIUM CHANNELS; FEMALE; HUMANS; INHIBITORY CONCENTRATION 50; MICROELECTRODES; MICROINJECTIONS; MUTATION; OOCYTES; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS; XENOPUS LAEVIS;

EID: 77649189512     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2009.11.009     Document Type: Article

References (44)

1. Caballero R., Moreno I., Gonzalez T., Arias C., Valenzuela C., Delpon E., Tamarqo J. Spironolactone and its main metabolite, canrenoic acid, block human ether-a-go-go-related gene channels. Circulation 2003, 107:889-895.
2. Camerino D.C., Desaphy J.F., Tricarico D., Pierno S., Liantonio A. Therapeutic approaches to ion channel diseases. Adv. Genet. 2008, 64:81-145.
3. Carmeliet E. Use-dependent block and use-dependent unblock of the delayed rectifier K+ current by almokalant in rabbit ventricular myocytes. Circ. Res. 1993, 73:857-868.
4. Caterina M.J., Schumacher M.A., Tominaga M., Rosen T.A., Levine J.D., Julius D. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 1997, 389:816-824.
5. Chow J., Norng M., Zhang J., Chai J. TRPV6 mediates capsaicin-induced apoptosis in gastric cancer cells-mechanisms behind a possible new "hot" cancer treatment. Biochim. Biophys. Acta 2007, 1773:565-576.
6. De Ponti F., Poluzzi E., Cavalli A., Recanatini M., Montanaro N. Safety of non-antiarrhythmic drugs that prolong the QT interval or induce torsade de pointes: an overview. Drug Saf. 2002, 25:263-286.
7. Dumaine R., Roy M.L., Brown A.M. Blockade of HERG and Kv1.5 by ketoconazole. J. Pharmacol. Exp. Ther. 1998, 286:727-735.
8. + channel: accessibility to F656 and Y652. Biochem. Biophys. Res. Commun. 2006, 341:500-556.
9. Duncan R.S., McPate M.J., Ridley J.M., Gao Z., James A.F., Leishman D.J., Leaney J.L., Witchel H.J., Hancox J.C. Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin. Biochem. Pharmacol. 2007, 74:425-437.
10. Fitzgerald P.T., Ackerman M.J. Drug-induced torsades de pointes: the evolving role of pharmacogenetics. Heart Rhythm 2005, 2:S30-37.
11. + channels by esnarinone. Mol. Pharmacol. 2001, 60:244-253.
12. Karczewski J., Wang J., Kane S.A., Kiss L., Koblan K.S., Culberson J.C., Spencer R.H. Analogs of MK-499 are differentially affected by a mutation in the S6 domain of the hERG K+ channel. Biochem. Pharmacol. 2009, 77:1602-1611.
13. + currents in melanotrophs of the rat pituitary. Br. J. Pharmacol. 1994, 112:616-624.
14. Lee Y.S., Kang Y.S., Lee J.S., Nicolova S., Kim J.A. Involvement of NADPH oxidase-mediated generation of reactive oxygen species in the apototic cell death by capsaicin in HepG2 human hepatoma cells. Free Radic. Res. 2004, 38:405-412.
15. Lees-Miller J.P., Duan Y., Teng G.Q., Duff H.J. Molecular determinant of high-affinity dofetilide binding to HERG expressed in Xenopus oocytes: involvement of S6 sites. Mol. Pharmacol. 2000, 57:367-374.
16. Lo Y.C., Yang Y.C., Wu I.C., Kuo F.C., Liu C.M., Wang H.W., Kuo C.H., Wu J.Y., Wu D.C. Capsaicin-induced cell death in a human gastric adenocarcinoma cell line. World J. Gastroenterol. 2005, 11:6254-6257.
17. Milnes J.T., Crociani O., Arcangeli A., Hancox J.C., Witchel H.J. Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652. Br. J. Pharmacol. 2003, 139:887-898.
18. Mitcheson J.S. Drug binding to HERG channels: evidence for a 'non-aromatic' binding site for fluvoxamine. Br. J. Pharmacol. 2003, 139:883-884.
19. Mitcheson J.S., Perry M.D. Molecular determinants of high affinity drug binding to HERG channels. Curr. Opin. Drug Discov. Dev. 2003, 6:667-674.
20. 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. U. S. A. 2000, 97:12329-12333.
21. Mitcheson J.S., Chen J., Sanquinetti M.C. Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate. J. Gen. Physiol. 2000, 115:229-240.
22. Napolitano C., Priori S., Schwartz P. Torsade de pointes: mechanism and management. Drugs 1994, 47:51-65.
23. Neil A.Castle Differential inhibition of potassium currents in rat ventricular myocytes by capsaicin. Cardiovasc. Res. 1992, 26:1137-1144.
24. O'Sullivan S.E., Kendall D.A., Randall M.D. Heterogeneity in the mechanisms of vasorelaxation to anandamide in resistance and conduit rat mesenteric arteries. Br. J. Pharmacol. 2004, 142:435-442.
25. Pardo-Lopez L., Zhang M., Liu J., Jiang M., Possani L.D., Tseng G.N. Mapping the binding site of a human ether-ago-go-related gene-specific peptide toxin (ErgTx) to the channel's outer vestibule. J. Biol. Chem. 2002, 277:16403-16411.
26. Petersen M., Wagner G., Pierau F.-K. Modulation of calcium currents by capsaicin in a subpopulation of sensory neurones of guinea-pig. Naunyn Schmiedebergs Arch. Pharmacol. 1989, 339:184-191.
27. Sakaguchi T., Itoh H., Ding W.G., Tsuji K., Nagaoka I., Oka Y., Ashihara T., Ito M., Yumoto Y., Zenda N., Higashi Y., Takeyama Y., Matsuura H., Horie M. Hydroxyzine, a first generation h1-receptor antagonist, inhibits Human Ether-a-go-go-Related Gene (HERG) current and causes syncope in a patient with the HERG mutation. J. Pharmacol. Sci. 2008, 108:462-471.
28. Sanchez-Chapula J.A., Ferrer T., Navarro Polanco R.A., Sanguinetti M.C. Voltage-dependent profile of humane the a-go-go-related gene channel block is influenced by a single residue in the S6 transmembrane domain. Mol. Pharmacol. 2000, 57:367-374.
29. + channel block. J. Biol. Chem. 2002, 277:23587-23595.
30. Sanguinetti M.C., Mitcheson J.S. Predicting drug-HERG channel interactions that cause acquired long QT syndrome. Trends Pharmacol. Sci. 2005, 26:119-124.
31. Sanguinetti M.C., Jiang C., Curran M.E., Keating M.T. A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell 1995, 81:299-307.
32. Snyders D.J., Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol. Pharmacol. 1996, 49:949-955.
33. Spector P.S., Curran M.E., Keating M.T., Sanguinetti M.C. Class III antiarrhythmic drugs block HERG, a human cardiac delayed rectifier K+ channel. Open-channel block by methanesulphonanilides. Circ. Res. 1996, 78:499-503.
34. Teschemacher A.G., Seward E.P., Hancox J.C., Witchel H.J. Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline. Br. J. Pharmacol. 1999, 128:479-485.
35. Thomas D., Kiehn J., Katus H.A., Karle C.A. Defective protein trafficking in hERG-associated hereditary long QT syndrome (LQT2): molecular mechanisms and restoration of intracellular protein processing. Cardiovasc. Res. 2003, 60:239-245.
36. Trudeau M.C., Warmke J.W., Ganetzky B., Robertson G.A. HERG, a human inward rectifier in the voltage gated potassium channel family. Science 1995, 269:92-95.
37. Tu D.N., Zou A.R., Liao Y.H., DU Y.M., Wang X.P., Li L. Blockade of the human ether-a-go-go-related gene potassium channel by ketanserin. Sheng Li Xue Bao 2008, 60:525-534.
38. Vandenberg J.I., Walker B.D., Campbell T.J. HERG K+ channels: friend and foe. Trends Pharmacol. Sci. 2001, 22:240-246.
39. Viskin S. Long QT. Syndromes and torsade de pointes. Lancet 1999, 354:1625-1633.
40. Volberg W.A., Koci B.J., Su W., Lin J., Zhou J. Blockade of human cardiac potassium channel human ether-a-go-go-related gene (HERG) by macrolide antibiotics. J. Pharmacol. Exp. Ther. 2002, 302:320-327.
41. Warmke J.W., Ganetzky B. A family of potassium channel genes related to eag in Drosophila and mammals. Proc. Natl. Acad. Sci. U. S. A. 1994, 91:3438-3442.
42. Witchel H.J., Pabbathi V.K., Hofmann G., Paul A.A., Hancox J.C. Inhibitory actions of the selective serotonin re-uptake inhibitor citalopram on HERG and ventricular L-type calcium currents. FEBS Lett. 2002, 512:59-66.
43. Wolf C.M., Berul C.I. Molecular mechanisms of inherited arrhythmias. Curr. Genomics. 2008, 9:160-168.
44. Zhang J., Naqasaki M., Tanaka Y., Morikawa S. Capsaicin inhibits growth of adult T-cell leukemia cells. Leuk. Res. 2003, 27:275-283.