The membrane permeable calcium chelator BAPTA-AM directly blocks human ether a-go-go-related gene potassium channels stably expressed in HEK 293 cells

Biochemical Pharmacology

Volumn 74, Issue 11, 2007, Pages 1596-1607

  Tang, Qiang ^a,b   Jin, Man Wen ^b   Xiang, Ji Zhou ^b   Dong, Min Qing ^a   Sun, Hai Ying ^a   Lau, Chu Pak ^a   Li, Gui Rong ^a  

^a UNIVERSITY OF HONG KONG   (Hong Kong)

^b HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

Author keywords

BAPTA AM; hERG; hKv1.3; hKv1.5; Open channel blocker

Indexed keywords

ALANINE; EGTAZIC ACID; EGTAZIC ACID TETRAACETOXYMETHYL ESTER; ETHYLENE GLYCOL 1,2 BIS(2 AMINOPHENYL) ETHER N,N,N',N' TETRAACETIC ACID; ETHYLENE GLYCOL 1,2 BIS(2 AMINOPHENYL) ETHER N,N,N',N' TETRAACETIC ACID TETRAACETOXYMETHYL ESTER; POTASSIUM CHANNEL HERG; POTASSIUM CHANNEL KV1.3; POTASSIUM CHANNEL KV1.5; SERINE; TYROSINE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ARTICLE; CELL STRAIN HEK293; CHANNEL GATING; CHELATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; HUMAN; HUMAN CELL; IC 50; POTASSIUM CURRENT; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; STEADY STATE;

CALCIUM; CELL LINE; CELL MEMBRANE PERMEABILITY; CHELATING AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; EGTAZIC ACID; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; KV1.3 POTASSIUM CHANNEL; KV1.5 POTASSIUM CHANNEL; MEMBRANE POTENTIALS; MUTAGENESIS, SITE-DIRECTED; PORINS; TRANSFECTION;

EID: 35348955352     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2007.07.042     Document Type: Article

References (51)

1. Tsien R.Y. A non-disruptive technique for loading calcium buffers and indicators into cells. Nature 290 (1981) 527-528
2. i. Am J Physiol 267 (1994) G465-G475
3. 2+)-ATPase inhibitor thapsigargin. Exp Cell Res 212 (1994) 84-92
4. Na is in the common final pathway to heart block in murine hearts overexpressing calcineurin. Am J Physiol 291 (2006) H2669-H2679
5. + transient outward current via the calcineurin pathway. J Biol Chem 279 (2004) 40634-40639
6. 2+-selective TRPV6 channel. J Biol Chem 279 (2004) 36546-36552
7. Bugaj V., Alexeenko V., Zubov A., Glushankova L., Nikolaev A., Wang Z., et al. Functional properties of endogenous receptor- and store-operated calcium influx channels in HEK293 cells. J Biol Chem 280 (2005) 16790-16797
8. 2+ in the expression of the amiloride-sensitive epithelial sodium channel. Cell Calcium 35 (2004) 21-28
9. Niesen C., Charlton M.P., and Carlen P.L. Postsynaptic and presynaptic effects of the calcium chelator BAPTA on synaptic transmission in rat hippocampal dentate granule neurons. Brain Res 555 (1991) 319-325
10. 2+ chelators reduce early excitotoxic and ischemic neuronal injury in vitro and in vivo. Neuron 11 (1993) 221-235
11. Gutman G.A., Chandy K.G., Adelman J.P., Aiyar J., Bayliss D.A., Clapham D.E., et al. International Union of Pharmacology. XLI. Compendium of voltage-gated ion channels: potassium channels. Pharmacol Rev 55 (2003) 583-586
12. Kr: the hERG channel. J Mol Cell Cardiol 33 (2001) 835-849
13. Sanguinetti M.C., and Mitcheson J.S. Predicting drug-hERG channel interactions that cause acquired long QT syndrome. Trends Pharmacol Sci 26 (2005) 119-124
14. 2+/calmodulin binding to the cytosolic N- and C-termini. FEBS J 273 (2006) 1074-1086
15. Schonherr R., Lober K., and Heinemann S.H. Inhibition of human ether a go-go potassium channels by Ca(2+)/calmodulin. EMBO J 19 (2000) 3263-3271
16. Trudeau M.C., Warmke J.W., Ganetzky B., and Robertson G.A. HERG, a human inward rectifier in the voltage-gated potassium channel family. Science 269 (1995) 92-95
17. Dong M.Q., Lau C.P., Gao Z., Tseng G.N., and Li G.R. Characterization of recombinant human cardiac KCNQ1/KCNE1 channels (I (Ks)) stably expressed in HEK 293 cells. J Membr Biol 210 (2006) 183-192
18. Guo J., Gang H., and Zhang S. Molecular determinants of cocaine block of human ether-a-go-go-related gene potassium channels. J Pharmacol Exp Ther 317 (2006) 865-874
19. + permeation and block of hERG potassium channels. J Gen Physiol 128 (2006) 55-71
20. Bahring R., Vardanyan V., and Pongs O. Differential modulation of Kv1 channel-mediated currents by co-expression of Kvbeta3 subunit in a mammalian cell-line. Mol Membr Biol 21 (2004) 19-25
21. Tian M., Dong M.Q., Chiu S.W., Lau C.P., and Li G.R. Effects of the antifungal antibiotic clotrimazole on human cardiac repolarization potassium currents. Br J Pharmacol 147 (2006) 289-297
22. Li G.R., Lau C.P., Ducharme A., Tardif J.C., and Nattel S. Transmural action potential and ionic current remodeling in ventricles of failing canine hearts. Am J Physiol 283 (2002) H1031-H1041
23. Caballero R., Moreno I., Gonzalez T., Arias C., Valenzuela C., Delpon E., et al. Spironolactone and its main metabolite, canrenoic acid, block human ether-a-go-go-related gene channels. Circulation 107 (2003) 889-895
24. Smith P.L., Baukrowitz T., and Yellen G. The inward rectification mechanism of the HERG cardiac potassium channel. Nature 379 (1996) 833-836
25. + current by verapamil in human atrial myocytes. J Mol Cell Cardiol 36 (2004) 257-263
26. Kamiya K., Mitcheson J.S., Yasui K., Kodama I., and Sanguinetti M.C. Open channel block of HERG K(+) channels by vesnarinone. Mol Pharmacol 60 (2001) 244-253
27. Zhang S., Zhou Z., Gong Q., Makielski J.C., and January C.T. Mechanism of block and identification of the verapamil binding domain to HERG potassium channels. Circ Res 84 (1999) 989-998
28. Yang B.F., Xu D.H., Xu C.Q., Li Z., Du Z.M., Wang H.Z., et al. Inactivation gating determines drug potency: a common mechanism for drug blockade of HERG channels. Acta Pharmacol Sin 25 (2004) 554-560
29. + channel. J Mol Cell Cardiol 36 (2004) 151-160
30. Suessbrich H., Schonherr R., Heinemann S.H., Lang F., and Busch A.E. Specific block of cloned Herg channels by clofilium and its tertiary analog LY97241. FEBS Lett 414 (1997) 435-438
31. Watkins C.S., and Mathie A. Effects on K+ currents in rat cerebellar granule neurones of a membrane-permeable analogue of the calcium chelator BAPTA. Br J Pharmacol 118 (1996) 1772-1778
32. + currents in cultured bovine chromaffin cells. Neuroreport 9 (1998) 3403-3407
33. Collatz M.B., Rudel R., and Brinkmeier H. Intracellular calcium chelator BAPTA protects cells against toxic calcium overload but also alters physiological calcium responses. Cell Calcium 21 (1997) 453-459
34. Dieter P., Fitzke E., and Duyster J. BAPTA induces a decrease of intracellular free calcium and a translocation and inactivation of protein kinase C in macrophages. Biol Chem Hoppe Seyler 374 (1993) 171-174
35. Larson L., Arnaudeau S., Gibson B., Li W., Krause R., Hao B., et al. Gelsolin mediates calcium-dependent disassembly of Listeria actin tails. Proc Natl Acad Sci USA 102 (2005) 1921-1926
36. 2+ inhibits murine keratinocyte differentiation in vitro. J Cell Physiol 163 (1995) 105-114
37. Paschen W., Hotop S., and Aufenberg C. Loading neurons with BAPTA-AM activates xbp1 processing indicative of induction of endoplasmic reticulum stress. Cell Calcium 33 (2003) 83-89
38. Pu Y., and Chang D.C. Cytosolic Ca(2+) signal is involved in regulating UV-induced apoptosis in hela cells. Biochem Biophys Res Commun 282 (2001) 84-89
39. Takahashi K., Inanami O., and Kuwabara M. Effects of intracellular calcium chelator BAPTA-AM on radiation-induced apoptosis regulated by activation of SAPK/JNK and caspase-3 in MOLT-4 cells. Int J Radiat Biol 75 (1999) 1099-1105
40. Milnes J.T., Crociani O., Arcangeli A., Hancox J.C., and Witchel H.J. Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652. Br J Pharmacol 139 (2003) 887-898
41. + channel. J Mol Cell Cardiol 40 (2006) 107-118
42. + channels. Circ Res 82 (1998) 386-395
43. + channel blockade by the antipsychotic drug thioridazine: an obligatory role for the S6 helix residue F656. Biochem Biophys Res Commun 351 (2006) 273-280
44. Perry M., Stansfeld P.J., Leaney J., Wood C., de Groot M.J., Leishman D., et al. Drug binding interactions in the inner cavity of HERG channels: molecular insights from structure-activity relationships of clofilium and ibutilide analogs. Mol Pharmacol 69 (2006) 509-519
45. Ridley J.M., Milnes J.T., Duncan R.S., McPate M.J., James A.F., Witchel H.J., et al. Inhibition of the HERG K+ channel by the antifungal drug ketoconazole depends on channel gating and involves the S6 residue F656. FEBS Lett 580 (2006) 1999-2005
46. Sanchez-Chapula J.A., Ferrer T., Navarro-Polanco R.A., and Sanguinetti M.C. Voltage-dependent profile of human ether-a-go-go-related gene channel block is influenced by a single residue in the S6 transmembrane domain. Mol Pharmacol 63 (2003) 1051-1058
47. Thomas D., Wu K., Wimmer A.B., Zitron E., Hammerling B.C., Kathofer S., et al. Activation of cardiac human ether-a-go-go related gene potassium currents is regulated by alpha(1A)-adrenoceptors. J Mol Med 82 (2004) 826-837
48. Kiehn J., Karle C., Thomas D., Yao X., Brachmann J., and Kubler W. HERG potassium channel activation is shifted by phorbol esters via protein kinase A-dependent pathways. J Biol Chem 273 (1998) 25285-25291
49. Thomas D., Zhang W., Wu K., Wimmer A.B., Gut B., Wendt-Nordahl G., et al. Regulation of HERG potassium channel activation by protein kinase C independent of direct phosphorylation of the channel protein. Cardiovasc Res 59 (2003) 14-26
50. Chung I., and Schlichter L.C. Native Kv1.3 channels are upregulated by protein kinase C. J Membr Biol 156 (1997) 73-85
51. Williams C.P., Hu N., Shen W., Mashburn A.B., and Murray K.T. Modulation of the human Kv1.5 channel by protein kinase C activation: role of the Kvbeta1.2 subunit. J Pharmacol Exp Ther 302 (2002) 545-550