Direct block of hERG potassium channels by the protein kinase C inhibitor bisindolylmaleimide I (GF109203X)

Cardiovascular Research

Volumn 64, Issue 3, 2004, Pages 467-476

  Thomas, Dierk ^a   Hammerling, Bettina C ^a   Wimmer, Anna Britt ^a   Wu, Kezhong ^a   Ficker, Eckhard ^b   Kuryshev, Yuri A ^b   Scherer, Daniel ^a   Kiehn, Johann ^a   Katus, Hugo A ^a   Schoels, Wolfgang ^a   Karle, Christoph A ^a  

^a UNIVERSITY HOSPITAL HEIDELBERG   (Germany)

^b CASE WESTERN RESERVE UNIVERSITY   (United States)

Author keywords

Arrhythmia (mechanisms); Hormones; Ion channels; K channel; Long QT syndrome

Indexed keywords

2 [1 (3 DIMETHYLAMINOPROPYL) 3 INDOLYL] 3 (3 INDOLYL)MALEIMIDE; ALANINE; BISINDOLYLMALEIMIDE; INWARDLY RECTIFYING POTASSIUM CHANNEL; PHENYLALANINE; POTASSIUM CHANNEL HERG; PROTEIN KINASE C INHIBITOR; TYROSINE; VOLTAGE GATED POTASSIUM CHANNEL;

ARTICLE; CONCENTRATION RESPONSE; DRUG INHIBITION; DRUG RECEPTOR BINDING; GENETIC TRANSFECTION; HEART ELECTROPHYSIOLOGY; HEART MUSCLE POTENTIAL; HUMAN; HUMAN CELL; IC 50; POINT MUTATION; POTASSIUM CURRENT; PRIORITY JOURNAL; QT PROLONGATION; VOLTAGE CLAMP; XENOPUS LAEVIS;

ACTION POTENTIALS; ANIMALS; CATION TRANSPORT PROTEINS; CELLS, CULTURED; DOSE-RESPONSE RELATIONSHIP, DRUG; ETHER-A-GO-GO POTASSIUM CHANNELS; FEMALE; GUINEA PIGS; HUMANS; INDOLES; KIDNEY; MALEIMIDES; MUTATION; MYOCYTES, CARDIAC; OOCYTES; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PROTEIN KINASE C; XENOPUS LAEVIS;

EID: 8644254252     PISSN: 00086363     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.cardiores.2004.07.023     Document Type: Article

References (32)

1. J.W. Warmke, and B. Ganetzky A family of potassium channel genes related to eag in Drosophila and mammals Proc. Natl. Acad. Sci. U. S. A. 91 1994 3438 3442
2. Kr potassium channel Cell 81 1995 299 307
3. C. Napolitano, S. Priori, and P. Schwartz Torsade de pointes: mechanism and management Drugs 47 1994 51 65
4. S. Viskin, and Q.T. Long Syndromes and torsade de pointes Lancet 354 1999 1625 1633
5. D. Thomas, J. Kiehn, H.A. Katus, and C.A. Karle Defective protein trafficking in hERG-associated hereditary long QT syndrome (LQT2): molecular mechanisms and restoration of intracellular protein processing Cardiovasc. Res. 60 2003 239 245
6. L. Bianchi, B. Wible, A. Arcangeli, M. Tagliatatela, F. Morra, and P. Castaldo Herg encodes a K+ current highly conserved in tumors of different histogenesis: a selective advantage for cancer cells? Cancer Res. 58 1998 815 822
7. A. Cherubini, G.L. Taddei, O. Crociani, M. Paglierani, A.M. Buccoliero, and L. Fontana HERG potassium channels are more frequently expressed in human endometrial cancer as compared to non-cancerous endometrium Br. J. Cancer 83 2000 1722 1729
8. O. Crociani, L. Guasti, M. Balzi, A. Becchetti, E. Wanke, and M. Olivotto Cell-cycle-dependent expression of HERG1 and HERG1B isoforms in tumor cells J. Biol. Chem. 278 2003 2947 2955
9. G.A.M. Smith, H.W. Tsui, E.W. Newell, X. Jiang, X.P. Zhu, and F.WL. Tsui Functional up-regulation of HERG K+ channels in neoplastic hematopoietic cells J. Biol. Chem. 277 2002 18528 18534
10. H. Wang, Y. Zhang, L. Cao, H. Han, J. Wang, and B. Yang HERG K+ channel, a regulator of tumor cell apoptosis and proliferation Cancer Res. 62 2002 4843 4848
11. J. Bian, J. Cui, and T.V. McDonald HERG K(+) channel activity is regulated by changes in phosphatidyl inositol 4,5-bisphosphate Circ. Res. 89 2001 1168 1176
12. D. Thomas, W. Zhang, K. Wu, A.B. Wimmer, B. Gut, and G. Wendt-Nordahl Regulation of HERG potassium channel activation by protein kinase C independent of direct phosphorylation of the channel protein Cardiovasc. Res. 59 2003 14 26
13. C.F. Lo, and G.E. Breitwieser Protein kinase-independent inhibition of muscarinic K+ channels by staurosporine Am. J. Physiol. 266 1994 C1128 C1132
14. H.C. Hartzell, A. Rinderknecht, and C. Calphostin a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels Am. J. Physiol. 270 1996 C1293 C1299
15. J.S. Choi, S.J. Hahn, D.J. Rhie, Y.H. Jo, and M.S. Kim Staurosporine directly blocks Kv1.3 channels expressed in Chinese hamster ovary cells Naunyn-Schmiedeberg's Arch. Pharmacol. 359 1999 256 261
16. B.H. Choi, J.S. Choi, S.W. Jeong, S.J. Hahn, S.H. Yoon, and Y.H. Jo Direct block by bisindolylmaleimide of rat Kv1.5 expressed in Chinese hamster ovary cells J. Pharmacol. Exp. Ther. 293 2000 634 640
17. H. Cho, J.B. Youm, Y.E. Earm, and W.K. Ho Inhibition of acetylcholine-activated K(+) current by chelerythrine and bisindolylmaleimide I in atrial myocytes from mice Eur. J. Pharmacol. 424 2001 173 178
18. W. Schledermann, I. Wulfsen, J.R. Schwarz, and C.K. Bauer Modulation of rat erg1, erg2, erg3 and HERG K+ currents by thyreotropin-releasing hormone in anterior pituitary cells via the native signal cascade J. Physiol. 532 2001 143 163
19. J. Kiehn, D. Thomas, C.A. Karle, W. Schöls, and W. Kübler Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels Naunyn-Schmiedeberg's Arch. Pharmacol. 359 1999 212 219
20. E.P. Scholz, E. Zitron, C. Kiesecker, S. Lueck, S. Kathöfer, and D. Thomas Drug binding to aromatic residues in the HERG channel pore cavity as possible explanation for acquired long QT syndrome by antiparkinsonian drug budipine Naunyn-Schmiedeberg's Arch. Pharmacol. 368 2003 404 414
21. M.C. Sanguinetti, M.E. Curran, A. Zou, J. Shen, P.S. Spector, and D.L. Atkinson Coassembly of KvLQT1 and minK (IsK) proteins to form IKs potassium channel Nature 384 1996 80 83
22. D. Thomas, G. Wendt-Nordahl, K. Röckl, E. Ficker, A.M. Brown, and J. Kiehn High-affinity blockade of HERG human cardiac potassium channels by the novel antiarrhythmic drug BRL-32872 J. Pharmacol. Exp. Ther. 297 2001 753 761
23. D. Thomas, W. Zhang, C.A. Karle, S. Kathofer, W. Schols, and J. Kiehn Deletion of protein kinase A phosphorylation sites in the HERG potassium channel inhibits activation shift by protein kinase A J. Biol. Chem. 274 1999 27457 27462
24. E. Ficker, Y.A. Kuryshev, A.T. Dennis, C. Obejero-Paz, L. Wang, and P. Hawryluk Mechanisms of arsenic-induced prolongation of cardiac repolarization Mol. Pharmacol. 66 2004 33 44
25. J.S. Mitcheson, J. Chen, M. Lin, C. Culberson, and M.C. Sanguinetti A structural basis for drug-induced long QT syndrome Proc. Natl. Acad. Sci. U. S. A. 97 2000 12329 12333
26. J. Barhanin, F. Lesage, E. Guillemare, M. Fink, M. Lazdunski, and G. Romey KvLQT1 and IsK (minK) proteins associate to form the IKs potassium channel Nature 384 1996 78 80
27. J. Kiehn, C. Karle, D. Thomas, X. Yao, J. Brachmann, and W. Kübler HERG potassium channel activation is shifted by phorbol esters via protein kinase A-dependent pathways J. Biol. Chem. 273 1998 25285 25291
28. J.S. Mitcheson, J. Chen, and M.C. Sanguinetti Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate J. Gen. Physiol. 115 2000 229 240
29. J.S. Mitcheson Drug binding to HERG channels: evidence for a 'non-aromatic' binding site for fluvoxamine Br. J. Pharmacol. 139 2003 883 884
30. Kr potassium channels with HERG and is associated with cardiac arrhythmia Cell 97 1999 175 187
31. M. Weerapura, S. Nattel, D. Chartier, R. Caballero, and T.E. Hebert A comparison of currents carried by HERG, with and without coexpression of MiRP1, and the native rapid delayed rectifier current. Is MiRP1 the missing link? J. Physiol. 540 2002 15 27
32. D. Thomas, B. Gut, S. Karsai, A.B. Wimmer, K. Wu, and G. Wendt-Nordahl Inhibition of cloned HERG potassium channels by the antiestrogen tamoxifen Naunyn-Schmiedeberg's Arch. Pharmacol. 368 2003 41 48