Predicting drug-hERG channel interactions that cause acquired long QT syndrome

Trends in Pharmacological Sciences

Volumn 26, Issue 3, 2005, Pages 119-124

  Sanguinetti, Michael C ^a   Mitcheson, John S ^b  

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

^b UNIVERSITY OF LEICESTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1' (6 CYANO 1,2,3,4 TETRAHYDRO 2 NAPHTHYL) 3,4 DIHYDRO 6 METHANESULFONAMIDOSPIRO[2H 1 BENZOPYRAN 2,4' PIPERIDIN] 4 OL; POTASSIUM CHANNEL; POTASSIUM CHANNEL BLOCKING AGENT;

BINDING SITE; CARDIOVASCULAR RISK; COMPUTER MODEL; DRUG DESIGN; ELECTROCARDIOGRAM; HEART ARRHYTHMIA; HEART REPOLARIZATION; HUMAN; LONG QT SYNDROME; MUTAGENESIS; NONHUMAN; PRIORITY JOURNAL; QUANTITATIVE STRUCTURE ACTIVITY RELATION; REVIEW; TORSADE DES POINTES;

EID: 14644412444     PISSN: 01656147     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tips.2005.01.003     Document Type: Article

References (46)

1. D.S. Echt Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmia Suppression Trial New Engl. J. Med. 324 1991 781 788
2. W. Haverkamp The potential for QT prolongation and proarrhythmia by non-antiarrhythmic drugs: clinical and regulatory implications. Report on a policy conference of the European Society of Cardiology Eur. Heart J. 21 2000 1216 1231
3. M.H. Lehmann Sex difference in risk of torsade de pointes with d,l-sotalol Circulation 94 1996 2535 2541
4. 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
5. Kr potassium channel Cell 81 1995 299 307
6. M. Trudeau HERG, a human inward rectifier in the voltage-gated potassium channel family Science 269 1995 92 95
7. M.T. Keating, and M.C. Sanguinetti Molecular and cellular mechanisms of cardiac arrhythmias Cell 104 2001 569 580
8. N.M. Plaster Mutations in Kir2.1 cause the developmental and episodic electrical phenotypes of Andersen's syndrome Cell 105 2001 511 519
9. P.J. Mohler Ankyrin-B mutation causes type 4 long-QT cardiac arrhythmia and sudden cardiac death Nature 421 2003 634 639
10. V1.2 calcium channel dysfunction causes a multisystem disorder including arrhythmia and autism Cell 119 2004 19 31
11. F. Sesti A common polymorphism associated with antibiotic-induced cardiac arrhythmia Proc. Natl. Acad. Sci. U. S. A. 97 2000 10613 10618
12. I. Splawski Variant of SCN5A sodium channel implicated in risk of cardiac arrhythmia Science 297 2002 1333 1336
13. B. Fermini, and A.A. Fossa The impact of drug-induced QT interval prolongation on drug discovery and development Nat. Rev. Drug Discov. 2 2003 439 447
14. I. Cavero Drugs that prolong QT interval as an unwanted effect: assessing their likelihood of inducing hazardous cardiac dysrhythmias Expert Opin. Pharmacother. 1 2000 947 973
15. R.R. Fenichel Drug-induced torsades de pointes and implications for drug development J. Cardiovasc. Electrophysiol. 15 2004 475 495
16. L. Kiss High throughput ion-channel pharmacology: planar-array-based voltage clamp Assay Drug Dev Technol 1 2003 127 135
17. K.N. Schroeder IonWorks HT: a new high-throughput electrophysiology measurement platform J. BioMol. Screen 8 2003 50 64
18. K. Finlayson [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen Eur. J. Pharmacol. 430 2001 147 148
19. C.S. Cheng A high-throughput HERG potassium channel function assay: an old assay with a new look Drug Dev. Ind. Pharm. 28 2002 177 191
20. L.M. Hondeghem Instability and triangulation of the action potential predict serious proarrhythmia, but action potential duration prolongation is antiarrhythmic Circulation 103 2001 2004 2013
21. L.M. Hondeghem Phase 2 prolongation, in the absence of instability and triangulation, antagonizes class III proarrhythmia Cardiovasc. Res. 50 2001 345 353
22. L.M. Hondeghem, and P. Hoffmann Blinded test in isolated female rabbit heart reliably identifies action potential duration prolongation and proarrhythmic drugs: importance of triangulation, reverse use dependence, and instability J. Cardiovasc. Pharmacol. 41 2003 14 24
23. J.S. Mitcheson A structural basis for drug-induced long QT syndrome Proc. Natl. Acad. Sci. U. S. A. 97 2000 12329 12333
24. D.A. Doyle The structure of the potassium channel: molecular basis of K+ conduction and selectivity Science 280 1998 69 77
25. Y. Jiang Crystal structure and mechanism of a calcium-gated potassium channel Nature 417 2002 515 522
26. R. Pearlstein Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior J. Med. Chem. 46 2003 2017 2022
27. H.J. Witchel The low potency, voltage-dependent HERG blocker propafenone - molecular determinants and drug trapping Mol. Pharmacol. 66 2004 1201 1212
28. Y. Jiang The open pore conformation of potassium channels Nature 417 2002 523 526
29. + channel block J. Biol. Chem. 277 2002 23587 23595
30. J.A. Sanchez-Chapula 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
31. + channels by vesnarinone Mol. Pharmacol. 60 2001 244 253
32. + channel J. Mol. Cell. Cardiol. 36 2004 701 705
33. M. Perry Structural determinants of HERG channel block by clofilium and ibutilide Mol. Pharmacol. 66 2004 240 249
34. J.P. Lees-Miller Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites Mol. Pharmacol. 57 2000 367 374
35. D. Fernandez Physicochemical features of the hERG channel drug binding site J. Biol. Chem. 279 2003 10120 10127
36. + channel blockers J. Med. Chem. 45 2002 3844 3853
37. S. Ekins Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel J. Pharmacol. Exp. Ther. 301 2002 427 434
38. R.A. Pearlstein Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches Bioorg. Med. Chem. Lett. 13 2003 1829 1835
39. + channels Circ. Res. 82 1998 386 395
40. M.C. Sanguinetti, and Q.P. Xu Mutations of the S4-S5 linker alter activation properties of HERG potassium channels expressed in Xenopus oocytes J. Physiol. 514 1999 667 675
41. J.S. Mitcheson Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate J. Gen. Physiol. 115 2000 229 240
42. + channels defined by high-affinity metal bridges Nature 428 2004 864 868
43. G. Gessner, and S.H. Heinemann Inhibition of hEAG1 and hERG1 potassium channels by clofilium and its tertiary analogue LY97241 Br. J. Pharmacol. 138 2003 161 171
44. J. Chen Position of aromatic residues in the S6 domain, not inactivation, dictates cisapride sensitivity of HERG and eag potassium channels Proc. Natl. Acad. Sci. U. S. A. 99 2002 12461 12466
45. + channel blockade: current knowledge and strategies for the early prediction during drug development Med. Res. Rev. 25 2005 133 166
46. T.K. Morgan, and M.E. Sullivan An overview of class III electrophysiological agents: a new generation of antiarrhythmic therapy G.P. Ellis D.K. Luscombe Progress in Medicinal Chemistry Vol. 29 1992 Elsevier 65 108