The hERG potassium channel as a therapeutic target

Bibliography

• GUTMAN GA, CHANDY KG, GRISSMER S et al.: International Union of Pharmacology. LIII. Nomenclature and molecular relationships of voltage-gated potassium channels. Pharmacol. Rev. (2005) 57(4):473-508.
   PubMed Web of Science ®Google Scholar
• WARMKE JW, GANETZKY B: A family of potassium channel genes related to eag in Drosophila and mammals. Proc. Natl. Acad. Sci. USA (1994) 91:3438-3442.
   PubMed Web of Science ®Google Scholar
• SANGUINETTI MC, JIANG C, CURRAN ME, KEATING MT: A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell (1995) 81(2):299-307.
   PubMed Web of Science ®Google Scholar
• TRUDEAU MC, WARMKE JW, GANETZKY B, ROBERTSON GA: HERG, a human inward rectifier in the voltage gated potassium channel family. Science (1995) 269:92-95.
   PubMed Web of Science ®Google Scholar
• KEATING MT, SANGUINETTI MC: Molecular and cellular mechanisms of cardiac arrhythmias. Cell (2001) 104(4):569-580.
   PubMed Web of Science ®Google Scholar
• SANGUINETTI MC, TRISTANI-FIROUZI M: hERG potassium channels and cardiac arrhythmia. Nature (2006) 440(7083):463-469.
   PubMed Web of Science ®Google Scholar
• WITCHEL HJ, HANCOX JC: Familial and acquired Long QT Syndrome and the cardiac rapid delayed rectifier potassium current. Clin. Exp. Pharm. Physiol. (2000) 27(10):753-766.
   PubMed Web of Science ®Google Scholar
• CURRAN ME, SPLAWSKI I, TIMOTHY KW et al.: A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome. Cell (1995) 80:795-803.
   PubMed Web of Science ®Google Scholar
• HONDEGHEM LM: Thorough QT/QTc not so thorough: removes torsadogenic predictors from the T-wave, incriminates safe drugs, and misses profibrillatory drugs. J. Cardiovasc. Electrophysiol. (2006) 17(3):337-340.
   PubMed Web of Science ®Google Scholar
• HONDEGHEM LM, CARLSSON L, DUKER G: Instability and triangulation of the action potential predict serious proarrhythmia, but action potential duration prolongation is antiarrhythmic. Circulation (2001) 103(15):2004-2013.
   PubMed Web of Science ®Google Scholar
• WITCHEL HJ, HANCOX JC, NUTT DJ: Psychotropic drugs, cardiac arrhythmia, and sudden death. J. Clin. Psychopharmacol. (2003) 23(1):58-77.
   PubMed Web of Science ®Google Scholar
• LOWN B: Sudden cardiac death: biobehavioral perspective. Circulation (1987) 76(1 Pt. 2):I186-I196.
   Google Scholar
• SANGUINETTI MC, KEATING MT: Role of delayed rectifier potassium channels in cardiac repolarization and arrhythmias. News Physiol. Sci. (1997) 12:152-157.
   Google Scholar
• SCHWARTZ PJ, PERITI M, MALLIANI A: The long Q-T syndrome. Am. Heart J. (1975) 89(3):378-390.
   PubMed Web of Science ®Google Scholar
• SANGUINETTI MC, JURKIEWICZ NK: Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents. J. Gen. Physiol. (1990) 96(1):195-215.
   PubMed Web of Science ®Google Scholar
• SPECTOR PS, CURRAN ME, KEATING MT, SANGUINETTI MC: Class III antiarrhythmic drugs block HERG, a human cardiac delayed rectifier K+ channel. Open-channel block by methanesulfonanilides. Circ. Res. (1996) 78:499-503.
   PubMed Web of Science ®Google Scholar
• SNYDERS DJ, CHAUDHARY A: High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol. Pharm. (1996) 49:949-955.
   PubMed Web of Science ®Google Scholar
• LOMBARDI F, TERRANOVA P: Pharmacological treatment of atrial fibrillation: mechanisms of action and efficacy of class III drugs. Curr. Med. Chem. (2006) 13(14):1635-1653.
   PubMedGoogle Scholar
• CRUMB W, CAVERO I: QT interval prolongation by non-cardiovascular drugs: issues and solutions for novel drug development. Pharm. Sci. Technol. Today (1999) 2(7):270-280.
   PubMedGoogle Scholar
• REDFERN WS, CARLSSON L, DAVIS AS et al.: Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development. Cardiovasc. Res. (2003) 58(1):32-45.
   PubMed Web of Science ®Google Scholar
• ZHOU Z, GONG Q, YE B et al.: Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature. Biophys. J. (1998) 74:230-241.
   PubMed Web of Science ®Google Scholar
• HANCOX JC, LEVI AJ, WITCHEL HJ: Time course and voltage dependence of expressed HERG current compared with native ‘rapid’ delayed rectifier K current during the cardiac ventricular action potential. Pflügers Arch. (1998) 436:843-853.
   PubMed Web of Science ®Google Scholar
• JIANG Y, LEE A, CHEN J et al.: X-ray structure of a voltage-dependent K+ channel. Nature (2003) 423(6935):33-41.
   PubMed Web of Science ®Google Scholar
• MORAIS CABRAL JH, LEE A, COHEN SL et al.: Crystal structure and functional analysis of the HERG potassium channel N terminus: a eukaryotic PAS domain. Cell (1998) 95:649-655.
   PubMed Web of Science ®Google Scholar
• SMITH PL, BAUKROWITZ T, YELLEN G: The inward rectification mechanism of the HERG cardiac potassium channel. Nature (1996) 379:833-836.
   PubMed Web of Science ®Google Scholar
• AKHAVAN A, ATANASIU R, NOGUCHI T et al.: Identification of the cyclic-nucleotide-binding domain as a conserved determinant of ion-channel cell-surface localization. J. Cell Sci. (2005) 118(Pt. 13):2803-2812.
   PubMed Web of Science ®Google Scholar
• CUI J, MELMAN Y, PALMA E, FISHMAN GI, MCDONALD TV: Cyclic AMP regulates the HERG K+ channel by dual pathways. Curr. Biol. (2000) 10(11):671-674.
   PubMed Web of Science ®Google Scholar
• WIMMERS S, BAUER CK, SCHWARZ JR: Biophysical properties of heteromultimeric erg K+ channels. Pflügers Arch. (2002) 445(3):423-430.
   PubMedGoogle Scholar
• MACKINNON R: Determination of the subunit stoichiometry of a voltage-activated potassium channel. Nature (1991) 350(6315):232-235.
   PubMed Web of Science ®Google Scholar
• LONDON B, TRUDEAU MC, NEWTON KP et al.: Two isoforms of the mouse ether-a-go-go-related gene coassemble to form channels with properties similar to the rapidly activating component of the cardiac delayed rectifier K+ current. Circ. Res. (1997) 81:870-878.
   PubMed Web of Science ®Google Scholar
• LEES-MILLER JP, KONDO C, WANG L, DUFF HJ: Electrophysiological characterization of an alternatively processed ERG K+ channel in mouse and human hearts. Circ. Res. (1997) 81:719-726.
   PubMed Web of Science ®Google Scholar
• JONES EM, ROTI ROTI EC, WANG J, DELFOSSE SA, ROBERTSON GA: Cardiac IKr channels minimally comprise of HERG 1a and HERG 1b channels. J. Biol. Chem. (2004) 279(43):44690-44694.
   PubMed Web of Science ®Google Scholar
• KUPERSHMIDT S, SNYDERS DJ, RAES A, RODEN DM: A K+ channel splice variant common in human heart lacks a C-terminal domain required for expression of rapidly activating delayed rectifier current. J. Biol. Chem. (1998) 273:27231-27235.
   PubMedGoogle Scholar
• SHI W, WYMORE RS, WANG H-S et al.: Identification of two nervous system-specific members of the erg potassium channel gene family. J. Neurosci. (1997) 17(24):9423-9432.
   PubMed Web of Science ®Google Scholar
• MCDONALD TV, YU Z, MING Z et al.: A minK-HERG complex regulates the cardiac potassium current IKr. Nature (1997) 388:289-292.
   PubMed Web of Science ®Google Scholar
• ABBOTT GW, SESTI F, SPLAWSKI I et al.: MiRP1 forms IKr potassium channels with HERG and is associated with cardiac arrhythmia. Cell (1999) 97:175-187.
   PubMed Web of Science ®Google Scholar
• SESTI F, ABBOTT GW, WEI J et al.: A common polymorphism associated with antibiotic-induced cardiac arrhythmia. Proc. Natl. Acad. Sci. USA (2000) 97(19):10613-10618.
   PubMed Web of Science ®Google Scholar
• ZHANG M, JIANG M, TSENG GN: minK-related peptide 1 associates with Kv4.2 and modulates its gating function: potential role as β subunit of cardiac transient outward channel? Circ. Res. (2001) 88(10):1012-1019.
   PubMed Web of Science ®Google Scholar
• ABBOTT GW, GOLDSTEIN SA: Disease-associated mutations in KCNE potassium channel subunits (MiRPs) reveal promiscuous disruption of multiple currents and conservation of mechanism. FASEB J. (2002) 16(3):390-400.
   PubMedGoogle Scholar
• WEERAPURA M, NATTEL S, CHARTIER D, CABALLERO R, HEBERT TE: 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. (2002) 540(Pt. 1):15-27.
   PubMedGoogle Scholar
• LONG SB, CAMPBELL EB, MACKINNON R: Crystal structure of a mammalian voltage-dependent Shaker family K+ channel. Science (2005) 309(5736):897-903.
   PubMed Web of Science ®Google Scholar
• VANDENBERG JI, WALKER BD, CAMPBELL TJ: HERG K+ channels: friend and foe. Trends Pharmacol. Sci. (2001) 22(5):240-246.
   PubMed Web of Science ®Google Scholar
• MITCHESON JS, CHEN J, SANGUINETTI MC: Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate. J. Gen. Physiol. (2000) 115(3):229-240.
   PubMed Web of Science ®Google Scholar
• MITCHESON JS, PERRY MD: Molecular determinants of high-affinity drug binding to HERG channels. Curr. Opin. Drug Discov. Devel. (2003) 6(5):667-674.
   PubMed Web of Science ®Google Scholar
• MITCHESON JS, CHEN J, LIN M, CULBERSON C, SANGUINETTI MC: A structural basis for drug-induced long QT syndrome. Proc. Natl. Acad. Sci. USA (2000) 97(22):12329-12333.
   PubMed Web of Science ®Google Scholar
• WITCHEL HJ, DEMPSEY CE, SESSIONS RB et al.: The low potency, voltage-dependent HERG blocker propafenone – molecular determinants and drug trapping. Mol. Pharmacol. (2004) 66(5):1201-1212.
   PubMed Web of Science ®Google Scholar
• FERNANDEZ D, GHANTA A, KAUFFMAN GW, SANGUINETTI MC: Physicochemical features of the HERG channel drug binding site. J. Biol. Chem. (2004) 279(11):10120-10127.
   PubMed Web of Science ®Google Scholar
• ZOU A, XU QP, SANGUINETTI MC: A mutation in the pore region of HERG K+ channels expressed in Xenopus oocytes reduces rectification by shifting the voltage dependence of inactivation. J. Physiol. (London) (1998) 509(Pt. 1):129-137.
   PubMed Web of Science ®Google Scholar
• HANCOX JC, WITCHEL HJ, VARGHESE A: Alteration of HERG current profile during the cardiac ventricular action potential, following a pore mutation. Biochem. Biophys. Res. Commun. (1998) 253(3):719-724.
   PubMed Web of Science ®Google Scholar
• LEES-MILLER JP, DUAN Y, TENG GQ, DUFF HJ: Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites. Mol. Pharmacol. (2000) 57(2):367-374.
   PubMed Web of Science ®Google Scholar
• PAUL A, WITCHEL HJ, HANCOX JC: Inhibition of HERG potassium channel current by the class 1a antiarrhythmic agent disopyramide. Biochem. Biophys. Res. Commun. (2001) 280:1243-1250.
   PubMed Web of Science ®Google Scholar
• FICKER E, JAROLIMEK W, BROWN AM: Molecular determinants of inactivation and dofetilide block in ether a-go-go (EAG) channels and EAG-related K+ channels. Mol. Pharmacol. (2001) 60(6):1343-1348.
   PubMed Web of Science ®Google Scholar
• CHEN J, SEEBOHM G, SANGUINETTI MC: Position of aromatic residues in the S6 domain, not inactivation, dictates cisapride sensitivity of HERG and eag potassium channels. Proc. Natl. Acad. Sci. USA (2002) 99(19):12461-12466.
   PubMed Web of Science ®Google Scholar
• LAFUENTE-LAFUENTE C, MOULY S, LONGAS-TEJERO MA, MAHE I, BERGMANN JF: Antiarrhythmic drugs for maintaining sinus rhythm after cardioversion of atrial fibrillation: a systematic review of randomized controlled trials. Arch. Intern. Med. (2006) 166(7):719-728.
   PubMed Web of Science ®Google Scholar
• CAMM J: Medical management of atrial fibrillation: state of the art. J. Cardiovasc. Electrophysiol. (2006) 17(Suppl. 2):S2-S6.
   Web of Science ®Google Scholar
• WYSE DG, WALDO AL, DIMARCO JP et al.: A comparison of rate control and rhythm control in patients with atrial fibrillation. N. Engl. J. Med. (2002) 347(23):1825-1833.
   PubMed Web of Science ®Google Scholar
• Committee for Proprietary Medicinal Products: Points to consider: the assessment for the potential for QT prolongation by non-cardiovascular medicinal products (1997); Report # CPMP/986/96, European Agency for the Evaluation of Medicinal Products, London, UK.
   Google Scholar
• ICH (Expert Working Group (safety) of the international conference on harmonisation of technical requirements for registration of pharmaceuticals for human use): S7A Safety Pharmacology Studies for Human Pharmaceuticals: Guidance for Industry (2001). FDA: Rockville, Maryland, USA.
   Google Scholar
• BEDNAR MM, HARRIGAN EP, RUSKIN JN: Torsades de pointes associated with nonantiarrhythmic drugs and observations on gender and QTc. Am. J. Cardiol. (2002) 89(11):1316-1319.
   PubMed Web of Science ®Google Scholar
• MAKKAR RR, FROMM BS, STEINMAN RT, MEISSNER MD, LEHMANN MH: Female gender as a risk factor for torsades de pointes associated with cardiovascular drugs. JAMA (1993) 270(21):2590-2597.
   PubMed Web of Science ®Google Scholar
• ICH (Expert Working Group (safety) of the international conference on harmonisation of technical requirements for Registration of pharmaceuticals for human use): The non-clinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals, S7B (2005). FDA: Rockville, Maryland, USA.
   Google Scholar
• WITCHEL HJ, MILNES JT, MITCHESON JS, HANCOX JC: Troubleshooting a heterologous potassium channel current used for in vitro screening for QT interval prolongation: HERG, mammalian cell lines and Xenopus oocytes. J. Pharmacol. Toxicol. Methods (2003) 48:65-80.
   Web of Science ®Google Scholar
• KIRSCH GE, TREPAKOVA ES, BRIMECOMBE JC et al.: Variability in the measurement of hERG potassium channel inhibition: effects of temperature and stimulus pattern. J. Pharmacol. Toxicol. Methods (2004) 50(2):93-101.
   PubMedGoogle Scholar
• FINLAYSON K, TURNBULL L, JANUARY CT, SHARKEY J, KELLY JS: [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur. J Pharmacol. (2001) 430(1):147-148.
   PubMed Web of Science ®Google Scholar
• CHIU PJ, MARCOE KF, BOUNDS SE et al.: Validation of a [3H] astemizole binding assay in HEK293 cells expressing HERG K+ channels. J. Pharmacol. Sci. (2004) 95(3):311-319.
   PubMed Web of Science ®Google Scholar
• WANG J, DELLA PK, WANG H et al.: Functional and pharmacological properties of canine ERG potassium channels. Am. J Physiol Heart Circ. Physiol (2003) 284(1):H256-H267.
   Google Scholar
• ZHOU Z, VORPERIAN VR, GONG Q, ZHANG S, JANUARY CT: Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J. Cardiovasc. Electrophysiol. (1999) 10(6):836-843.
   PubMed Web of Science ®Google Scholar
• KAMIYA K, NIWA R, MITCHESON JS, SANGUINETTI MC: Molecular determinants of HERG channel block. Mol. Pharmacol. (2006) 69(5):1709-1716.
   PubMed Web of Science ®Google Scholar
• WEBSTER R, LEISHMAN D, WALKER D: Towards a drug concentration effect relationship for QT prolongation and torsades de pointes. Curr. Opin. Drug Discov. Devel. (2002) 5(1):116-126.
   PubMed Web of Science ®Google Scholar
• ANGELO K, KOROLKOVA YV, GRUNNET M et al.: A radiolabeled peptide ligand of the hERG channel, [125I]-BeKm-1. Pflügers Arch. (2003) 447(1):55-63.
   PubMedGoogle Scholar
• ZHANG M, KOROLKOVA YV, LIU J et al.: BeKm-1 is a HERG-specific toxin that shares the structure with ChTx but the mechanism of action with ErgTx1. Biophys. J. (2003) 84(5):3022-3036.
   PubMedGoogle Scholar
• TANG W, KANG J, WU X et al.: Development and evaluation of high throughput functional assay methods for HERG potassium channel. J. Biomol. Screen. (2001) 6(5):325-331.
   PubMed Web of Science ®Google Scholar
• SOROTA S, ZHANG XS, MARGULIS M, TUCKER K, PRIESTLEY T: Characterization of a hERG screen using the IonWorks HT: comparison to a hERG rubidium efflux screen. Assay. Drug Dev. Technol. (2005) 3(1):47-57.
   PubMed Web of Science ®Google Scholar
• NETZER R, EBNETH A, BISCHOFF U, PONGS O: Screening lead compounds for QT interval prolongation. Drug Discov. Today. (2001) 6(2):78-84.
   PubMed Web of Science ®Google Scholar
• DUBIN AE, NASSER N, ROHRBACHER J et al.: Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp. J. Biomol. Screen. (2005) 10(2):168-181.
   PubMed Web of Science ®Google Scholar
• KISS L, BENNETT PB, UEBELE VN et al.: High throughput ion-channel pharmacology: planar-array-based voltage clamp. Assay. Drug Dev. Technol. (2003) 1(1 Pt. 2):127-135.
   PubMed Web of Science ®Google Scholar
• FINKEL A, WITTEL A, YANG N et al.: Population patch clamp improves data consistency and success rates in the measurement of ionic currents. J. Biomol. Screen. (2006) 11(5):488-496.
   PubMed Web of Science ®Google Scholar
• GUSSAK I, BRUGADA P, BRUGADA J et al.: Idiopathic short QT interval: a new clinical syndrome? Cardiology (2000) 94(2):99-102.
   PubMed Web of Science ®Google Scholar
• BJERREGAARD P, JAHANGIR A, GUSSAK I: Targeted therapy for short QT syndrome. Expert Opin. Ther. Targets (2006) 10(3):393-400.
   PubMed Web of Science ®Google Scholar
• GAITA F, GIUSTETTO C, BIANCHI F et al.: Short QT Syndrome: a familial cause of sudden death. Circulation (2003) 108(8):965-970.
   PubMed Web of Science ®Google Scholar
• BRUGADA R, HONG K, DUMAINE R et al.: Sudden death associated with short-QT syndrome linked to mutations in HERG. Circulation (2004) 109(1):30-35.
   PubMed Web of Science ®Google Scholar
• MCPATE MJ, WITCHEL HJ, HANCOX JC: Short QT syndrome. Fut. Cardiol. (2006) 2(3):293-301.
   PubMedGoogle Scholar
• CLARKE CE, HILL AP, ZHAO J et al.: Effect of S5P α-helix charge mutants on inactivation of hERG K+ channels. J. Physiol. (2006) 573(Pt. 2):291-304.
   PubMed Web of Science ®Google Scholar
• HONG K, BJERREGAARD P, GUSSAK I, BRUGADA R: Short QT syndrome and atrial fibrillation caused by mutation in KCNH2. J. Cardiovasc. Electrophysiol. (2005) 16(4):394-396.
   PubMed Web of Science ®Google Scholar
• CORDEIRO JM, BRUGADA R, WU YS, HONG K, DUMAINE R: Modulation of IKr inactivation by mutation N588K in KCNH2: a link to arrhythmogenesis in short QT syndrome. Cardiovasc. Res. (2005) 67(3):498-509.
   PubMed Web of Science ®Google Scholar
• MCPATE MJ, DUNCAN RS, MILNES JT, WITCHEL HJ, HANCOX JC: The N588K-HERG K+ channel mutation in the ‘short QT syndrome’: mechanism of gain-in-function determined at 37 °C. Biochem. Biophys. Res. Commun. (2005) 334(2):441-449.
   PubMed Web of Science ®Google Scholar
• SCHIMPF R, WOLPERT C, BIANCHI F et al.: Congenital short QT syndrome and implantable cardioverter defibrillator treatment: inherent risk for inappropriate shock delivery. J Cardiovasc. Electrophysiol. (2003) 14(12):1273-1277.
   PubMed Web of Science ®Google Scholar
• GAITA F, GIUSTETTO C, BIANCHI F et al.: Short QT syndrome: pharmacological treatment. J. Am. Coll. Cardiol. (2004) 43(8):1494-1499.
   PubMed Web of Science ®Google Scholar
• MILNES JT, CROCIANI O, ARCANGELI A, HANCOX JC, WITCHEL HJ: Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652. Br. J. Pharmacol. (2003) 139(5):887-898.
   PubMed Web of Science ®Google Scholar
• MCPATE MJ, DUNCAN RS, WITCHEL HJ, HANCOX JC: Disopyramide is an effective inhibitor of mutant HERG K(+) channels involved in variant 1 short QT syndrome. J. Mol. Cell Cardiol. (2006) 41(3):563-566.
   PubMed Web of Science ®Google Scholar
• GUSSAK I, BJERREGAARD P: Short QT syndrome – 5 years of progress. J. Electrocardiol. (2005) 38(4):375-377.
   PubMedGoogle Scholar
• ARCANGELI A: Expression and role of hERG channels in cancer cells. Novartis Found. Symp. (2005) 266:225-232.
   PubMedGoogle Scholar
• CHERUBINI A, TADDEI GL, CROCIANI O et al.: HERG potassium channels are more frequently expressed in human endometrial cancer as compared to non-cancerous endometrium. Br. J. Cancer (2000) 83(12):1722-1729.
   PubMedGoogle Scholar
• LASTRAIOLI E, GUASTI L, CROCIANI O et al.: herg1 gene and herg1 protein are overexpressed in colorectal cancers and regulate cell invasion of tumor cells. Cancer Res. (2004) 64(2):606-611.
   PubMed Web of Science ®Google Scholar
• HOFMANN G, BERNABEI PA, CROCIANI O et al.: HERG K+ channels activation during β1 integrin-mediated adhesion to fibronectin induces an up-regulation of αvβ3 integrin in the preosteoclastic leukemia cell line FLG 29.1. J. Biol. Chem. (2001) 276(7):4923-4931.
   PubMed Web of Science ®Google Scholar
• PILLOZZI S, BRIZZI MF, BALZI M et al.: HERG potassium channels are constitutively expressed in primary human acute myeloid leukemias and regulate cell proliferation of normal and leukemic hemopoietic progenitors. Leukemia (2002) 16(9):1791-1798.
   PubMed Web of Science ®Google Scholar
• SMITH GA, TSUI HW, NEWELL EW et al.: Functional up-regulation of HERG K+ channels in neoplastic hematopoietic cells. J. Biol. Chem. (2002) 277(21):18528-18534.
   PubMed Web of Science ®Google Scholar
• BIANCHI L, WIBLE B, ARCANGELI A et al.: herg encodes a K+ current highly conserved in tumors of different histogenesis: a selective advantage for cancer cells? Cancer Res. (1998) 58(4):815-822.
   PubMed Web of Science ®Google Scholar
• CROCIANI O, GUASTI L, BALZI M et al.: Cell cycle-dependent expression of HERG1 and HERG1B isoforms in tumor cells. J. Biol. Chem. (2003) 278(5):2947-2955.
   PubMed Web of Science ®Google Scholar
• HOFMANN G, BERNABEI PA, CROCIANI O et al.: HERG K+ channels activation during β1 integrin-mediated adhesion to fibronectin induces an up-regulation of αvβ3 integrin in the preosteoclastic leukemia cell line FLG 29.1. J. Biol. Chem. (2001) 276(7):4923-4931.
   PubMed Web of Science ®Google Scholar
• MASI A, BECCHETTI A, RESTANO-CASSULINI R et al.: hERG1 channels are overexpressed in glioblastoma multiforme and modulate VEGF secretion in glioblastoma cell lines. Br. J. Cancer (2005) 93(7):781-792.
   PubMedGoogle Scholar
• GLASS DJ: Signalling pathways that mediate skeletal muscle hypertrophy and atrophy. Nat. Cell Biol. (2003) 5(2):87-90.
   PubMed Web of Science ®Google Scholar
• WANG X, HOCKERMAN GH, GREEN HW, III et al.: Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J. (2006) 20(9):1531-1533.
   PubMedGoogle Scholar
• ECHT DS, LIEBSON PR, MITCHELL LB et al.: Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmia Suppression Trial. N. Engl. J. Med. (1991) 324(12):781-788.
   PubMed Web of Science ®Google Scholar
• COLATSKY TJ, FOLLMER CH, STARMER CF: Channel specificity in antiarrhythmic drug action: mechanism of potassium channel block and its role in suppressing and aggravating cardiac arrhythmias. Circulation (1990) 72:1092-1103.
   Google Scholar
• ANDERSON JL, PRYSTOWSKY EN: Sotalol: An important new antiarrhythmic. Am. Heart J. (1999) 137(3):388-409.
   PubMed Web of Science ®Google Scholar
• SINGH BN: Electrophysiologic basis for the antiarrhythmic actions of sotalol and comparison with other agents. Am. J. Cardiol. (1993) 72(4):8A-18A.
   PubMedGoogle Scholar
• WALDO AL, CAMM AJ, DERUYTER H et al.: Effect of d-sotalol on mortality in patients with left ventricular dysfunction after recent and remote myocardial infarction. The SWORD Investigators. Survival with oral d-sotalol. Lancet (1996) 348(9019):7-12.
   PubMed Web of Science ®Google Scholar
• PERRY M, DE GROOT MJ, HELLIWELL R et al.: Structural determinants of HERG channel block by clofilium and ibutilide. Mol. Pharmacol. (2004) 66(5):240-249.
   PubMed Web of Science ®Google Scholar
• MILNES JT, DEMPSEY CE, RIDLEY JM et al.: Preferential closed channel blockade of HERG potassium currents by chemically synthesised BeKm-1 scorpion toxin. FEBS Lett. (2003) 547(1-3):20-26.
   PubMedGoogle Scholar
• TESCHEMACHER AG, SEWARD EP, HANCOX JC, WITCHEL HJ: Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline. Br. J. Pharmacol. (1999) 128(2):479-485.
   PubMed Web of Science ®Google Scholar
• RIDLEY JM, MILNES JT, WITCHEL HJ, HANCOX JC: High affinity HERG K+ channel blockade by the antiarrhythmic agent dronedarone: resistance to mutations of the S6 residues Y652 and F656. Biochem. Biophys. Res. Commun. (2004) 325(3):883-891.
   PubMed Web of Science ®Google Scholar
• KANG J, CHEN XL, WANG H et al.: Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol. Pharmacol. (2005) 67(3):827-836.
   PubMedGoogle Scholar
• HANSEN RS, DINESS TG, CHRIST T et al.: Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643). Mol. Pharmacol. (2006) 69(1):266-277.
   PubMedGoogle Scholar
• HANSEN RS, DINESS TG, CHRIST T et al.: Biophysical characterization of the new human ether-a-go-go-related gene channel opener NS3623 [N-(4-bromo-2-(1H-tetrazol-5-yl)-phenyl)-N′-(3′-trifluoromethylphenyl)urea]. Mol. Pharmacol. (2006) 70:1319-1329.
   PubMedGoogle Scholar
• ZHOU J, AUGELLI-SZAFRAN CE, BRADLEY JA et al.: Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity. Mol. Pharmacol. (2005) 68:876-884.
   PubMed Web of Science ®Google Scholar
• ZENG H, LOZINSKAYA IM, LIN Z et al.: Mallotoxin is a novel human ether-a-go-go-related gene (hERG) potassium channel activator. J. Pharmacol. Exp. Ther. (2006) 319(2):957-962.
   PubMedGoogle Scholar
• CASIS O, OLESEN SP, SANGUINETTI MC: Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol. Pharmacol. (2006) 69(2):658-665.
   PubMedGoogle Scholar
• THOMAS D, ZHANG W, KARLE CA et al.: Deletion of protein kinase A phosphorylation sites in the HERG potassium channel inhibits activation shift by protein kinase A. J. Biol. Chem. (1999) 274(39):27457-27462.
   PubMedGoogle Scholar
• KIEHN J, KARLE C, THOMAS D et al.: HERG potassium channel activation is shifted by phorbol esters via protein kinase A-dependent pathways. J. Biol. Chem. (1998) 273(39):25285-25291.
   PubMedGoogle Scholar
• THOMAS D, ZHANG W, WU K et al.: Regulation of HERG potassium channel activation by protein kinase C independent of direct phosphorylation of the channel protein. Cardiovasc. Res. (2003) 59(1):14-26.
   PubMedGoogle Scholar
• ZHOU Z, GONG Q, JANUARY CT: Correction of defective protein trafficking of a mutant HERG potassium channel in human long QT syndrome. Pharmacological and temperature effects. J. Biol. Chem. (1999) 274(44):31123-31126.
   PubMed Web of Science ®Google Scholar
• FICKER E, OBEJERO-PAZ CA, ZHAO S, BROWN AM: The binding site for channel blockers that rescue misprocessed human long QT syndrome Type 2 ether-a-gogo-related gene (HERG) mutations. J. Biol. Chem. (2002) 277(7):4989-4998.
   PubMed Web of Science ®Google Scholar
• DELISLE BP, ANDERSON CL, BALIJEPALLI RC et al.: Thapsigargin selectively rescues the trafficking-defective LQT2 channels G601S and F805C. J. Biol. Chem. (2003) 278(37):35749-54357.
   PubMed Web of Science ®Google Scholar
• RAJAMANI S, ANDERSON CL, ANSON BD, JANUARY CT: Pharmacological rescue of human K+ channel long-QT2 mutations: human ether-a-go-go-related gene rescue without block. Circulation (2002) 105(24):2830-2835.
   PubMed Web of Science ®Google Scholar
• FICKER E, DENNIS AT, WANG L, BROWN AM: Role of the cytosolic chaperones Hsp70 and Hsp90 in maturation of the cardiac potassium channel HERG. Circ. Res. (2003) 92(12):e87-e100.
   PubMed Web of Science ®Google Scholar
• ANDERSON CL, DELISLE BP, ANSON BD et al.: Most LQT2 mutations reduce Kv11.1 (hERG) current by a class 2 (trafficking-deficient) mechanism. Circulation (2006) 113(3):365-373.
   PubMed Web of Science ®Google Scholar
• HOLLON T: Researchers and regulators reflect on first gene therapy death. Nat. Med. (2000) 6(1):6.
   PubMed Web of Science ®Google Scholar
• CHOUABE C, DRICI MD, ROMEY G, BARHANIN J, LAZDUNSKI M: HERG and KvLQT1/IsK, the cardiac K+ channels involved in long QT syndromes, are targets for calcium channel blockers. Mol. Pharm. (1998) 54(4):695-703.
   PubMed Web of Science ®Google Scholar
• RIDLEY JM, MILNES JT, HANCOX JC, WITCHEL HJ: Clemastine, a conventional antihistamine, is a high potency inhibitor of the HERG K+ channel. J. Mol. Cell Cardiol. (2006) 40(1):107-118.
   PubMed Web of Science ®Google Scholar
• WITCHEL HJ, PABBATHI VK, HOFMANN G, PAUL AA, HANCOX JC: Inhibitory actions of the selective serotonin re-uptake inhibitor citalopram on HERG and ventricular L-type calcium currents. FEBS Lett. (2002) 512(1-3):59-66.
   PubMed Web of Science ®Google Scholar
• PACHER P, BAGI Z, LAKO-FUTO Z et al.: Cardiac electrophysiological effects of citalopram in guinea pig papillary muscle comparison with clomipramine. Gen. Pharmacol. (2000) 34(1):17-23.
   PubMedGoogle Scholar
• CARLSSON L: In vitro and in vivo models for testing arrhythmogenesis in drugs. J. Intern. Med. (2006) 259(1):70-80.
   PubMed Web of Science ®Google Scholar
• CARLSSON L, ABRAHAMSSON C, ANDERSSON B, DUKER G, SCHILLER-LINHARDT G: Proarrhythmic effects of the class III agent almokalant: importance of infusion rate, QT dispersion, and early afterdepolarisations. Cardiovasc. Res. (1993) 27(12):2186-2193.
   PubMed Web of Science ®Google Scholar
• HONDEGHEM LM: TRIad: foundation for proarrhythmia (triangulation, reverse use dependence and instability). Novartis Found. Symp. (2005) 266:235-244.
   PubMedGoogle Scholar
• HONDEGHEM LM, DUJARDIN K, DE CLERCK F: Phase II prolongation, in the absence of instability and triangulation, antagonizes class III proarrhythmia. Cardiovasc. Res. (2001) 50(2):345-353.
   PubMed Web of Science ®Google Scholar
• TESTAI L, CALDERONE V, SALVADORI A et al.: QT prolongation in anaesthetized guinea-pigs: an experimental approach for preliminary screening of torsadogenicity of drugs and drug candidates. J. Appl. Toxicol. (2004) 24(3):217-222.
   PubMedGoogle Scholar
• LANGHEINRICH U, VACUN G, WAGNER T: Zebrafish embryos express an orthologue of HERG and are sensitive toward a range of QT-prolonging drugs inducing severe arrhythmia. Toxicol. Appl. Pharmacol. (2003) 193(3):370-382.
   PubMed Web of Science ®Google Scholar
• JAMIESON C, MOIR EM, RANKOVIC Z, WISHART G: Medicinal chemistry of hERG optimizations: Highlights and hang-ups. J. Med. Chem. (2006) 49(17):5029-5046.
   PubMed Web of Science ®Google Scholar
• ZHU BY, JIA ZJ, ZHANG P et al.: Inhibitory effect of carboxylic acid group on hERG binding. Bioorg. Med. Chem. Lett. (2006) 16(21):5507-5512.
   PubMed Web of Science ®Google Scholar
• VANDENBERG JI, TORRES AM, CAMPBELL TJ, KUCHEL PW: The HERG K+ channel: progress in understanding the molecular basis of its unusual gating kinetics. Eur. Biophys. J. (2004) 33(2):89-97.
   PubMedGoogle Scholar
• RODEN DM: Pharmacogenetics and drug-induced arrhythmias. Cardiovasc. Res. (2001) 50(2):224-231.
   PubMed Web of Science ®Google Scholar
• WALKER BD, KRAHN AD, KLEIN GJ et al.: Congenital and acquired long QT syndromes. Can. J. Cardiol. (2003) 19(1):76-87.
   PubMedGoogle Scholar
• PUDDU PE, CRINITI A, MONTI F: Screening for drug-induced (acquired) long QT syndrome: is it time to apply new methods? Eur. Heart J. (2001) 22(5):363-369.
   PubMedGoogle Scholar
• PAULUSSEN AD, GILISSEN RA, ARMSTRONG M et al.: Genetic variations of KCNQ1, KCNH2, SCN5A, KCNE1, and KCNE2 in drug-induced long QT syndrome patients. J. Mol. Med. (2004) 82(3):182-188.
   PubMed Web of Science ®Google Scholar