Hexachlorophene Is a Potent KCNQ1/KCNE1 Potassium Channel Activator Which Rescues LQTs Mutants

PLoS ONE

Volumn 7, Issue 12, 2012, Pages

  Zheng, Yueming ^a   Zhu, Xuejing ^a   Zhou, Pingzheng ^a   Lan, Xi ^a   Xu, Haiyan ^a   Li, Min ^a,b   Gao, Zhaobing ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ENZYME ACTIVATOR; HEXACHLOROPHENE; PHOSPHATIDYLINOSITOL 4,5 BISPHOSPHATE; POTASSIUM CHANNEL KCNE1; POTASSIUM CHANNEL KCNQ1;

ACTION POTENTIAL DURATION; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CARDIOVASCULAR PARAMETERS; CHANNEL GATING; CONCENTRATION (PARAMETERS); CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG POTENTIATION; DRUG SCREENING; DRUG STRUCTURE; ELECTRICAL POTENTIAL PARAMETERS; GUINEA PIG; HEART MUSCLE CELL; HEART MUSCLE POTENTIAL; LONG QT SYNDROME; LOSS OF FUNCTION MUTATION; MEDIAN EFFECTIVE CONCENTRATION; NONHUMAN; PROTEIN BINDING; PROTEIN EXPRESSION; PROTEIN STABILITY;

ACTION POTENTIALS; ANIMALS; CELL LINE; CHO CELLS; CRICETINAE; HEART; HEXACHLOROPHENE; KCNQ1 POTASSIUM CHANNEL; LONG QT SYNDROME; MUTATION; MYOCYTES, CARDIAC; PHOSPHATIDYLINOSITOL 4,5-DIPHOSPHATE;

EID: 84871233474     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0051820     Document Type: Article

References (34)

1. Robbins J, (2001) KCNQ potassium channels: physiology, pathophysiology, and pharmacology. Pharmacol Ther 90: 1-19.
2. Barhanin J, Lesage F, Guillemare E, Fink M, Lazdunski M, et al. (1996) K(V)LQT1 and lsK (minK) proteins associate to form the I(Ks) cardiac potassium current. Nature 384: 78-80.
3. Sanguinetti MC, Curran ME, Zou A, Shen J, Spector PS, et al. (1996) Coassembly of K(V)LQT1 and minK (IsK) proteins to form cardiac I(Ks) potassium channel. Nature 384: 80-3.
4. Bianchi L, Priori SG, Napolitano C, Surewicz KA, Dennis AT, et al. (2000) Mechanisms of I(Ks) suppression in LQT1 mutants, Am J Physiol Heart Circ Physiol. 279: H3003-11.
5. Napolitano C, Schwartz PJ, Brown AM, Ronchetti E, Bianchi L, et al. (2000) Evidence for a cardiac ion channel mutation underlying drug-induced QT prolongation and life-threatening arrhythmias. J Cardiovasc Electrophysiol 11: 691-6.
6. Splawski I, Shen J, Timothy KW, Lehmann MH, Priori S, et al. (2000) Spectrum of mutations in long-QT syndrome genes. KVLQT1, HERG, SCN5A, KCNE1, and KCNE2. Circulation 102: 1178-85.
7. Herbert E, Trusz-Gluza M, Moric E, Smilowska-Dzielicka E, Mazurek U, et al. (2002) KCNQ1 gene mutations and the respective genotype-phenotype correlations in the long QT syndrome. Med Sci Monit 8: RA240-8.
8. Brown DA, (2009) Passmore GM, (2009) Neural KCNQ (Kv7) channels. Br J Pharmacol 156: 1185-95.
9. Xiong Q, Gao Z, Wang W & Li M, (2008) Activation of Kv7 (KCNQ) voltage-gated potassium channels by synthetic compounds. Trends Pharmacol Sci 29: 99-107.
10. Jia C, Qi J, Zhang F, Mi Y, Zhang X, et al. (2011) Activation of KCNQ2/3 potassium channels by novel pyrazolo [1,5-a] pyrimidin-7(4H)-one derivatives. Pharmacology 87: 297-310.
11. Gribkoff VK, (2008) The therapeutic potential of neuronal KV7 (KCNQ) channel modulators: an update. Expert Opin Ther Targets 12: 565-81.
12. Wickenden AD, (2009) McNaughton-Smith G, (2009) Kv7 channels as targets for the treatment of pain. Curr Pharm Des 15: 1773-98.
13. Gao Z, Xiong Q, Sun H & Li M, (2008) Desensitization of chemical activation by auxiliary subunits: convergence of molecular determinants critical for augmenting KCNQ1 potassium channels. J Biol Chem 283: 22649-58.
14. Salata JJ, Jurkiewicz NK, Wang J, Evans BE, Orme H T, et al. (1998) A novel benzodiazepine that activates cardiac slow delayed rectifier K+ currents. Mol Pharmacol 54: 220-30.
15. Peretz A, Degani N, Nachman R, Uziyel Y, Gibor G, et al. (2005) Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties. Mol Pharmacol 67: 1053-66.
16. Karen Mruk, William RK, (2009) Discovery of a Novel Activator of KCNQ1-KCNE1 K+ Channel Complexes. PLoS ONE 4: e4236.
17. Jungermann E, (1968) Soap bacteriostats. J Am Oil Chem Soc 45: 345-50.
18. Akao M, Ohler A, O'Rourke B & Marban E, (2001) Mitochondrial ATP-sensitive potassium channels inhibit apoptosis induced by oxidative stress in cardiac cells. Circ Res 88: 1267-75.
19. Hedley PL, Jorgensen P, Schlamowitz S, Wangari R, Moolman-Smook J, et al. (2009) The genetic basis of long QT and short QT syndromes: a mutation update. Hum Mutat 30: 1486-511.
20. Franqueza L, Lin M, Shen J, Splawski I, Keating M T, et al. (1999) Long QT syndrome-associated mutations in the S4-S5 linker of KvLQT1 potassium channels modify gating and interaction with minK subunits. J Biol Chem 274: 21063-70.
21. Park KH, Piron J, Dahimene S, Merot J, Baro I, et al. (2005) Impaired KCNQ1-KCNE1 and phosphatidylinositol-4,5-bisphosphate interaction underlies the long QT syndrome. Circ Res 96: 730-9.
22. Hsu JT, Kuo CJ, Hsieh HP, Wang YC, Huang KK, et al. (2004) Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV. FEBS Lettn 574: 116-20.
23. Heath RJ, Li J, Roland GE, (2000) Rock CO, (2000) Inhibition of the Staphylococcus aureus NADPH-dependent enoyl-acyl carrier protein reductase by triclosan and hexachlorophene. J Biol Chem 275: 4654-9.
24. Park S, Gwak J, Cho M, Song T, Won J, et al. (2006) Hexachlorophene inhibits Wnt/beta-catenin pathway by promoting Siah-mediated beta-catenin degradation. Mol Pharmacol 70: 960-6.
25. Seebohm G, Pusch M, Chen J & Sanguinetti M C, (2003) Pharmacological activation of normal and arrhythmia-associated mutant KCNQ1 potassium channels. Circ Res 93: 941-7.
26. Busch AE, Busch GL, Ford E, Suessbrich H, Lang HJ, et al. (1997) The role of the IsK protein in the specific pharmacological properties of the IKs channel complex. Br J Pharmacol. 122: 187-9.
27. Abitbol I, Peretz A, Lerche C, Busch AE, (1999) Attali B, (1999) Stilbenes and fenamates rescue the loss of I(KS) channel function induced by an LQT5 mutation and other IsK mutants. Embo J 18: 4137-48.
28. Vatta M, Li H, (2000) Towbin JA, (2000) Molecular biology of arrhythmic syndromes. Curr Opin Cardiol 15: 12-22.
29. Wollnik B, Schroeder BC, Kubisch C, Esperer HD, Wieacker P, et al. (1997) Pathophysiological mechanisms of dominant and recessive KVLQT1 K+ channel mutations found in inherited cardiac arrhythmias, Hum Mol Genet. 6: 1943-9.
30. Chouabe C, Neyroud N, Richard P, Denjoy I, Hainque B, et al. (2000) Novel mutations in KvLQT1 that affect Iks activation through interactions with Isk. Cardiovasc Res 45: 971-80.
31. Yamashita F, Horie M, Kubota T, Yoshida H, Yumoto Y, et al. (2001) Characterization and subcellular localization of KCNQ1 with a heterozygous mutation in the C terminus. J Mol Cell Cardiol 33: 197-207.
32. Suh BC, (2005) Hille B, (2005) Regulation of ion channels by phosphatidylinositol 4,5-bisphosphate. Curr Opin Neurobiol 15: 370-8.
33. Suh BC, (2008) Hille B, (2008) PIP2 is a necessary cofactor for ion channel function: how and why?. Annu Rev Biophys 37: 175-95.
34. Li Y, Zaydman MA, Wu D, Shi J, Guan M, et al. (2011) KCNE1 enhances phosphatidylinositol 4,5-bisphosphate (PIP2) sensitivity of IKs to modulate channel activity. Proc Natl Acad Sci U S A 108: 9095-100.