Ginsenoside Rg3 activates human KCNQ1 K+ channel currents through interacting with the K318 and V319 residues: A role of KCNE1 subunit

European Journal of Pharmacology

Volumn 637, Issue 1-3, 2010, Pages 138-147

  Choi, Sun Hye ^a   Shin, Tae Joon ^a   Lee, Byung Hwan ^a   Chu, Dae hyun ^b   Choe, Han ^b   Pyo, Mi Kyung ^a   Hwang, Sung Hee ^a   Kim, Bo Ra ^a   Lee, Sang Mok ^a   Lee, Jun Ho ^c   Kim, Dong Hyun ^d   Kim, Hyoung Chun ^e   Rhim, Hye whon ^f   Nah, Seung Yeol ^a  

^a Konkuk University   (South Korea)

^b University of Ulsan College of Medicine   (South Korea)

^c Kyung Hee University   (South Korea)

^d Kyung Hee University   (South Korea)

^e Kangwon National University   (South Korea)

^f Korea Institute of Science and Technology   (South Korea)

Author keywords

Ginseng; Ginsenoside; Heart; Interaction site; KCNQ channel

Indexed keywords

GINSENOSIDE RG 3; POTASSIUM CHANNEL KCNE1; POTASSIUM CHANNEL KCNQ1; GINSENOSIDE; KCNE1 PROTEIN, HUMAN; LYSINE; PROTEIN SUBUNIT; VALINE; VOLTAGE GATED POTASSIUM CHANNEL;

ANIMAL CELL; ARTICLE; CHANNEL GATING; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG PROTEIN BINDING; DRUG STABILITY; DRUG STRUCTURE; IC 50; MOLECULAR DOCKING; NONHUMAN; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN INTERACTION; PROTEIN QUATERNARY STRUCTURE; STRUCTURE ANALYSIS; XENOPUS; ACTION POTENTIAL; ANIMAL; CHEMISTRY; DOSE RESPONSE; DRUG EFFECT; DRUG POTENTIATION; ENZYME ACTIVE SITE; GENETICS; GINSENG; HUMAN; METABOLISM; MUTATION; NUCLEOTIDE SEQUENCE; PHYSIOLOGY; XENOPUS LAEVIS;

ACTION POTENTIALS; ANIMALS; BASE SEQUENCE; CATALYTIC DOMAIN; DOSE-RESPONSE RELATIONSHIP, DRUG; GINSENOSIDES; HUMANS; ION CHANNEL GATING; KCNQ1 POTASSIUM CHANNEL; LYSINE; MUTATION; OOCYTES; PANAX; POTASSIUM CHANNELS, VOLTAGE-GATED; PROTEIN SUBUNITS; VALINE; XENOPUS LAEVIS;

EID: 77953289251     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.04.001     Document Type: Article

References (25)

1. Attele A.S., Wu J.A., Yuan C.S. Ginseng pharmacology: multiple constituents and multiple actions. Biochem. Pharmacol. 1999, 58:1685-1693.
2. Ks cardiac potassium current. Nature 1996, 384:78-80.
3. Bai C.X., Sunami A., Namiki T., Sawanobori T., Furukawa T. Electrophysiological effects of ginseng and ginsenoside Re in guinea pig ventricular myocytes. Eur. J. Pharmacol. 2003, 476:35-44.
4. 2+ current by ginsenoside Re, an ingredient of Panax ginseng, in guinea-pig cardiomyocytes. Br. J. Pharmacol. 2004, 142:567-575.
5. Chen C.X., Zhang H.Y. Protective effect of ginsenoside Re on isoproterenol-induced triggered ventricular arrhythmia in rabbits. Zhongguo Dang Dai Er Ke Za Zhi 2009, 11:384-388.
6. 2+ channel current inhibitions. Biol. Pharm. Bull. 2009, 32:1224-1230.
7. Furukawa T., Bai C.X., Kaihara A., Ozaki E., Kawano T., Nakaya Y., Awais M., Sato M., Umezawa Y., Kurokawa J. Ginsenoside Re, a main phytosterol of Panax ginseng, activates cardiac potassium channels via a nongenomic pathway of sex hormones. Mol. Pharmacol. 2006, 70:1916-1924.
8. Hille B. Ion channels of excitable membranes 2001, Sinauer Associates Inc., Sunderland, MA.
9. 3 action on ion channels. Mol. Cells. 2004, 18:383-389.
10. Kang C., Tian C., Sönnichsen F.D., Smith J.A., Meiler J., George A.L., Vanoye C.G., Kim H.J., Sanders C.R. Structure of KCNE1 and implications for how it modulates the KCNQ1 potassium channel. Biochemistry 2008, 47:7999-8006.
11. 3 inhibits human Kv1.4 channel currents by interacting with the Lys531 residue. Mol. Pharmacol. 2008, 73:619-626.
12. Lerche C., Bruhova I., Lerche H., Steinmeyer K., Wei A.D., Strutz-Seebohm N., Lang F., Busch A.E., Zhorov B.S., Seebohm G. Chromanol 293B binding in KCNQ1 (Kv7.1) channels involves electrostatic interactions with a potassium ion in the selectivity filter. Mol. Pharmacol. 2007, 71:1503-1511.
13. McCrossan Z.A., Abbott G.W. The MinK-related peptides. Neuropharmacology 2004, 47:787-821.
14. Morin T.J., Kobertz W.R. Counting membrane-embedded KCNE beta-subunits in functioning K+channel complexes. Proc. Natl Acad. Sci. USA 2008, 105:1478-1482.
15. Pusch M., Magrassi R., Wollnik B., Conti F. Activation and inactivation of homomeric KvLQT1 potassium channels. Biophys. J. 1998, 75:785-792.
16. Rees S., Curtis M.J. Which cardiac potassium channel subtype is the preferable target for suppression of ventricular arrhythmias?. Pharmacol. Ther. 1996, 69:199-217.
17. Robbins J. KCNQ potassium channels: physiology, pathophysiology, and pharmacology. Pharmacol. Ther. 2001, 90:1-19.
18. Sali A., Blundell T.L. Comparative protein modeling by satisfaction of spatial restraints. J. Mol. Biol. 1993, 234:779-815.
19. Salata J.J., Jurkiewicz N.K., Wang J., Evans B.E., Orme H.T., Sanguinetti M.C. A novel benzodiazepine that activates cardiac slow delayed rectifier K+currents. Mol. Pharmacol. 1998, 54:220-230.
20. Sanguinetti M.C., Curran M.E., Zou A., Shen J., Spector P.S., Atkinson D.L., Keating M.T. Coassembly of K(V)LQT1 and minK (IsK) proteins to form cardiac I(Ks) potassium channel. Nature 1996, 384:80-83.
21. Seebohm G., Chen J., Strutz N., Culberson C., Lerche C., Sanguinetti M.C. Molecular determinants of KCNQ1 channel block by a benzodiazepine. Mol. Pharmacol. 2003, 64:70-77.
22. Splawski I., Tristani-Firouzi M., Lehmann M.H., Sanguinetti M.C., Keating M.T. Mutations in the hmin K gene cause long QT syndrome and suppress IKs function. Nat. Genet. 1997, 17:338-340.
23. Tyler V.E. Herbal medicines. J. Pharm. Technol. 1995, 11:214-220.
24. Verdonk M.L., Cole J.C., Hartshorn M.J., Murray C.W., Taylor R.D. Improved protein-ligand docking using GOLD. Proteins 2003, 52:609-623.
25. Wang S., Morales M.J., Qu Y.J., Bett G.C., Strauss H.C., Rasmussion R.L. Kv1.4 channel block by quinidine: evidence for a drug-induced allosteric effect. J. Physiol. 2003, 546:387-401.