Ginsenoside Rg3 inhibits human Kv1.4 channel currents by interacting with the Lys531 residue

Molecular Pharmacology

Volumn 73, Issue 3, 2008, Pages 619-626

  Lee, Jun Ho ^a   Lee, Byung Hwan ^a   Choi, Sun Hye ^a   Yoon, In Soo ^a   Mi, Kyung Pyo ^a   Shin, Tae Joon ^a   Choi, Woo Sung ^a   Lim, Yoongho ^a   Rhim, Hyewhon ^b   Kwang, Hee Won ^c   Yong, Whan Lim ^c   Choe, Han ^c   Kim, Dong Hyun ^d   Yang, In Kim ^e   Nah, Seung Yeol ^a  

^a Konkuk University   (South Korea)

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

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

^d Kyung Hee University   (South Korea)

^e Korea University College of Medicine   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

GINSENOSIDE RG 3; TETRYLAMMONIUM; VOLTAGE GATED POTASSIUM CHANNEL; GINSENOSIDE; LYSINE; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL KV1.4;

ANIMAL EXPERIMENT; ARTICLE; DRUG BINDING SITE; DRUG EFFECT; DRUG INHIBITION; DRUG STRUCTURE; HYDROGEN BOND; MUTATION; NONHUMAN; NUCLEOTIDE SEQUENCE; PH; PRIORITY JOURNAL; WILD TYPE; AMINO ACID SUBSTITUTION; ANIMAL; BINDING SITE; CHEMICAL STRUCTURE; CHEMISTRY; COMPARATIVE STUDY; DOSE RESPONSE; DRUG ANTAGONISM; FEMALE; GENETICS; HUMAN; IC 50; METABOLISM; OOCYTE; PATCH CLAMP; PROTEIN BINDING; XENOPUS LAEVIS;

AMINO ACID SUBSTITUTION; ANIMALS; BINDING SITES; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GINSENOSIDES; HUMANS; HYDROGEN BONDING; INHIBITORY CONCENTRATION 50; KV1.4 POTASSIUM CHANNEL; LYSINE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; OOCYTES; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNEL BLOCKERS; PROTEIN BINDING; TETRAETHYLAMMONIUM; XENOPUS LAEVIS;

EID: 40849085416     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.107.040360     Document Type: Article

References (43)

1. Adams JP, Anderson AE, Varga AW, Dineley KT, Cook RG, Pfaffinger PJ, and Sweatt JD (2000) The A-type potassium channel Kv4.2 is a substrate for the mitogen-activated protein kinase ERK. J Neurochem 75:2277-2287.
2. Alonso G and Widmer H (1997) Clustering of Kv4.2 potassium channels in postsynaptic membrane of rat supraoptic neurons: an ultrastructural study. Neuroscience 77:617-621.
3. Attele AS, Wu JA, Yuan CS (1999) Ginseng pharmacology: multiple constituents and multiple actions. Biochem Pharmacol 58:1685-1693.
4. +channels: lipophilic interactions at the intracellular mouth of the pore. J Physiol 556:109-120.
5. Campbell DL, Rasmusson RL, Qu Y, Strauss HC (1993) The calcium-independent transient outward potassium current in isolated ferret right ventricular myocytes. I. Basic characterization and kinetic analysis. J Gen Physiol 101:571-601.
6. Choi S, Lee JH, Oh S, Rhim H, Lee SM, and Nah SY (2003) Effects of ginsenoside Rg2 on the 5-HT3A receptor-mediated ion current in Xenopus oocytes. Mol Cells 15:108-113.
7. + channels is regulated by extracellular charges. Biophys J 87:2407-2418.
8. Cooper EC, Milroy A, Jan YN, Jan LY, and Lowenstein DH (1998) Presynaptic localization of Kv1.4-containing A-type potassium channels near excitatory synapses in the hippocampus. J Neurosci 18:965-974.
9. + conductance in hippocampus. Nature 389:286-289.
10. Fedida D and Hesketh JC (2001) Gating of voltage-dependent potassium channels. Prog Biophys Mol Biol 75:165-199.
11. Gao BY, Li XJ, Liu L, and Zhang BH (1992) Effect of panaxatriol saponins isolated from Panax notoginseng (PTS) on myocardial ischemic arrhythmia in mice and rats. Yao Xue Xue Bao 27:641-644.
12. Gillis CN (1997) Panax ginseng pharmacology: a nitric oxide link? Biochem Pharmacol 54:1-8.
13. Gòmez-Hernandez JM, Lorra C, Pardo LA, Stuhmer W, Pongs O, Heinemann SH, and Elliott AA (1997) Molecular basis for different pore properties of potassium channels from the rat brain Kv1 gene family. Pflugers Arch 434:661-668.
14. Hille B (2001) Ion channels of excitable membranes. Sinauer Associates, Inc, Sunderland, MA.
15. Heginbotham L and Mackinnon R (1992) The aromatic binding site for tetraethylammonium ion on potassium channels. Neuron 8:483-491.
16. + channels in dendrites of hippocampal CA1 pyramidal neurons by activation of PKA and PKC. J Neurosci 18:3521-3528.
17. Jackson MB, Konnerth A, and Augustine GJ (1991) Action potential broadening and frequency-dependent facilitation of calcium signals in pituitary nerve terminals. Proc Natl Acad Sci U S A 88:380-384.
18. 3 action on ion channels. Mol Cells 18:383-389.
19. Judge SI, Monteiro MJ, Yeh JZ, and Bever CT (1999) Inactivation gating and 4-AP sensitivity in human brain Kv1.4 potassium channel. Brain Res 831:43-54.
20. + channel inhibition. Mol Cells 19:137-142.
21. + channels. Eur J Pharmacol 367:51-57.
22. + channels. Eur J Pharmacol 367:41-49.
23. Kim S, Ahn K, Oh TH, Nah SY, and Rhim H (2002) Inhibitory effect of ginsenosides on NMDA receptor-mediated signals in rat hippocampal neurons. Biochem Biophys Res Commun 296:247-254.
24. Lee BH, Jeong SM, Ha TS, Park CS, Lee JH, Kim JH, Kim DH, Han JS, Kim HC, Ko SR, et al. (2004) Ginsenosides regulate ligand-gated ion channels from the outside. Mol Cells 18:115-121.
25. + current inhibition. Mol Pharmacol 68:1114-1126.
26. 3A receptors. Neuropharmacology 52:1139-1150.
27. + channels by American ginseng. Eur J Pharmacol 413:47-54.
28. Lu G and Moriyama EN (2004) Vector NTI, a balanced all-in-one sequence analysis suite. Brief Bioinform 5:378-388.
29. MacDonald S, Elliott AA, Harrold JA, and Elliott JR (1998) Influence of outer pore residue K533 on the inhibition of Kv1.4 potassium channel s by n-alkyl sulphate anions. Pflugers Arch 436:623-626.
30. + channels. Biochemistry 43:13242-13247.
31. Nah SY (1997) Ginseng: recent advances and trends. Kor J Ginseng Sci 21:1-12.
32. 2+ channels through a pertussis toxin-sensitive G protein. Proc Natl Acad Sci U S A 92:8739-8743.
33. Patel SP and Campbell DL (2005) Transient outward potassium current, 'Ito', phenotypes in the mammalian left ventricle: underlying molecular, cellular and biophysical mechanisms. J Physiol 569:7-39.
34. + channel. Proc Natl Acad Sci U S A 89:2466-2470.
35. 2 on human neuronal nicotinic acetylcholine receptors. J Pharmacol Exp Ther 301:1052-1059.
36. Sali A and Blundell TL (1993) Comparative protein modelling by satisfaction of spatial restraints. J Mol Biol 234:779-815.
37. + channel block by catechol derivatives: defining nonselective and selective pharmacophores. J Pharmacol Exp Ther 319:758-764.
38. 3 inhibition of catecholamine secretion in bovine adrenal chromaffin cells. Biochem Pharmacol 62:943-951.
39. Verdonk ML, Cole JC, Hartshorn MJ, Murray CW, and Taylor RD (2003) Improved protein-ligand docking using GOLD. Proteins 52:609-623.
40. Wang S, Morales MJ, Qu YJ, Bett GCL, Strauss HC, and Rasmussion RL (2003) Kv1.4 channel block by quinidine: evidence for a drug-induced allosteric effect. J Physiol 546:387-401.
41. Watanabe I, Zhu J, Recio-Pinto E, and Thornhill WB (2004) Glycosylation affects the protein stability and cell surface expression of Kv1.4 but Not Kv1.1 potassium channels. A pore region determinant dictates the effect of glycosylation on trafficking. J Biol Chem 279:8879-8885.
42. Yang Y, He K, Wu T, Li Q, Zhang JS, and Fu ZG (1999) Effects of ginsenosides on myocardial reperfusion arrhythmia and lipid superoxidation in high cholesterol diet rats. Shi Yan Sheng Wu Xue Bao 32:349-352.
43. + channel inhibitor identified by high-throughput screening in yeast. Mol. Pharmacol 65:214-219.