The KCNQ2/3 selective channel opener ICA-27243 binds to a novel voltage-sensor domain site

Neuroscience Letters

Volumn 465, Issue 2, 2009, Pages 138-142

  Padilla, Karen ^a   Wickenden, Alan D ^b   Gerlach, Aaron C ^a   McCormack, Ken ^a  

^a Icagen Inc   (United States)

^b JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Binding site; ICA 27243; K+ channel opener; KCNQ; Kv7; Retigabine; Sub type selective; Voltage sensor domain

Indexed keywords

ICA 27243; N (6 CHLORO PYRIDIN 3 YL) 3,4 DIFLUOROBENZAMIDE; POTASSIUM CHANNEL KCNQ2; POTASSIUM CHANNEL KCNQ3; POTASSIUM CHANNEL STIMULATING AGENT; RETIGABINE; TRYPTOPHAN; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; CHO CELL; CONTROLLED STUDY; CRYSTALLOGRAPHY; DRUG ACTIVITY; DRUG BINDING SITE; DRUG SELECTIVITY; FEMALE; GENE MUTATION; GENETIC VARIABILITY; MOLECULAR INTERACTION; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN INTERACTION; SEQUENCE ALIGNMENT;

AMINO ACID SEQUENCE; ANIMALS; ANTICONVULSANTS; BENZAMIDES; BINDING SITES; CARBAMATES; CHO CELLS; CRICETINAE; CRICETULUS; HUMANS; KCNQ POTASSIUM CHANNELS; KCNQ2 POTASSIUM CHANNEL; KCNQ3 POTASSIUM CHANNEL; MEMBRANE POTENTIALS; MEMBRANE TRANSPORT MODULATORS; MOLECULAR SEQUENCE DATA; MUTATION; PHENYLENEDIAMINES; PYRIDINES; SEQUENCE ALIGNMENT; TRYPTOPHAN;

EID: 70349329230     PISSN: 03043940     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neulet.2009.08.071     Document Type: Article

References (31)

1. Beirvert C., Schroeder B.C., Kubisch C., Berkovic S.F., Propping P., Jentsch T.J., and Steinlein O.K. A potassium channel mutation in neonatal human epilepsy. Science 279 (1998) 403-406
2. Bentzen B.H., Schmitt N., Calloe K., Dalby Brown W., Grunnet M., and Olesen S.P. The acrylamide (S)-1 differentially affects Kv7 (KCNQ) potassium channels. Neuropharmacology 51 (2006) 1068-1077
3. Gribkoff V.K. The therapeutic potential of neuronal Kv7 (KCNQ) channel modulators: an update. Expert Opin. Ther. Targets 12 (2008) 565-581
4. Kapetanovic I.M., Yonekawa W.D., and Kupferberg H.J. The effects of D-23129, a new experimental anticonvulsant drug, on neurotransmitter amino acids in the rat hippocampus in vitro. Epilepsy Res. 22 (1995) 167-173
5. Kubisch C., Schroeder B.C., Friedrich T., Jutjohann B., El-Amraoui A., Marlin S., Petit C., and Jentsch T.J. KCNQ4, a novel potassium channel expressed in sensory outer hair cells is mutated in dominant deafness. Cell 96 (1999) 437-446
6. Lange W., Geissendoerfer J., Schenzer A., Groetzinger J., Seebohm G., Friedich T., and Schwake M. Refinement of the binding site and mode of action of the anticonvulsant retigabine on KCNQ K+ channels. Mol. Pharmacol. 75 (2009) 272-280
7. Lawson K., and McKay N.G. Modulation of potassium channels as a therapeutic approach. Curr. Pharm. Des. 12 (2006) 459-470
8. Lerche C., Scherer C.R., Seebohm G., Derst C., Wei A.G., Busch A.E., and Steinmeyer K. Molecular cloning and functional expression of KCNQ5, a potassium channel subunit that may contribute to neuronal M-current diversity. J. Biol. Chem. 275 (2000) 22395-22400
9. Long S.B., Tao X., Campbell E.R., and MacKinnon R. Atomic structure of a voltage-dependent K+ channel in a lipid membrane-like environment. Nature 450 (2007) 376-382
10. Lu Z., Klem A.M., and Ramu Y. Coupling between voltage sensors and activation gate in voltage-gated K+ channels. J. Gen. Physiol. 120 (2002) 663-676
11. Main M.J., Cryan J.E., Dupere J.R., Cox B., Clare J.J., and Burbidge S.A. Modulation of KCNQ2/3 potassium channels by the novel anticonvulsant retigabine. Mol. Pharmacol. 58 (2000) 253-262
12. Neyroud N., Tesson F., Denjoy I., Leibovici M., Conger C., Barhanin J., Faure S., Gary F., Coumel P., Petit C., Schwartz K., and Guicheney P. A novel mutation in the potassium channel gene KVLQT1 causes the Jervell and Lange-Nielsen cardioauditory syndrome. Nat. Genet. 15 (1997) 186-189
13. Patten C.H., Caprini M., Planell-Cases R., and Montal M. Structural and functional modularity of voltage-gated potassium channels. FEBS Lett. 464 (1999) 375-381
14. Porter R.J., Partiot A., Sachdeo R., Nohria V., and Alves W.M. Randomized, multicenter, dose-ranging trial of retigabine for partial-onset seizures. Neurology 68 (2007) 1197-1204
15. Roeloffs R., Wickenden A.D., Crean C., Werness S., McNaughton-Smith G., Stables J., McNamara J.O., Ghodadra N., and Rigdon G.C. In vivo profile of ICA-27243 [N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide] a potent and selective KCNQ2/Q3 (Kv7. 2/Kv7. 3) activator in rodent anticonvulsant models. J. Pharmacol. Exp. Ther. 326 (2008) 818-828
16. Rostock A., Tober C., Rundfeldt C., Bartsch R., Engel J., Polymeropoulos E.E., Kutscher B., Löscher W., Hönack D., White H.S., and Wolf H.H. D-23129: a new anticonvulsant with a broad spectrum activity in animal models of epileptic seizures. Epilepsy Res. 23 (1996) 211-223
17. Rundfeldt C., and Netzer R. The novel anticonvulsant retigabine activates M-currents in Chinese hamster ovary-cells tranfected with human KCNQ2/3 subunits. Neurosci Lett. 282 (2000) 73-76
18. Rundfeldt C., and Netzer R. Investigations into the mechanism of action of the new anticonvulsant retigabine. Arzneimittelforschung 50 (2000) 1063-1070
19. Schenzer A., Friedrich T., Pusch M., Saftig P., Jentsch T.J., Grötzinger J., and Schwake M. Molecular determinants of KCNQ (Kv7) K+ channel sensitivity to the anticonvulsant retigabine. J. Neurosci. 25 (2005) 5051-5060
20. Schrøder R.L., Jespersen T., Christophersen P., Strøbaek D., Jensen B.S., and Olesen S.P. KCNQ4 channel activation by BMS-204352 and retigabine. Neuropharmacology 40 (2001) 888-898
21. Schwake M., Jentsch T.J., and Friedrich T. A carboxy-terminal domain determines the subunit specificity of KCNQ K+ channel assembly. EMBO Rep. 4 (2003) 76-81
22. Seebohm G., Pusch M., Chen J., and Sanguinetti M.C. Pharmacological activation of normal and arrhythmia-associated mutant KCNQ1 potassium channels. Circ. Res. 93 (2003) 941-947
23. Singh N.A., Charlier C., Stauffer D., DuPont B.R., Leach R.J., Melis R., Ronen G.M., Bjerre I., Quattlebaum T., Murphy J.V., McHarg M.L., Gagnon D., Rosales T.O., Peiffer A., Anderson V.E., and Leppert M. A novel potassium channel gene, KCNQ2 is mutated in an inherited form of epilepsy of newborns. Nat. Genet. 18 (1998) 25-29
24. Tatulian L., Delmas P., Abogadie F.C., and Brown D.A. Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine. J. Neurosci. 21 (2001) 5535-5545
25. Wang Q., Curran M.E., Splawski I., Burn T.C., Millholland J.M., VanRaay T.J., Shen J., Timothy K.W., Vincent G.M., de Jager T., Schwartz P.J., Toubin J.A., Moss A.J., Atkinson D.L., Landes G.M., Connors T.D., and Keating M.T. Positional cloning of a novel potassium channel gene: KVLQT1 mutations cause cardiac arrythmias. Nat. Genet. 12 (1996) 17-23
26. Wang H.S., Pan Z., Shi W., Brown B.S., Wymore R., Cohen I.S., Dixon J.E., and McKinnon D. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 282 (1998) 1890-1893
27. Wickenden A.D., Krajewski J.L., London B., Wagoner P.K., Wilson W.A., Clark S., Roeloffs R., McNaughton-Smith G., and Rigdon G.C. N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel selective KCNQ2/Q3 potassium channel activator. Mol. Pharmacol. 73 (2008) 977-986
28. Wickenden A.D., Zou A., Wagoner P.K., and Jegla T. Characterization of KCNQ5/Q3 potassium channels expressed in mammalian cells. Br. J. Pharmacol. 132 (2001) 381-384
29. Wickenden A.D., Yu W., Zou A., Jegla T., and Wagoner P.K. Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol. Pharmacol. 58 (2000) 591-600
30. Wuttke T.V., Seebohm G., Bail S., Maljevic S., and Lerche H. The new anticonvulsant retigabine favors voltage-dependent opening of the Kv7.2 (KCNQ2) channel by binding to its activation gate. Mol. Pharmacol. 67 (2005) 1009-1017
31. Xiong Q., Gao Z., Wang W., and Li M. Activation of Kv7 (KCNQ) voltage-gated potassium channels by synthetic compounds. Trends Pharm. Sci. 29 (2007) 99-107