Physiologie, pharmacologie et modélisation de canaux potassiques : zoom sur les canaux SK

canaux potassiques; canaux SK; physiologie; pharmacologie; modélisation moléculaire; Potassium channels; SK channels; physiology; pharmacology; molecular modelling

Abstract :

[fr] Différents types de canaux potassiques sont impliqués dans le contrôle de l'activité neuronale. Parmi ceux-ci les canaux SK constituent une cible thérapeutique intéressante car ils sous-tendent la posthyperpolarisation de durée moyenne qui limite l'excitabilité de divers types de neurones du système nerveux central. Une connaissance approfondie de la physiologie de ces canaux et la découverte de modulateurs non peptidiques sélectifs susceptibles de passer la barrière hémato-encéphaliques apparaissent donc indispensables dans la perspective de développer de futurs médicaments visant des maladies cérébrales telles que celles liées à un dysfonctionnement des sytèmes dopaminergiques et sérotoninergiques.
[en] Various types of ion channels are involved in the control of neuronal activity. Among them, SK channels represent an interesting therapeutic target. Indeed, they underlie medium duration afterhyperpolarizations in many types of neurons, thus inhibiting cell excitability. A thorough knowledge of the physiology of these channels and the discovery of non-peptidic selective modulators able to pass the blood-brain barrier are essential in view of developing future drugs for brain diseases such as those related to a dysfunction of dopaminergic and serotonergic systems.

Research Center/Unit :

Giga-Neurosciences / CIRM

Disciplines :

Computer science
Pharmacy, pharmacology & toxicology

Author, co-author :

Dilly, Sébastien ; Université de Liège - ULiège > Département de Pharmacie / Giga-Neurosciences > Chimie pharmaceutique / Pharmacologie

Poncin, Sylvie; Université de Liège - ULiège > Giga-Neurosciences > Pharmacologie

Lamy, Cédric; Université de Liège - ULiège > Giga-Neurosciences > Pharmacologie

Liégeois, Jean-François ; Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique

Seutin, Vincent ; Université de Liège - ULiège > Giga-Neurosciences > Pharmacologie

Language :

French

Title :

Physiologie, pharmacologie et modélisation de canaux potassiques : zoom sur les canaux SK

Alternative titles :

[en] Physiology, pharmacology and modelling of potassium channels: focus on SK channels

Publication date :

April 2012

Journal title :

MS. Medecine Sciences

ISSN :

0767-0974

eISSN :

1958-5381

Publisher :

EDK, Paris, France

Volume :

Pages :

395-402

Peer reviewed :

Peer Reviewed verified by ORBi

Funders :

ULiège - Université de Liège
F.R.S.-FNRS - Fonds de la Recherche Scientifique

Available on ORBi :

since 16 January 2012

Statistics

Number of views

234 (50 by ULiège)

Number of downloads

15 (9 by ULiège)

More statistics

Scopus citations^®

Scopus citations^®
without self-citations

OpenCitations

OpenAlex citations

Bibliography

Liégeois JF, Mercier F, Graulich A, et al. Modulation of small conductance calcium-activated potassium (SK) channels: a new challenge in medicinal chemistry. Curr Med Chem 2003;10:625-47. (Pubitemid 36348085)
Shieh CC, Coghlan M, Sullivan J P, Gopalakrishnan M. Potassium channels: molecular defects, diseases, and therapeutic opportunities. Pharmacol Rev 2000;52:557-94.
Burg ED, Remillard CV, Yuan JX. K+ channels in apoptosis. J Membr Biol 2006;209:3-20. (Pubitemid 43725458)
Potier M, Joulin V, Roger S, et al. Identification of SK3 channel as a new mediator of breast cancer cell migration. Mol Cancer Ther 2006;5:2946-53. (Pubitemid 44849022)
Schwab A, Nechyporuk-Zloy V, Fabian A, Stock C. Cells move when ions and water flow. Pflugers Arch 2007;453:421-32. (Pubitemid 46011163)
Gutman GA, Chandy KG, Adelman JP, et al. International union of pharmacology. XLI. Compendium of voltage-gated ion channels: potassium channels. Pharmacol Rev 2003;55:583-6. (Pubitemid 37500518)
Moulton G, Attwood TK, Parry-Smith DJ, Packer JC. Phylogenomic analysis and evolution of the potassium channel gene family. Receptor Channel 2003;9:363-77. (Pubitemid 38008223)
Choe S. Potassium channel structures. Nat Rev Neurosci 2002;3:115-21. (Pubitemid 135706580)
Bayliss DA, Barrett PQ. Emerging roles for two-pore-domain potassium channels and their potential therapeutic impact. Trends Pharmacol Sci 2008;29:566-75.
Lotshaw D P. Biophysical, pharmacological, and functional characteristics of cloned and native mammalian two-pore domain K+ channels. Cell Biochem Biophys 2007;47:209-56. (Pubitemid 47338363)
Doyle DA, Morais Cabral J, Pfuetzner RA, et al. The structure of the potassium channel: molecular basis of K+ conduction and selectivity. Science 1998;280:69-77. (Pubitemid 28169082)
Heginbotham L, Lu Z, Abramson T, MacKinnon R. Mutations in the K + channel signature sequence. Biophys J 1994;66:1061-7. (Pubitemid 24106352)
Roux B, MacKinnon R. The cavity and pore helices in the KcsA K + channel: electrostatic stabilization of monovalent cations. Science 1999;285:100-2. (Pubitemid 29307574)
Zhou Y, Morais-Cabral JH, Kaufman A, MacKinnon R. Chemistry of ion coordination and hydration revealed by a K+ channel-Fab complex at 2.0 A resolution. Nature 2001;414:43-8. (Pubitemid 33041616)
Morais-Cabral JH, Zhou Y, MacKinnon R. Energetic optimization of ion conduction rate by the K+ selectivity filter. Nature 2001;414:37-42.
Parent L, Sauvé R, Bernèche S, Roux B. À bas les barrières⋯ d'énergie dans les canaux potassiques ! Med Sci (Paris) 2002;18:605-9. (Pubitemid 34614773)
Dilly S, Lamy C, Marrion NV, et al. Ion-channel modulators: more diversity than previously thought. Chembiochem 2011;12:1808-12.
Swartz KJ, MacKinnon R. Hanatoxin modifies the gating of a voltagedependent K+ channel through multiple binding sites. Neuron 1997;18:665-73. (Pubitemid 27194645)
Kavanaugh M P, Varnum MD, Osborne PB, et al. Interaction between tetraethylammonium and amino acid residues in the pore of cloned voltage-dependent potassium channels. J Biol Chem 1991;266:7583-7. (Pubitemid 21906405)
Miller C. Competition for block of a Ca2+-activated K + channel by charybdotoxin and tetraethylammonium. Neuron 1988;1:1003-6.
Lamy C, Goodchild SJ, Weatherall KL, et al. Allosteric block of KCa2 channels by apamin. J Biol Chem 2010;285:27067-77.
Stocker M, Pedarzani P. Differential distribution of three Ca 2+-activated K+ channel subunits, SK1, SK2, and SK3, in the adult rat central nervous system. Mol Cell Neurosci 2000;15:476-93. (Pubitemid 30395372)
Rouchet N, Waroux O, Lamy C, et al. SK channel blockade promotes burst firing in dorsal raphe serotonergic neurons. Eur J Neurosci 2008;28:1108-15.
Waroux O, Massotte L, Alleva L, et al. SK channels control the firing pattern of midbrain dopaminergic neurons in vivo. Eur J Neurosci 2005;22:3111-21. (Pubitemid 43001994)
Diness JG, Sorensen US, Nissen JD, et al. Inhibition of small-conductance Ca2+-activated K+ channels terminates and protects against atrial fibrillation. Circ Arrhythm Electrophysiol 2010;3:380-90.
Grube S, Gerchen MF, Adamcio B, et al. A CAG repeat polymorphism of KCNN3 predicts SK3 channel function and cognitive performance in schizophrenia. EMBO Mol Med 2011;3:309-19.
Shakkottai VG, Regaya I, Wulff H, et al. Design and characterization of a highly selective peptide inhibitor of the small conductance calcium-activated K+ channel, SkCa2. J Biol Chem 2001;276:43145-51.
Hugues M, Romey G, Duval D, et al. Apamin as a selective blocker of the calcium-dependent potassium channel in neuroblastoma cells: voltage-clamp and biochemical characterization of the toxin receptor. Proc Natl Acad Sci USA 1982;79:1308-12. (Pubitemid 12105598)
Grunnet M, Jensen BS, Olesen S P, Klaerke DA. Apamin interacts with all subtypes of cloned smallconductance Ca2+-activated K+ channels. Pflugers Arch 2001;441:544-50. (Pubitemid 32128151)
Pedarzani P, Stocker M. Molecular and cellular basis of small-and intermediate-conductance, calcium-activated potassium channel function in the brain. Cell Mol Life Sci 2008;65:3196-217.
Weatherall KL, Seutin V, Liegeois JF, Marrion NV. Crucial role of a shared extracellular loop in apamin sensitivity and maintenance of pore shape of small-conductance calcium-activated potassium (SK) channels. Proc Natl Acad Sci USA 2011;108:18494-9.
Campos Rosa J, Galanakis D, Piergentili A, et al. Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca2+-activated K + channel. J Med Chem 2000;43:420-31. (Pubitemid 30102082)
Chen JQ, Galanakis D, Ganellin CR, et al. bis-Quinolinium cyclophanes: 8, 14-diaza-1, 7 (1, 4)-diquinolinacyclotetradecaphane (UCL 1848), a highly potent and selective, nonpeptidic blocker of the apamin-sensitive Ca 2+-activated K+ channel. J Med Chem 2000;43:3478-81.
Olesen SP, Munch E, Moldt P, Drejer J. Selective activation of Ca 2+-dependent K+ channels by novel benzimidazolone. Eur J Pharmacol 1994;251:53-9.
Girault A, Haelters J P, Potier M, et al. New alkyl-lipid blockers of SK3 channels reduce cancer-cell migration and occurrence of metastasis. Curr Cancer Drug Targets 2011;11:1111-25.
Strobaek D, Hougaard C, Johansen TH, et al. Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1, 2, 3, 4-tetrahydro-1- naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons. Mol Pharmacol 2006;70:1771-82.
Pedarzani P, Mosbacher J, Rivard A, et al. Control of electrical activity in central neurons by modulating the gating of small conductance Ca 2+-activated K+ channels. J Biol Chem 2001;276:9762-9.
Jenkins D P, Strobaek D, Hougaard C, et al. Negative gating modulation by (R)-N-(benzimidazol-2-yl)-1, 2, 3, 4-tetrahydro-1-naphthylamine (NS8593) depends on residues in the inner pore vestibule: pharmacological evidence of deep-pore gating of K (Ca) 2 channels. Mol Pharmacol 2011;79:899-909.
Potier M, Chantome A, Joulin V, et al. The SK3/K (Ca) 2.3 potassium channel is a new cellular target for edelfosine. Br J Pharmacol 2011;162:464-79.
Seutin V, Scuvée-Moreau J, Dresse A. Evidence for a non-GABAergic action of quaternary salts of bicuculline on dopaminergic neurones. Neuropharmacology 1997;36:1653-7. (Pubitemid 28085925)
Scuvée-Moreau J, Boland A, Graulich A, et al. Electrophysiological characterization of the SK channel blockers methyl-laudanosine and methyl-noscapine in cell lines and rat brain slices. Br J Pharmacol 2004;143:753-64. (Pubitemid 39611611)
Scuvée-Moreau J, Liégeois JF, Massotte L, Seutin V. Methyl-laudanosine: a new pharmacological tool to investigate the function of small-conductance Ca2+-activated K+ channels. J Pharmacol Exp Ther 2002;302:1176-83. (Pubitemid 34920241)
Graulich A, Dilly S, Farce A, et al. Synthesis and radioligand binding studies of bis-isoquinolinium derivatives as small conductance Ca 2+-activated K+ channel blockers. J Med Chem 2007;50:5070-5. (Pubitemid 47585704)
Dilly S, Graulich A, Farce A, et al. Identification of a pharmacophore of SKCa channel blockers. J Enzyme Inhib Med Chem 2005;20:517-23. (Pubitemid 43994749)
Martina M, Turcotte ME, Halman S, Bergeron R. The sigma-1 receptor modulates NMDA receptor synaptic transmission and plasticity via SK channels in rat hippocampus. J Physiol 2007;578:143-57. (Pubitemid 44971116)
Lamy C, Scuvée-Moreau J, Dilly S, et al. The sigma agonist 1, 3-di-o-tolylguanidine directly blocks SK channels in dopaminergic neurons and in cell lines. Eur J Pharmacol 2010;641:23-8.
Graulich A, Lamy C, Alleva L, et al. Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca2+-activated K+ channel blockers. Bioorg Med Chem Lett 2008;18:3440-5. (Pubitemid 351718304)
Neny M, Lemmer Y, Graulich A, et al. The SK channel blocker AG525E1 increases locomotor activity and in vivo dopamine release in the rat nucleus accumbens. In: Phillips PEM SS, Ahn S, Phillips AG, eds. Proceedings of the 12th International conference on in vivo methods monitoring molecules in neuroscience. Vancouver: University of Bristish Columbia, 2008:267-70.
Dilly S, Lamy C, Liégeois JF, Seutin V. Combined experimental and computational approaches to study the action of blockers of small conductance calcium-activated potassium (SK) channels. Acta Physiol Scand 2010; suppl 678:O-10.
Nolting A, Ferraro T, D'Hoedt D, Stocker M. An amino acid outside the pore region influences apamin sensitivity in small conductance Ca 2+-activated K+ channels. J Biol Chem 2007;282:3478-86. (Pubitemid 47084459)
Goodchild SJ, Lamy C, Seutin V, Marrion NV. Inhibition of K (Ca) 2.2 and K (Ca) 2.3 channel currents by protonation of outer pore histidine residues. J Gen Physiol 2009;134:295-308.
Seutin V. Régulation de l'activité des neurones monoaminergiques par des canaux ioniques: une opportunité pour de nouvelles approches thérapeutiques? Bull Mem Acad R Med Belg 2008;163:213-23.