Probing kinetic drug binding mechanism in voltage-gated sodium ion channel: open state versus inactive state blockers

References

• Hodgkin AL. Evidence for electrical transmission in nerve Part I. J Physiol 1937; 90:183-210; PMID:16994885; http://dx.doi.org/10.1113/jphysiol.1937.sp003507
   PubMedGoogle Scholar
• Hodgkin AL. Evidence for electrical transmission in nerve Part II. J. Physiol 1937; 90:211-32; PMID:16994886; http://dx.doi.org/10.1113/jphysiol.1937.sp003508
   PubMedGoogle Scholar
• Catterall WA. Sodium channels, inherited epilepsy, and antiepileptic drugs. Annu Rev Pharmacol Toxicol 2014; 54:317-38 PMID:24392695; http://dx.doi.org/10.1146/annurev-pharmtox-011112-140232
   PubMed Web of Science ®Google Scholar
• Scholz A. Mechanisms of (local) anaesthetics on voltage-gated sodium and other ion channels. Br J Anaesth 2002; 89:52-61; PMID:12173241; http://dx.doi.org/10.1093/bja/aef163
   PubMed Web of Science ®Google Scholar
• Kiss T. Persistent Na-channels: origin and function. A review. Acta Biol Hung 2008; 59:1-12; PMID:18652365; http://dx.doi.org/10.1556/ABiol.59.2008.Suppl.1
   PubMed Web of Science ®Google Scholar
• Mustafa BA. Djamgoz and rustem onkal. Persistent current blockers of voltage-gated sodium channels: a clinical opportunity for controlling metastatic disease. Recent Pat Anticancer Drug Discov 2013; 8:66-84; PMID:23116083
   PubMed Web of Science ®Google Scholar
• Lin WH, Wright DE, Muraro NI, Baines RA, Alternative splicing in the voltage-gated sodium channel DmNav regulates activation, inactivation, and persistent current. J Neurophysiol 2009; 102:1994-2006
   PubMed Web of Science ®Google Scholar
• Wayne E. Crill. Persistent sodium current in mammalian central neurons. Annu Rev Physiol 1996; 58:349-62
   PubMed Web of Science ®Google Scholar
• Catterall WA, Goldin AL, Waxman SG. International Union of Pharmacology. XLVII. Nomenclature and Structure-Function Relationships of Voltage-Gated Sodium Channels. Pharmacol Rev 2005; 57:397-409; PMID:16382098; http://dx.doi.org/10.1124/pr.57.4.4
   PubMed Web of Science ®Google Scholar
• Catterall WA. From Ionic Currents to Molecular Mechanisms: The Structure and Function of Voltage-Gated Sodium Channels. Neuron 2000; 26:13-25; PMID:10798388; http://dx.doi.org/10.1016/S0896-6273(00)81133-2
   PubMed Web of Science ®Google Scholar
• Ashcroft FM. From molecule to malady. Nature 2006; 440:440-7; PMID:16554803; http://dx.doi.org/10.1038/nature04707
   PubMed Web of Science ®Google Scholar
• Dichgans M, Freilinger T, Eckstein G, Babini E, Lorenz-Depiereux B, Biskup S, Ferrari MD, Herzog J, van den Maagdenberg AM, Pusch M, et.al, Mutation in the neuronal voltage-gated sodium channel SCN1A in familial hemiplegic migraine. Lancet 2005; 366:371-7; PMID:16054936; http://dx.doi.org/10.1016/S0140-6736(05)66786-4
   PubMed Web of Science ®Google Scholar
• George AL Jr. Inherited disorders of voltage-gated sodium channels. J Clin Invest 2005; 115:1990-9; PMID:16075039; http://dx.doi.org/10.1172/JCI25505
   PubMed Web of Science ®Google Scholar
• Wickenden A1, Priest B, Erdemli G. Ion channel drug discovery: challenges and future directions. Future Med Chem 2012; 4:661-79; PMID:22458684; http://dx.doi.org/10.4155/fmc.12.4
   PubMed Web of Science ®Google Scholar
• Clare JJ. Targeting ion channels for drug discovery. Discov Med 2010; 9:253-60; PMID:20350493
   PubMed Web of Science ®Google Scholar
• Perrior T. Overcoming Bottlenecks in drug discovery; Drug Discovery World 2010; Fall: 29-33; fall-10-bottlenecks-p29.pdf
   Google Scholar
• Echt DS, Liebson PR, Mitchell LB, Peters RW, Obias-Manno D, Barker AH, Arensberg D, Baker A, Friedman L, Greene HL. Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmia Suppression Trial. N Engl J Med 1991; 324:781-8; PMID:1900101; http://dx.doi.org/10.1056/NEJM199103213241201
   PubMed Web of Science ®Google Scholar
• Task Force of the Working Group on Arrhythmias of the European Society of Cardiology. The Sicilian gambit. A new approach to the classification of antiarrhythmic drugs based on their actions on arrhythmogenic mechanisms. Circulation 1991; 84:1831-51; PMID:1717173; http://dx.doi.org/10.1161/01.CIR.84.4.1831
   PubMed Web of Science ®Google Scholar
• Carmeliet E. Voltage-dependent block by tetrodotoxin of the sodium channel in rabbit cardiac Purkinje fibers. Biophys J 1987; 51:109-14; PMID:2432950; http://dx.doi.org/10.1016/S0006-3495(87)83315-5
   PubMed Web of Science ®Google Scholar
• Sarma SP, Kumar GS, Sudarslal S, Iengar P, Ramasamy P, Sikdar SK, Krishnan KS, Balaram P. Solution structure of delta-Am2766: a highly hydrophobic delta−conotoxin from conus amadis that inhibits inactivation of neuronal voltage-gated sodium channels. Chem Biodivers 2005; 2:535-56; PMID:17192003; http://dx.doi.org/10.1002/cbdv.200590035
   PubMed Web of Science ®Google Scholar
• Armstrong CM, Bezanilla F, Rojas E. Destruction of sodium conductance inactivation in squid axons perfused with pronase. J Gen Physiol 1973; 62:375-91; PMID:4755846; http://dx.doi.org/10.1085/jgp.62.4.375
   PubMed Web of Science ®Google Scholar
• Clancy CE, Zhu ZI, Rudy Y. Pharmacogenetics and anti arrhythmic drug therapy: a theoretical investigation. Am J Physiol Heart Circ Physiol 2007; 292:H66-75; PMID:16997895
   PubMed Web of Science ®Google Scholar
• Zamponi GW, Doyle DD, French RJ. State-dependent block underlies the tissue specificity of lidocaine action on batrachotoxin-activated cardiac sodium channels. Biophysical J 1993; 65:91-100; http://dx.doi.org/10.1016/S0006-3495(93)81043-9
   PubMed Web of Science ®Google Scholar
• Zamponi GW, French RJ. Dissecting lidocaine action: die diethylamide and phenol mimic separate modes of lidocaine block of sodium channels from heart and skeletal muscle. Biophysical J 1993; 65:2335-47; http://dx.doi.org/10.1016/S0006-3495(93)81292-X
   PubMed Web of Science ®Google Scholar
• Vandenberg CA, Bezanilla F. A sodium channel gating model based on single channel, macroscopic ionic, and gating currents in the squid giant axon. Biophysics J 1991; 60:1511-33; http://dx.doi.org/10.1016/S0006-3495(91)82186-5
   PubMed Web of Science ®Google Scholar
• Millonas MM, Hanck DA. Nonequilibrium response spectroscopy of voltage-sensitive ion channel gating. Biophys J 1998; 74:210-29; PMID:9449324; http://dx.doi.org/10.1016/S0006-3495(98)77781-1
   PubMed Web of Science ®Google Scholar
• Hosein-Sooklal A, Kargol A. Wavelet analysis of nonequilibrium ionic currents in human heart sodium channel (hH1a). J Membr Biol 2002; 188:199-212; PMID:12181611; http://dx.doi.org/10.1007/s00232-001-0188-9
   PubMed Web of Science ®Google Scholar
• Kargol A, Hosein-Sooklal A, Constantin L, Przestalski M. Application of oscillating potentials to Shaker potassium channel. Gen Physiol Biophys 2004; 23:53-75; PMID:15270129
   PubMed Web of Science ®Google Scholar
• Llinas R, Yarom Y. Oscillatory properties of guinea-pig inferior olivary Neurones and their pharmacological modulation: An in vitro study. J Physiol 1986; 376:163-82; PMID:3795074; http://dx.doi.org/10.1113/jphysiol.1986.sp016147
   PubMed Web of Science ®Google Scholar
• Llinas RR, Grace AA, Yarom Y. In vitro neurons in mammalian cortical layer 4 exhibit intrinsic oscillatory activity in the 10- to 50-Hz frequency range. Proc Nati Acad Sci USA 1991; 88:897-901; http://dx.doi.org/10.1073/pnas.88.3.897
   PubMed Web of Science ®Google Scholar
• Fozzard HA, Lipkind GM. The tetrodotoxin binding site is within the outer vestibule of the sodium channel. Marine Drugs 2010; 8:219-34; PMID:20390102; http://dx.doi.org/10.3390/md8020219
   PubMed Web of Science ®Google Scholar
• Starmer CF, Lastra AA, Nesterenko VV, Grant AO. Proarrhythmic response to sodium channel blockade. Theoretical model and numerical experiments. Circulation 1991; 84:1364-77; PMID:1653123; http://dx.doi.org/10.1161/01.CIR.84.3.1364
   PubMed Web of Science ®Google Scholar
• Stramer CF. How antiarrhytmic drugs increase the rate of sudden cardiac death. Int J Bifurcation Chaos 2002; 12:1953; http://dx.doi.org/10.1142/S0218127402005625
   Web of Science ®Google Scholar
• Hille B. Local anesthetics: Hydrophilic and hydrophobic pathways for the drug receptor reaction. J Gen Physiol 1977; 69:497-515; PMID:300786; http://dx.doi.org/10.1085/jgp.69.4.497
   PubMed Web of Science ®Google Scholar
• Wang GK, Strichartz GR. State-Dependent Inhibition of Sodium Channels by Local Anesthetics: A 40-Year Evolution. Biochem (Mosc) Suppl Ser A Membr Cell Biol 2012; 6:120-7; PMID:23710324; http://dx.doi.org/10.1134/S1990747812010151
   PubMedGoogle Scholar
• Khodorov BI, Shishkova L, Peganov E, Revenko S. Inhibition of sodium currents in frog Ranvier node treated with local anesthetics. Role of slow sodium inactivation. Biochim Biophys Acta 1976; 433:409; http://dx.doi.org/10.1016/0005-2736(76)90105-X
   Web of Science ®Google Scholar
• Courtney KR. Mechanism of frequency-dependent inhibition of sodium currents in frog myelinated nerve by the lidocaine derivative GEA. J Pharm Exp Therop 1975; 195:225-36
   PubMed Web of Science ®Google Scholar
• Lee PJ, Sunami A, Fozzard HA. Cardiac specific external paths for lidocaine, defined by isoform-specific residues, accelerate recovery from use-dependent block. Circ Res 2001; 89:1014-21; PMID:11717158; http://dx.doi.org/10.1161/hh2301.100002
   PubMed Web of Science ®Google Scholar
• Crumb WJ, Jr, Clarkson CW. Characterization of cocaine-induced block of cardiac sodium channels. Biophys J 1990; 57:589-99; PMID:2155033; http://dx.doi.org/10.1016/S0006-3495(90)82574-1
   PubMed Web of Science ®Google Scholar
• Lee CH, Ruben PC. Interaction between voltage-gated sodium channels and the neurotoxin, tetrodotoxin. Channels 2008; 2:407-12; PMID:19098433; http://dx.doi.org/10.4161/chan.2.6.7429
   PubMed Web of Science ®Google Scholar
• Lipkind GM, Fozzard HA. Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels. Mol Pharmacol 2005; 68:1611-22; PMID:16174788
   PubMed Web of Science ®Google Scholar
• Gilliam FR 3rd, Starmer CF, Grant AO. Blockade of rabbit atrial sodium channels by lidocaine characterization of continuous and frequency-dependent blocking. Circ Res 1989; 65:723-39; PMID:2548763; http://dx.doi.org/10.1161/01.RES.65.3.723
   PubMed Web of Science ®Google Scholar
• Campbell TJ, Wyse KR, Pallandi R. Di_erential e_ects on action potential of class IA, B and C antiarrhythmic drugs: modulation by stimulation rate and extracellular K+ concentration. Clinc Exp Pharmacol Physiol 1991; 18:533-41; http://dx.doi.org/10.1111/j.1440-1681.1991.tb01488.x
   PubMed Web of Science ®Google Scholar
• Lipkind GM, Fozzard HA. Molecular model of anticonvulsant drug binding to the voltage-gated sodium channel inner pore. Mol Pharmacol 2010; 78:631-8; PMID:20643904; http://dx.doi.org/10.1124/mol.110.064683
   PubMed Web of Science ®Google Scholar
• An RH, Bangalore R, Rosero SZ, Kass RS. Lidocaine block of LQT-3 mutant human Na channels. Circ Res 1996; 79:103-8; PMID:8925557; http://dx.doi.org/10.1161/01.RES.79.1.103
   PubMed Web of Science ®Google Scholar
• Bennett PB, Yazawa K, Makita N, George AL Jr. Molecular mechanism of an inherited cardiac arrhythmia. Nature 1995; 376:683-5; PMID:7651517; http://dx.doi.org/10.1038/376683a0
   PubMed Web of Science ®Google Scholar
• Dumaine R, Wang Q, Keating MT, Hartmann HA, Schwartz PJ, Brown AM, Kirsch GE. Multiple mecha nisms of Na+ channel linked long-QT syndrome. Circ Res 1996; 78:916-24; PMID:8620612; http://dx.doi.org/10.1161/01.RES.78.5.916
   PubMed Web of Science ®Google Scholar
• Bean BP, Cohen CJ, Tsien RW. Lidocaine block of cardiac sodium channels. J Gen Physiol 1983; 81:613-42; PMID:6306139; http://dx.doi.org/10.1085/jgp.81.5.613
   PubMed Web of Science ®Google Scholar
• Bennett PB, Valenzuela C, Chen LQ, Kallen RG. On the molecular nature of the lidocaine receptor of cardiac Na+ channels. Circ Res 1995; 77:584-92; PMID: 7641328; http://dx.doi.org/10.1161/01.RES.77.3.584
   PubMed Web of Science ®Google Scholar
• Dumaine R, Kirsch GE. Mechanism of lidocaine block of late current in long Q-T mutant Na+ channels. Am Physiol Soc 1998; 274:H477-87
   PubMed Web of Science ®Google Scholar
• Hondeghem LM. Interaction of class I drugs with the cardiac sodium channel. In: Antiarrhythmic Drugs. edited by Vaughan Williams E. M.. Berlin: Springer-Verlag, 1989, p. 157174
   Google Scholar
• Wang DW, Yazawa K, Makita N, George AL Jr, Bennett PB. Pharmacological targeting of long QT mutant sodium channels. J Clin Invest 1997; 99:1714-20; PMID:9120016; http://dx.doi.org/10.1172/JCI119335
   PubMed Web of Science ®Google Scholar
• Ge H, Qian H. Physical origins of entropy production, free energy dissipation, and their mathematical representations. Phys Rev 2010; E 81:051133
   Google Scholar
• Ono M, Sunami A, Sawanobori T, Hiraoka M. External pH modi_es sodium channel block by mexiletine in guinea pig ventricular myocytes. Cardiovasc Res 1994; 28:973-9; PMID:7954609; http://dx.doi.org/10.1093/cvr/28.7.973
   PubMed Web of Science ®Google Scholar
• Ono M, Sunami A, Hiraoka M. Interaction between external Na+ channel in guinea-pig ventricular Myocytes. Pugers Arch 1995; 431:101-9; http://dx.doi.org/10.1007/BF00374382
   PubMed Web of Science ®Google Scholar
• Stramer CF, Agustus O Grant. Phasic ion channel blockade, kinetic model and parameter estimation procedure. Mol Pharmacol 1985; 28:348-56; PMID:2414642
   PubMed Web of Science ®Google Scholar
• Vilin YY, Ruben PC. Slow inactivation in voltage-gated sodium channels, molecular substrates and contributions to channelopathies. Cell Biochem Biophys 2001; 35:171-90; PMID:11892790; http://dx.doi.org/10.1385/CBB:35:2:171
   PubMed Web of Science ®Google Scholar
• Luo CH, Rudy Y. A dynamic model of the cardiac ventricular action potential. I. Simulations of ionic currents and concentration changes. Circ Res 1994; 74:1071-96; PMID:7514509; http://dx.doi.org/10.1161/01.RES.74.6.1071
   PubMed Web of Science ®Google Scholar
• Clancy CE, Rudy Y. Na(+) channel mutation that causes both brugada and long-QT syndrome phenotypes a simulation study of mechanism. Circulation 2002; 105:1208-13; PMID:11889015; http://dx.doi.org/10.1161/hc1002.105183
   PubMed Web of Science ®Google Scholar
• Groome JR, Lehmann-Horn F, Holzherr BD. Open- and closed-state fast inactivation in sodium channels Differential effects of a site-3 anemone toxin. Channels 2011; 5:65-78; PMID:21099342; http://dx.doi.org/10.4161/chan.5.1.14031
   PubMed Web of Science ®Google Scholar
• Armstrong CM. Na channel inactivation from open and closed states. Proc Nat Aacad Sci 2006; 103:17991-6; http://dx.doi.org/10.1073/pnas.0607603103
   PubMed Web of Science ®Google Scholar