Target Information

General Information of This Target
Target ID
BTDT10256
Target Name
Sodium channel protein type 1 subunit alpha
Target Bioclass
Transporter and channel
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N.A.
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Mu-conotoxin GVIIJ Dissociation constant
11 nM
 [1- 5]
 Toxin Info    Mu-thomitoxin-Hme1c Inhibition rate . [6], [7]
 Toxin Info    Toxin Acra3 Inhibition rate . [8], [9]
 Toxin Info    Beta-mammal toxin Css2 Inhibition rate . [10- 19]
 Toxin Info    Potassium channel toxin alpha-KTx 1.16 Inhibition rate . [20], [21]
 Toxin Info    Potassium channel toxin alpha-KTx 1.17 Inhibition rate . [20], [21]
 Toxin Info    Omega toxin Ap5 Inhibition rate
6.6 %
 [22]
 Toxin Info    Beta-toxin Tf1a Inhibition rate
17 - 30 %
 [23]
 Toxin Info    Beta-mammal/insect toxin To1 Inhibition rate
53.3 %
 [24- 28]
 Toxin Info    Delta-actitoxin-Bcs1a Effective concentration 50
˜300 nM
 [29], [30], [31]
 Toxin Info    Delta-buthitoxin-Hj1a Effective concentration 50
17 nM
 [32]
 Toxin Info    Delta-buthitoxin-Hj2a Effective concentration 50
52.8 nM
 [32]
 Toxin Info    Delta-actitoxin-Bcg1b Effective concentration 50
165 nM
 [31- 35]
 Toxin Info    Delta-actitoxin-Afv1b Effective concentration 50
390.55 nM
 [30- 36]
 Toxin Info    Delta-actitoxin-Bcg1d Effective concentration 50
453 nM
 [31- 37]
 Toxin Info    Toxin GTx1-15 IC50
6 nM
 [38], [39]
 Toxin Info    Toxin GTx1-15 IC50
6 nM
 [40], [41]
 Toxin Info    Beta-theraphotoxin-Ps1a IC50
20 - 610 nM
 [39- 43]
 Toxin Info    Mu/omega-theraphotoxin-Tap1a IC50
81 - 301 nM
 [44]
 Toxin Info    Mu-conotoxin SxIIIC IC50
132 nM
 [45]
 Toxin Info    Mu/omega-theraphotoxin-Tap2a IC50
169 - 621 nM
 [44]
 Toxin Info    Beta-theraphotoxin-Cm1b IC50
170 - 407 nM
 [39- 46]
 Toxin Info    Mu-theraphotoxin-Pspp1 IC50
280.3 nM
 [47], [48], [49], [50]
 Toxin Info    Beta-theraphotoxin-Gr1b IC50
360 nM
 [51], [52], [49]
 Toxin Info    Beta-theraphotoxin-Gr1a IC50
630 nM
 [49- 53]
 Toxin Info    Beta-theraphotoxin-Cm1a IC50
0.523 - 1.06 μM
 [39- 54]
 Toxin Info    Hainantoxin-III 1 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 2 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 4 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 5 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 6 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 7 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 8 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 9 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 10 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 11 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    Hainantoxin-III 12 IC50
1.27 μM
 [55], [56], [57]
 Toxin Info    MuO-conotoxin MfVIA IC50
3.3 μM
 [58], [59]
 Toxin Info    Kappa-theraphotoxin-Gr2c IC50
5.7 μM
 [38- 52]
 Toxin Info    M-theraphotoxin-Gr1a IC50
7.4 - 14 μM
 [38- 70]
References
Ref 1 Evolution of separate predation- and defence-evoked venoms in carnivorous cone snails. Nat Commun. 2014 Mar 24;5:3521. doi: 10.1038/ncomms4521.
Ref 2 A disulfide tether stabilizes the block of sodium channels by the conotoxin O-GVIIJ. Proc Natl Acad Sci U S A. 2014 Feb 18;111(7):2758-63. doi: 10.1073/pnas.1324189111. Epub 2014 Feb 4.
Ref 3 Probing the Redox States of Sodium Channel Cysteines at the Binding Site of O-Conotoxin GVIIJ. Biochemistry. 2015 Jun 30;54(25):3911-20. doi: 10.1021/acs.biochem.5b00390. Epub 2015 Jun 18.
Ref 4 - and -subunit composition of voltage-gated sodium channels investigated with -conotoxins and the recently discovered O-conotoxin GVIIJ. J Neurophysiol. 2015 Apr 1;113(7):2289-301. doi: 10.1152/jn.01004.2014. Epub 2015 Jan 28.
Ref 5 Structural Basis for the Inhibition of Voltage-gated Sodium Channels by Conotoxin O-GVIIJ. J Biol Chem. 2016 Mar 25;291(13):7205-20. doi: 10.1074/jbc.M115.697672. Epub 2016 Jan 27.
Ref 6 Structure of membrane-active toxin from crab spider Heriaeus melloteei suggests parallel evolution of sodium channel gating modifiers in Araneomorphae and Mygalomorphae. J Biol Chem. 2015 Jan 2;290(1):492-504. doi: 10.1074/jbc.M114.595678. Epub 2014 Oct 28.
Ref 7 Spider toxin inhibits gating pore currents underlying periodic paralysis. Proc Natl Acad Sci U S A. 2018 Apr 24;115(17):4495-4500. doi: 10.1073/pnas.1720185115. Epub 2018 Apr 10.
Ref 8 Purification and cDNA cloning of a novel neurotoxic peptide (Acra3) from the scorpion Androctonus crassicauda. Peptides. 2012 Sep;37(1):106-12. doi: 10.1016/j.peptides.2012.07.009. Epub 2012 Jul 20.
Ref 9 Biological assays on the effects of Acra3 peptide from Turkish scorpion Androctonus crassicauda venom on a mouse brain tumor cell line (BC3H1) and production of specific monoclonal antibodies. Toxicon. 2013 Dec 15;76:350-61. doi: 10.1016/j.toxicon.2013.09.009. Epub 2013 Sep 19.
Ref 10 Purification and chemical and biological characterizations of seven toxins from the Mexican scorpion, Centruroides suffusus suffusus. J Biol Chem. 1987 Apr 5;262(10):4452-9.
Ref 11 Expression of functional recombinant scorpion beta-neurotoxin Css II in E. coli. Peptides. 2000 Jun;21(6):767-72. doi: 10.1016/s0196-9781(00)00206-0.
Ref 12 Four disulfide-bridged scorpion beta neurotoxin CssII: heterologous expression and proper folding in vitro. Biochim Biophys Acta. 2007 Aug;1770(8):1161-8. doi: 10.1016/j.bbagen.2007.04.006. Epub 2007 May 1.
Ref 13 Isolation and molecular cloning of beta-neurotoxins from the venom of the scorpion Centruroides suffusus suffusus. Toxicon. 2011 Apr;57(5):739-46. doi: 10.1016/j.toxicon.2011.02.006. Epub 2011 Feb 15.
Ref 14 Heterologous expressed toxic and non-toxic peptide variants of toxin CssII are capable to produce neutralizing antibodies against the venom of the scorpion Centruroides suffusus suffusus. Immunol Lett. 2009 Aug 15;125(2):93-9. doi: 10.1016/j.imlet.2009.06.001. Epub 2009 Jun 12.
Ref 15 Differential phospholipid binding by site 3 and site 4 toxins. Implications for structural variability between voltage-sensitive sodium channel domains. J Biol Chem. 2005 Mar 25;280(12):11127-33. doi: 10.1074/jbc.M412552200. Epub 2005 Jan 4.
Ref 16 Addition of positive charges at the C-terminal peptide region of CssII, a mammalian scorpion peptide toxin, improves its affinity for sodium channels Nav1.6. Peptides. 2011 Jan;32(1):75-9. doi: 10.1016/j.peptides.2010.11.001. Epub 2010 Nov 13.
Ref 17 Negative-shift activation, current reduction and resurgent currents induced by -toxins from Centruroides scorpions in sodium channels. Toxicon. 2012 Feb;59(2):283-93. doi: 10.1016/j.toxicon.2011.12.003. Epub 2011 Dec 16.
Ref 18 Generation of a Broadly Cross-Neutralizing Antibody Fragment against Several Mexican Scorpion Venoms. Toxins (Basel). 2019 Jan 10;11(1):32. doi: 10.3390/toxins11010032.
Ref 19 Solution structure of native and recombinant expressed toxin CssII from the venom of the scorpion Centruroides suffusus suffusus, and their effects on Nav1.5 sodium channels. Biochim Biophys Acta. 2012 Mar;1824(3):478-87. doi: 10.1016/j.bbapap.2012.01.003. Epub 2012 Jan 11.
Ref 20 Variability of Potassium Channel Blockers in Mesobuthus eupeus Scorpion Venom with Focus on Kv1.1: AN INTEGRATED TRANSCRIPTOMIC AND PROTEOMIC STUDY. J Biol Chem. 2015 May 8;290(19):12195-209. doi: 10.1074/jbc.M115.637611. Epub 2015 Mar 19.
Ref 21 K(V)1.2 channel-specific blocker from Mesobuthus eupeus scorpion venom: Structural basis of selectivity. Neuropharmacology. 2018 Dec;143:228-238. doi: 10.1016/j.neuropharm.2018.09.030. Epub 2018 Sep 22.
Ref 22 Purification and characterization of peptides Ap2, Ap3 and Ap5 (-toxins) from the venom of the Brazilian tarantula Acanthoscurria paulensis. Peptides. 2021 Nov;145:170622. doi: 10.1016/j.peptides.2021.170622. Epub 2021 Aug 5.
Ref 23 Subtype Specificity of -Toxin Tf1a from Tityus fasciolatus in Voltage Gated Sodium Channels. Toxins (Basel). 2018 Aug 22;10(9):339. doi: 10.3390/toxins10090339.
Ref 24 Identification and phylogenetic analysis of Tityus pachyurus and Tityus obscurus novel putative Na+-channel scorpion toxins. PLoS One. 2012;7(2):e30478. doi: 10.1371/journal.pone.0030478. Epub 2012 Feb 15.
Ref 25 Proteomic endorsed transcriptomic profiles of venom glands from Tityus obscurus and T. serrulatus scorpions. PLoS One. 2018 Mar 21;13(3):e0193739. doi: 10.1371/journal.pone.0193739. eCollection 2018.
Ref 26 Scorpion toxins from Tityus cambridgei that affect Na(+)-channels. Toxicon. 2002 May;40(5):557-62. doi: 10.1016/s0041-0101(01)00252-5.
Ref 27 Proteomics of the venom from the Amazonian scorpion Tityus cambridgei and the role of prolines on mass spectrometry analysis of toxins. J Chromatogr B Analyt Technol Biomed Life Sci. 2004 Apr 15;803(1):55-66. doi: 10.1016/j.jchromb.2003.09.002.
Ref 28 Electrophysiological characterization of Tityus obscurus toxin 1 (To1) on Na(+)-channel isoforms. Biochim Biophys Acta Biomembr. 2019 Jan;1861(1):142-150. doi: 10.1016/j.bbamem.2018.08.005. Epub 2018 Aug 14.
Ref 29 Characterization of peptides in sea anemone venom collected by a novel procedure. Toxicon. 1993 Jul;31(7):853-64. doi: 10.1016/0041-0101(93)90220-d.
Ref 30 Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop. J Biol Chem. 2004 Aug 6;279(32):33323-35. doi: 10.1074/jbc.M404344200. Epub 2004 May 28.
Ref 31 Development of a rational nomenclature for naming peptide and protein toxins from sea anemones. Toxicon. 2012 Sep 15;60(4):539-50. doi: 10.1016/j.toxicon.2012.05.020. Epub 2012 Jun 5.
Ref 32 Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel Na(V)1.1 Provide Novel Leads for Development of Antiepileptic Drugs. ACS Pharmacol Transl Sci. 2019 Nov 25;3(1):119-134. doi: 10.1021/acsptsci.9b00079. eCollection 2020 Feb 14.
Ref 33 Revisiting cangitoxin, a sea anemone peptide: purification and characterization of cangitoxins II and III from the venom of Bunodosoma cangicum. Toxicon. 2008 Jun 1;51(7):1303-7. doi: 10.1016/j.toxicon.2008.01.011. Epub 2008 Feb 2.
Ref 34 Characterization of selectivity and pharmacophores of type 1 sea anemone toxins by screening seven Na(v) sodium channel isoforms. Peptides. 2012 Mar;34(1):158-67. doi: 10.1016/j.peptides.2011.07.008. Epub 2011 Jul 20.
Ref 35 Actions of sea anemone type 1 neurotoxins on voltage-gated sodium channel isoforms. Toxicon. 2009 Dec 15;54(8):1102-11. doi: 10.1016/j.toxicon.2009.04.018. Epub 2009 Apr 23.
Ref 36 Amino acid sequence of two sea anemone toxins from Anthopleura fuscoviridis. Toxicon. 1987;25(2):211-9. doi: 10.1016/0041-0101(87)90243-1.
Ref 37 Proteomics of the neurotoxic fraction from the sea anemone Bunodosoma cangicum venom: Novel peptides belonging to new classes of toxins. Comp Biochem Physiol Part D Genomics Proteomics. 2008 Sep;3(3):219-25. doi: 10.1016/j.cbd.2008.04.002. Epub 2008 Apr 26.
Ref 38 Characterization of voltage-dependent calcium channel blocking peptides from the venom of the tarantula Grammostola rosea. Toxicon. 2011 Sep 1;58(3):265-76. doi: 10.1016/j.toxicon.2011.06.006. Epub 2011 Jun 28.
Ref 39 Gating modifier toxins isolated from spider venom: Modulation of voltage-gated sodium channels and the role of lipid membranes. J Biol Chem. 2018 Jun 8;293(23):9041-9052. doi: 10.1074/jbc.RA118.002553. Epub 2018 Apr 27.
Ref 40 Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel. J Med Chem. 2015 Mar 12;58(5):2299-314. doi: 10.1021/jm501765v. Epub 2015 Feb 19.
Ref 41 Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain. Toxins (Basel). 2016 Mar 17;8(3):78. doi: 10.3390/toxins8030078.
Ref 42 Four novel tarantula toxins as selective modulators of voltage-gated sodium channel subtypes. Mol Pharmacol. 2006 Feb;69(2):419-29. doi: 10.1124/mol.105.015941. Epub 2005 Nov 2.
Ref 43 Lengths of the C-Terminus and Interconnecting Loops Impact Stability of Spider-Derived Gating Modifier Toxins. Toxins (Basel). 2017 Aug 12;9(8):248. doi: 10.3390/toxins9080248.
Ref 44 A spider-venom peptide with multitarget activity on sodium and calcium channels alleviates chronic visceral pain in a model of irritable bowel syndrome. Pain. 2021 Feb 1;162(2):569-581. doi: 10.1097/j.pain.0000000000002041.
Ref 45 Discovery, Pharmacological Characterisation and NMR Structure of the Novel -Conotoxin SxIIIC, a Potent and Irreversible Na(V) Channel Inhibitor. Biomedicines. 2020 Oct 2;8(10):391. doi: 10.3390/biomedicines8100391.
Ref 46 Discovery and mode of action of a novel analgesic -toxin from the African spider Ceratogyrus darlingi. PLoS One. 2017 Sep 7;12(9):e0182848. doi: 10.1371/journal.pone.0182848. eCollection 2017.
Ref 47 Pharmacological characterisation of the highly Na(V)1.7 selective spider venom peptide Pn3a. Sci Rep. 2017 Jan 20;7:40883. doi: 10.1038/srep40883.
Ref 48 Corrigendum: Pharmacological characterisation of the highly Na(V)1.7 selective spider venom peptide Pn3a. Sci Rep. 2017 May 26;7:46816. doi: 10.1038/srep46816.
Ref 49 Chemical Synthesis, Proper Folding, Na(v) Channel Selectivity Profile and Analgesic Properties of the Spider Peptide Phlotoxin 1. Toxins (Basel). 2019 Jun 21;11(6):367. doi: 10.3390/toxins11060367.
Ref 50 Evaluation of the Spider (Phlogiellus genus) Phlotoxin 1 and Synthetic Variants as Antinociceptive Drug Candidates. Toxins (Basel). 2019 Aug 22;11(9):484. doi: 10.3390/toxins11090484.
Ref 51 Target promiscuity and heterogeneous effects of tarantula venom peptides affecting Na+ and K+ ion channels. J Biol Chem. 2010 Feb 5;285(6):4130-4142. doi: 10.1074/jbc.M109.054718. Epub 2009 Dec 2.
Ref 52 Structural Basis of Nav1.7 Inhibition by a Gating-Modifier Spider Toxin. Cell. 2019 Feb 7;176(4):702-715.e14. doi: 10.1016/j.cell.2018.12.018. Epub 2019 Jan 17.
Ref 53 Isolation and characterization of a novel toxin from the venom of the spider Grammostola rosea that blocks sodium channels. Toxicon. 2007 Jul;50(1):65-74. doi: 10.1016/j.toxicon.2007.02.015. Epub 2007 Mar 3.
Ref 54 Engineering Highly Potent and Selective Microproteins against Nav1.7 Sodium Channel for Treatment of Pain. J Biol Chem. 2016 Jul 1;291(27):13974-13986. doi: 10.1074/jbc.M116.725978. Epub 2016 Apr 22.
Ref 55 Molecular diversification of peptide toxins from the tarantula Haplopelma hainanum (Ornithoctonus hainana) venom based on transcriptomic, peptidomic, and genomic analyses. J Proteome Res. 2010 May 7;9(5):2550-64. doi: 10.1021/pr1000016.
Ref 56 Inhibition of neuronal tetrodotoxin-sensitive Na+ channels by two spider toxins: hainantoxin-III and hainantoxin-IV. Eur J Pharmacol. 2003 Sep 5;477(1):1-7. doi: 10.1016/s0014-2999(03)02190-3.
Ref 57 Structure and function of hainantoxin-III, a selective antagonist of neuronal tetrodotoxin-sensitive voltage-gated sodium channels isolated from the Chinese bird spider Ornithoctonus hainana. J Biol Chem. 2013 Jul 12;288(28):20392-403. doi: 10.1074/jbc.M112.426627. Epub 2013 May 23.
Ref 58 Isolation, characterization and total regioselective synthesis of the novel O-conotoxin MfVIA from Conus magnificus that targets voltage-gated sodium channels. Biochem Pharmacol. 2012 Aug 15;84(4):540-8. doi: 10.1016/j.bcp.2012.05.008. Epub 2012 May 16.
Ref 59 Development of a O-Conotoxin Analogue with Improved Lipid Membrane Interactions and Potency for the Analgesic Sodium Channel NaV1.8. J Biol Chem. 2016 May 27;291(22):11829-42. doi: 10.1074/jbc.M116.721662. Epub 2016 Mar 29.
Ref 60 cDNA sequence and in vitro folding of GsMTx4, a specific peptide inhibitor of mechanosensitive channels. Toxicon. 2003 Sep;42(3):263-74. doi: 10.1016/s0041-0101(03)00141-7.
Ref 61 Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J Gen Physiol. 2000 May;115(5):583-98. doi: 10.1085/jgp.115.5.583.
Ref 62 Solution structure of peptide toxins that block mechanosensitive ion channels. J Biol Chem. 2002 Sep 13;277(37):34443-50. doi: 10.1074/jbc.M202715200. Epub 2002 Jun 24.
Ref 63 Tarantula peptide inhibits atrial fibrillation. Nature. 2001 Jan 4;409(6816):35-6. doi: 10.1038/35051165.
Ref 64 Localization of the voltage-sensor toxin receptor on KvAP. Biochemistry. 2004 Aug 10;43(31):10071-9. doi: 10.1021/bi049463y.
Ref 65 Bilayer-dependent inhibition of mechanosensitive channels by neuroactive peptide enantiomers. Nature. 2004 Jul 8;430(6996):235-40. doi: 10.1038/nature02743.
Ref 66 Lipid membrane interaction and antimicrobial activity of GsMTx-4, an inhibitor of mechanosensitive channel. Biochem Biophys Res Commun. 2006 Feb 10;340(2):633-8. doi: 10.1016/j.bbrc.2005.12.046. Epub 2005 Dec 19.
Ref 67 Effects of tarantula toxin GsMTx4 on the membrane motor of outer hair cells. Neurosci Lett. 2006 Aug 14;404(1-2):213-6. doi: 10.1016/j.neulet.2006.05.059. Epub 2006 Jun 22.
Ref 68 Molecular dynamics simulations of a stretch-activated channel inhibitor GsMTx4 with lipid membranes: two binding modes and effects of lipid structure. Biophys J. 2007 Jun 15;92(12):4233-43. doi: 10.1529/biophysj.106.101071. Epub 2007 Mar 23.
Ref 69 Is lipid bilayer binding a common property of inhibitor cysteine knot ion-channel blockers?. Biophys J. 2007 Aug 15;93(4):L20-2. doi: 10.1529/biophysj.107.112375. Epub 2007 Jun 15.
Ref 70 Fast desensitization of acetylcholine receptors induced by a spider toxin. Channels (Austin). 2021 Dec;15(1):507-515. doi: 10.1080/19336950.2021.1961459.
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