General Information of This Target
Target ID
BTDT10162
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-9-alpha-10
Target Bioclass
Receptor
        Click to Show/Hide the Complete Species Lineage
N.A.
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Elevenin-Vc1 Effect . [1], [2], [3]
 Toxin Info    Alpha-conotoxin-like Pu1.2 Inhibition rate . [4], [5]
 Toxin Info    Alpha-conotoxin GeXIVA IC50
4.61 - 12 nM
[6], [7], [8], [9]
 Toxin Info    Alpha-conotoxin PeIA IC50
6.9 - 54.9 nM
[10- 18]
 Toxin Info    Alpha-conotoxin GVIIIB IC50
9.79 nM
[19], [20]
 Toxin Info    O-conotoxin GeXXXIA IC50
16.2 nM
[21]
 Toxin Info    Alpha-conotoxin GeXIVA IC50
22.7 nM
[6], [7], [8], [9]
 Toxin Info    Alpha-conotoxin Vc1a IC50
62.9 nM
[5- 36]
 Toxin Info    Alpha-conotoxin RVIIIA IC50
187 nM
[20- 38]
 Toxin Info    Alpha-conotoxin GeXIVA IC50
716 nM
[6], [7], [8], [9]
 Toxin Info    Alpha-conotoxin Vc1a IC50
766 nM
[5- 36]
 Toxin Info    Alpha-conotoxin MilIA IC50
>10 μM
[39]
 Toxin Info    Alpha-conotoxin Vc1.2 IC50
1 μM
[40]
 Toxin Info    Alpha-conotoxin GIB IC50
1.113 μM
[19- 41]
 Toxin Info    Alpha-conotoxin Lt28.1 IC50
3 μM
[42]
References
Ref 1 Diversity of conotoxin gene superfamilies in the venomous snail, Conus victoriae. PLoS One. 2014 Feb 5;9(2):e87648. doi: 10.1371/journal.pone.0087648. eCollection 2014.
Ref 2 Hormone-like peptides in the venoms of marine cone snails. Gen Comp Endocrinol. 2017 Apr 1;244:11-18. doi: 10.1016/j.ygcen.2015.07.012. Epub 2015 Aug 22.
Ref 3 Characterisation of Elevenin-Vc1 from the Venom of Conus victoriae: A Structural Analogue of -Conotoxins. Mar Drugs. 2023 Jan 25;21(2):81. doi: 10.3390/md21020081.
Ref 4 From the identification of gene organization of alpha conotoxins to the cloning of novel toxins. Toxicon. 2007 Jun 15;49(8):1135-49. doi: 10.1016/j.toxicon.2007.02.011. Epub 2007 Mar 1.
Ref 5 Structure-Activity Studies of Cysteine-Rich -Conotoxins that Inhibit High-Voltage-Activated Calcium Channels via GABA(B) Receptor Activation Reveal a Minimal Functional Motif. Angew Chem Int Ed Engl. 2016 Apr 4;55(15):4692-6. doi: 10.1002/anie.201600297. Epub 2016 Mar 7.
Ref 6 Expression, renaturation and biological activity of recombinant conotoxin GeXIVAWT. Appl Microbiol Biotechnol. 2013 Feb;97(3):1223-30. doi: 10.1007/s00253-012-4287-6. Epub 2012 Jul 24.
Ref 7 Cloning, synthesis, and characterization of O-conotoxin GeXIVA, a potent 910 nicotinic acetylcholine receptor antagonist. Proc Natl Acad Sci U S A. 2015 Jul 28;112(30):E4026-35. doi: 10.1073/pnas.1503617112. Epub 2015 Jul 13.
Ref 8 Anti-hypersensitive effect of intramuscular administration of O-conotoxin GeXIVA[1,2] and GeXIVA[1,4] in rats of neuropathic pain. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Apr 3;66:112-119. doi: 10.1016/j.pnpbp.2015.12.005. Epub 2015 Dec 17.
Ref 9 Structure and Activity Studies of Disulfide-Deficient Analogues of O-Conotoxin GeXIVA. J Med Chem. 2020 Feb 27;63(4):1564-1575. doi: 10.1021/acs.jmedchem.9b01409. Epub 2020 Feb 7.
Ref 10 A novel alpha-conotoxin, PeIA, cloned from Conus pergrandis, discriminates between rat alpha9alpha10 and alpha7 nicotinic cholinergic receptors. J Biol Chem. 2005 Aug 26;280(34):30107-12. doi: 10.1074/jbc.M504102200. Epub 2005 Jun 27.
Ref 11 Structure and activity of alpha-conotoxin PeIA at nicotinic acetylcholine receptor subtypes and GABA(B) receptor-coupled N-type calcium channels. J Biol Chem. 2011 Mar 25;286(12):10233-7. doi: 10.1074/jbc.M110.196170. Epub 2011 Jan 20.
Ref 12 -Conotoxin PeIA[S9H,V10A,E14N] potently and selectively blocks 623 versus 64 nicotinic acetylcholine receptors. Mol Pharmacol. 2012 Nov;82(5):972-82. doi: 10.1124/mol.112.080853. Epub 2012 Aug 22.
Ref 13 Positional scanning mutagenesis of -conotoxin PeIA identifies critical residues that confer potency and selectivity for 6/323 and 32 nicotinic acetylcholine receptors. J Biol Chem. 2013 Aug 30;288(35):25428-25439. doi: 10.1074/jbc.M113.482059. Epub 2013 Jul 11.
Ref 14 -Conotoxins Identify the 34* Subtype as the Predominant Nicotinic Acetylcholine Receptor Expressed in Human Adrenal Chromaffin Cells. Mol Pharmacol. 2015 Nov;88(5):881-93. doi: 10.1124/mol.115.100982. Epub 2015 Sep 1.
Ref 15 Correction to "-Conotoxins Identify the 34* Subtype as the Predominant Nicotinic Acetylcholine Receptor Expressed in Human Adrenal Chromaffin Cells". Mol Pharmacol. 2016 Feb;89(2):322. doi: 10.1124/mol.115.100982err.
Ref 16 Inhibition of cholinergic pathways in Drosophila melanogaster by -conotoxins. FASEB J. 2015 Mar;29(3):1011-8. doi: 10.1096/fj.14-262733. Epub 2014 Dec 2.
Ref 17 Dimerization of -Conotoxins as a Strategy to Enhance the Inhibition of the Human 7 and 910 Nicotinic Acetylcholine Receptors. J Med Chem. 2020 Mar 26;63(6):2974-2985. doi: 10.1021/acs.jmedchem.9b01536. Epub 2020 Mar 17.
Ref 18 Computational and Functional Mapping of Human and Rat 64 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs. J Med Chem. 2021 Feb 11;64(3):1685-1700. doi: 10.1021/acs.jmedchem.0c01973. Epub 2021 Feb 1.
Ref 19 Evolution of separate predation- and defence-evoked venoms in carnivorous cone snails. Nat Commun. 2014 Mar 24;5:3521. doi: 10.1038/ncomms4521.
Ref 20 S-conotoxin GVIIIB potently and selectively blocks 910 nicotinic acetylcholine receptors. Biochem Pharmacol. 2015 Aug 15;96(4):349-56. doi: 10.1016/j.bcp.2015.06.007. Epub 2015 Jun 11.
Ref 21 Identification of a Novel O-Conotoxin Reveals an Unusual and Potent Inhibitor of the Human 910 Nicotinic Acetylcholine Receptor. Mar Drugs. 2017 Jun 9;15(6):170. doi: 10.3390/md15060170.
Ref 22 A novel alpha-conotoxin identified by gene sequencing is active in suppressing the vascular response to selective stimulation of sensory nerves in vivo. Biochemistry. 2003 Jun 10;42(22):6904-11. doi: 10.1021/bi034043e.
Ref 23 Determining sequences and post-translational modifications of novel conotoxins in Conus victoriae using cDNA sequencing and mass spectrometry. J Mass Spectrom. 2004 May;39(5):548-57. doi: 10.1002/jms.624.
Ref 24 A conus peptide blocks nicotinic receptors of unmyelinated axons in human nerves. Neuroreport. 2005 Apr 4;16(5):479-83. doi: 10.1097/00001756-200504040-00012.
Ref 25 Molecular mechanism for analgesia involving specific antagonism of alpha9alpha10 nicotinic acetylcholine receptors. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17880-4. doi: 10.1073/pnas.0608715103. Epub 2006 Nov 13.
Ref 26 Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?. Mol Pharmacol. 2007 Dec;72(6):1406-10. doi: 10.1124/mol.107.040568. Epub 2007 Sep 5.
Ref 27 Analgesic alpha-conotoxins Vc1.1 and Rg1A inhibit N-type calcium channels in rat sensory neurons via GABAB receptor activation. J Neurosci. 2008 Oct 22;28(43):10943-51. doi: 10.1523/JNEUROSCI.3594-08.2008.
Ref 28 Scanning mutagenesis of alpha-conotoxin Vc1.1 reveals residues crucial for activity at the alpha9alpha10 nicotinic acetylcholine receptor. J Biol Chem. 2009 Jul 24;284(30):20275-84. doi: 10.1074/jbc.M109.015339. Epub 2009 May 15.
Ref 29 Determination of the -conotoxin Vc1.1 binding site on the 910 nicotinic acetylcholine receptor. J Med Chem. 2013 May 9;56(9):3557-67. doi: 10.1021/jm400041h. Epub 2013 Apr 29.
Ref 30 Cyclic analogues of -conotoxin Vc1.1 inhibit colonic nociceptors and provide analgesia in a mouse model of chronic abdominal pain. Br J Pharmacol. 2018 Jun;175(12):2384-2398. doi: 10.1111/bph.14115. Epub 2018 Feb 13.
Ref 31 The synthesis, structural characterization, and receptor specificity of the alpha-conotoxin Vc1.1. J Biol Chem. 2006 Aug 11;281(32):23254-63. doi: 10.1074/jbc.M604550200. Epub 2006 Jun 5.
Ref 32 The engineering of an orally active conotoxin for the treatment of neuropathic pain. Angew Chem Int Ed Engl. 2010 Sep 3;49(37):6545-8. doi: 10.1002/anie.201000620.
Ref 33 Dicarba -conotoxin Vc1.1 analogues with differential selectivity for nicotinic acetylcholine and GABAB receptors. ACS Chem Biol. 2013 Aug 16;8(8):1815-21. doi: 10.1021/cb4002393. Epub 2013 Jun 17.
Ref 34 Racemic and quasi-racemic X-ray structures of cyclic disulfide-rich peptide drug scaffolds. Angew Chem Int Ed Engl. 2014 Oct 13;53(42):11236-41. doi: 10.1002/anie.201406563. Epub 2014 Aug 28.
Ref 35 Less is More: Design of a Highly Stable Disulfide-Deleted Mutant of Analgesic Cyclic -Conotoxin Vc1.1. Sci Rep. 2015 Aug 20;5:13264. doi: 10.1038/srep13264.
Ref 36 Structure-Activity Studies Reveal the Molecular Basis for GABA(B)-Receptor Mediated Inhibition of High Voltage-Activated Calcium Channels by -Conotoxin Vc1.1. ACS Chem Biol. 2018 Jun 15;13(6):1577-1587. doi: 10.1021/acschembio.8b00190. Epub 2018 May 25.
Ref 37 Evolution of Conus peptide toxins: analysis of Conus californicus Reeve, 1844. Mol Phylogenet Evol. 2010 Jul;56(1):1-12. doi: 10.1016/j.ympev.2010.03.029. Epub 2010 Apr 2.
Ref 38 Alpha S-conotoxin RVIIIA: a structurally unique conotoxin that broadly targets nicotinic acetylcholine receptors. Biochemistry. 2005 May 31;44(21):7897-902. doi: 10.1021/bi047274+.
Ref 39 Structure-Function Elucidation of a New -Conotoxin, MilIA, from Conus milneedwardsi. Mar Drugs. 2019 Sep 16;17(9):535. doi: 10.3390/md17090535.
Ref 40 Embryonic toxin expression in the cone snail Conus victoriae: primed to kill or divergent function?. J Biol Chem. 2011 Jun 24;286(25):22546-57. doi: 10.1074/jbc.M110.217703. Epub 2011 Apr 19.
Ref 41 Globular and ribbon isomers of Conus geographus -conotoxins antagonize human nicotinic acetylcholine receptors. Biochem Pharmacol. 2021 Aug;190:114638. doi: 10.1016/j.bcp.2021.114638. Epub 2021 May 29.
Ref 42 Cloning, expression and functional characterization of a D-superfamily conotoxin Lt28.1 with previously undescribed cysteine pattern. Peptides. 2017 Aug;94:64-70. doi: 10.1016/j.peptides.2017.06.008. Epub 2017 Jun 27.
Data Quality & Feedback

Help us maintain data quality by reporting any errors or inaccuracies you may find.

samedaypayday.com visits since 2024

If you find any error in data or bug in web service, please kindly report it to biodb_contact@163.com et al.