General Information of This Target
Target ID
BTDT10148
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-6/alpha-3-beta-4
Target Bioclass
Receptor
Taxonomy ID
9606
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Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Alpha-conotoxin PeIA IC50
0.4 nM
[1- 9]
 Toxin Info    Alpha-conotoxin MII IC50
1.49 nM
[7- 22]
 Toxin Info    Alpha-conotoxin VnIB IC50
5.3 nM
[23]
 Toxin Info    Alpha-conotoxin PeIA IC50
6.75 nM
[1- 9]
References
Ref 1 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 2 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 3 -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 4 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 5 -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 6 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 7 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 8 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 9 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 10 The A-superfamily of conotoxins: structural and functional divergence. J Biol Chem. 2004 Apr 23;279(17):17596-606. doi: 10.1074/jbc.M309654200. Epub 2003 Dec 30.
Ref 11 Alpha-conotoxin GIC from Conus geographus, a novel peptide antagonist of nicotinic acetylcholine receptors. J Biol Chem. 2002 Sep 13;277(37):33610-5. doi: 10.1074/jbc.M205102200. Epub 2002 Jul 11.
Ref 12 A new alpha-conotoxin which targets alpha3beta2 nicotinic acetylcholine receptors. J Biol Chem. 1996 Mar 29;271(13):7522-8. doi: 10.1074/jbc.271.13.7522.
Ref 13 Human alpha6 AChR subtypes: subunit composition, assembly, and pharmacological responses. Neuropharmacology. 2000 Oct;39(13):2570-90. doi: 10.1016/s0028-3908(00)00144-1.
Ref 14 Analogs of alpha-conotoxin MII are selective for alpha6-containing nicotinic acetylcholine receptors. Mol Pharmacol. 2004 Apr;65(4):944-52. doi: 10.1124/mol.65.4.944.
Ref 15 Beta2 subunit contribution to 4/7 alpha-conotoxin binding to the nicotinic acetylcholine receptor. J Biol Chem. 2005 Aug 26;280(34):30460-8. doi: 10.1074/jbc.M504229200. Epub 2005 Jun 1.
Ref 16 Determinants of alpha-conotoxin BuIA selectivity on the nicotinic acetylcholine receptor beta subunit. Biochemistry. 2006 Sep 19;45(37):11200-7. doi: 10.1021/bi0611715.
Ref 17 Determinants of potency on alpha-conotoxin MII, a peptide antagonist of neuronal nicotinic receptors. Biochemistry. 2004 Mar 16;43(10):2732-7. doi: 10.1021/bi036180h.
Ref 18 Atypical alpha-conotoxin LtIA from Conus litteratus targets a novel microsite of the alpha3beta2 nicotinic receptor. J Biol Chem. 2010 Apr 16;285(16):12355-66. doi: 10.1074/jbc.M109.079012. Epub 2010 Feb 9.
Ref 19 -Conotoxins Enhance both the In Vivo Suppression of Ehrlich carcinoma Growth and In Vitro Reduction in Cell Viability Elicited by Cyclooxygenase and Lipoxygenase Inhibitors. Mar Drugs. 2020 Apr 7;18(4):193. doi: 10.3390/md18040193.
Ref 20 Three-dimensional solution structure of alpha-conotoxin MII, an alpha3beta2 neuronal nicotinic acetylcholine receptor-targeted ligand. Biochemistry. 1997 Dec 16;36(50):15693-700. doi: 10.1021/bi971443r.
Ref 21 Three-dimensional solution structure of alpha-conotoxin MII by NMR spectroscopy: effects of solution environment on helicity. Biochemistry. 1998 Nov 10;37(45):15621-30. doi: 10.1021/bi981535w.
Ref 22 Engineering stable peptide toxins by means of backbone cyclization: stabilization of the alpha-conotoxin MII. Proc Natl Acad Sci U S A. 2005 Sep 27;102(39):13767-72. doi: 10.1073/pnas.0504613102. Epub 2005 Sep 14.
Ref 23 -Conotoxin VnIB from Conus ventricosus is a potent and selective antagonist of 64* nicotinic acetylcholine receptors. Neuropharmacology. 2019 Oct;157:107691. doi: 10.1016/j.neuropharm.2019.107691. Epub 2019 Jun 28.
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