Target Information

General Information of This Target
Target ID
BTDT10150
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-6/alpha-3-beta-4
Target Bioclass
Receptor
Taxonomy ID
10116
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Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Rodentia
Family: Muridae
Genus: Rattus
Species: Rattus norvegicus
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Conotoxin Bt1.8 IC50
>100 nM
 [1]
 Toxin Info    Alpha-conotoxin PeIA IC50
0.2 nM
 [2- 10]
 Toxin Info    Alpha-conotoxin VnIB IC50
18 nM
 [11]
 Toxin Info    Alpha-conotoxin QcIA IC50
90.69 nM
 [12], [13]
 Toxin Info    Alpha-conotoxin LvIA IC50
121 nM
 [6- 15]
 Toxin Info    Alpha-conotoxin PeIA IC50
130 - 147 nM
 [2- 10]
 Toxin Info    Alpha-conotoxin Lt1a IC50
˜6 μM
 [16], [17], [18]
 Toxin Info    Alpha-conotoxin LvIC IC50
3.3 μM
 [19]
References
Ref 1 -Conotoxin Bt1.8 from Conus betulinus selectively inhibits 6/323 and 32 nicotinic acetylcholine receptor subtypes. J Neurochem. 2021 Oct;159(1):90-100. doi: 10.1111/jnc.15434. Epub 2021 Jun 22.
Ref 2 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 3 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 4 -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 5 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 6 -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 7 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 8 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 9 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 10 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 11 -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.
Ref 12 High-Throughput Identification and Analysis of Novel Conotoxins from Three Vermivorous Cone Snails by Transcriptome Sequencing. Mar Drugs. 2019 Mar 26;17(3):193. doi: 10.3390/md17030193.
Ref 13 A Novel 4/7-Conotoxin QuIA Selectively Inhibits 32 and 6/34 Nicotinic Acetylcholine Receptor Subtypes with High Efficacy. Mar Drugs. 2022 Feb 17;20(2):146. doi: 10.3390/md20020146.
Ref 14 A novel 4/7-conotoxin LvIA from Conus lividus that selectively blocks 32 vs. 6/323 nicotinic acetylcholine receptors. FASEB J. 2014 Apr;28(4):1842-53. doi: 10.1096/fj.13-244103. Epub 2014 Jan 7.
Ref 15 Recombinant Expression and Characterization of -Conotoxin LvIA in Escherichia coli. Mar Drugs. 2016 Jan 5;14(1):11. doi: 10.3390/md14010011.
Ref 16 Diversity and evolution of conotoxins based on gene expression profiling of Conus litteratus. Genomics. 2006 Dec;88(6):809-819. doi: 10.1016/j.ygeno.2006.06.014. Epub 2006 Aug 14.
Ref 17 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 18 Design, Synthesis, and Activity of an -Conotoxin LtIA Fluorescent Analogue. ACS Chem Neurosci. 2021 Oct 6;12(19):3662-3671. doi: 10.1021/acschemneuro.1c00392. Epub 2021 Sep 15.
Ref 19 Discovery, Characterization, and Engineering of LvIC, an 4/4-Conotoxin That Selectively Blocks Rat 6/34 Nicotinic Acetylcholine Receptors. J Med Chem. 2023 Feb 9;66(3):2020-2031. doi: 10.1021/acs.jmedchem.2c01786. Epub 2023 Jan 22.
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