General Information of This Target
Target ID
BTDT10165
Target Name
Nicotinic acetylcholine receptor (nAChR) beta-4-alpha-3-beta-4-alpha-3-alpha-5
Target Bioclass
Receptor
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N.A.
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Alpha-conotoxin PeIA IC50
9.2 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.
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