General Information of This Target
Target ID
BTDT10120
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-3-beta-2
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    Elevenin Effect . [1]
 Toxin Info    Elevenin Effect . [2]
 Toxin Info    Conotoxin Bt1.8 IC50
8.8 nM
[3]
 Toxin Info    Alpha-conotoxin LvIA IC50
17.5 nM
[4], [5], [6], [7]
 Toxin Info    Alpha-conotoxin G1.5 IC50
35.7 nM
[8], [9]
 Toxin Info    Alpha-conotoxin RegIIA IC50
132.4 - 704.1 nM
[10- 16]
 Toxin Info    Alpha-conotoxin Mr1.1 IC50
218.9 nM
[17], [18], [19]
 Toxin Info    Alpha-conotoxin FrXXA IC50
282 nM
[20]
 Toxin Info    Alpha-conotoxin FrXXA 2 IC50
282 nM
[20]
 Toxin Info    Haditoxin IC50
500 nM
[21], [22], [23]
 Toxin Info    Turritoxin F21-2 IC50
566.2 nM
[24]
References
Ref 1 A Combined Transcriptomics and Proteomics Approach Reveals the Differences in the Predatory and Defensive Venoms of the Molluscivorous Cone Snail Cylinder ammiralis (Caenogastropoda: Conidae). Toxins (Basel). 2021 Sep 10;13(9):642. doi: 10.3390/toxins13090642.
Ref 2 Comparative Venomics of the Cryptic Cone Snail Species Virroconus ebraeus and Virroconus judaeus. Mar Drugs. 2022 Feb 17;20(2):149. doi: 10.3390/md20020149.
Ref 3 -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 4 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 5 Recombinant Expression and Characterization of -Conotoxin LvIA in Escherichia coli. Mar Drugs. 2016 Jan 5;14(1):11. doi: 10.3390/md14010011.
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 Evolution of separate predation- and defence-evoked venoms in carnivorous cone snails. Nat Commun. 2014 Mar 24;5:3521. doi: 10.1038/ncomms4521.
Ref 9 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 10 RegIIA: an 4/7-conotoxin from the venom of Conus regius that potently blocks 34 nAChRs. Biochem Pharmacol. 2012 Feb 1;83(3):419-26. doi: 10.1016/j.bcp.2011.11.006. Epub 2011 Nov 16.
Ref 11 Hyperhydroxylation: a new strategy for neuronal targeting by venomous marine molluscs. Prog Mol Subcell Biol. 2006;43:83-103. doi: 10.1007/978-3-540-30880-5_4.
Ref 12 Alanine scan of -conotoxin RegIIA reveals a selective 34 nicotinic acetylcholine receptor antagonist. J Biol Chem. 2015 Jan 9;290(2):1039-48. doi: 10.1074/jbc.M114.605592. Epub 2014 Nov 19.
Ref 13 Molecular Basis for Differential Sensitivity of -Conotoxin RegIIA at Rat and Human Neuronal Nicotinic Acetylcholine Receptors. Mol Pharmacol. 2015 Dec;88(6):993-1001. doi: 10.1124/mol.115.100503. Epub 2015 Oct 5.
Ref 14 Key Structural Determinants in the Agonist Binding Loops of Human 2 and 4 Nicotinic Acetylcholine Receptor Subunits Contribute to 34 Subtype Selectivity of -Conotoxins. J Biol Chem. 2016 Nov 4;291(45):23779-23792. doi: 10.1074/jbc.M116.730804. Epub 2016 Sep 19.
Ref 15 Species specificity of rat and human 7 nicotinic acetylcholine receptors towards different classes of peptide and protein antagonists. Neuropharmacology. 2018 Sep 1;139:226-237. doi: 10.1016/j.neuropharm.2018.07.019. Epub 2018 Jul 17.
Ref 16 Rational Design of -Conotoxin RegIIA Analogues Selectively Inhibiting the Human 32 Nicotinic Acetylcholine Receptor through Computational Scanning. ACS Chem Neurosci. 2020 Sep 16;11(18):2804-2811. doi: 10.1021/acschemneuro.0c00293. Epub 2020 Sep 3.
Ref 17 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 18 Chemical synthesis and characterization of two 4/7-conotoxins. Acta Biochim Biophys Sin (Shanghai). 2010 Oct;42(10):745-53. doi: 10.1093/abbs/gmq074. Epub 2010 Aug 27.
Ref 19 Mechanism of Action and Structure-Activity Relationship of -Conotoxin Mr1.1 at the Human 910 Nicotinic Acetylcholine Receptor. J Med Chem. 2022 Dec 22;65(24):16204-16217. doi: 10.1021/acs.jmedchem.2c00494. Epub 2022 Sep 22.
Ref 20 A Novel Dimeric Conotoxin, FrXXA, from the Vermivorous Cone Snail Conus fergusoni, of the Eastern Pacific, Inhibits Nicotinic Acetylcholine Receptors. Toxins (Basel). 2022 Jul 26;14(8):510. doi: 10.3390/toxins14080510.
Ref 21 Beta-cardiotoxin: a new three-finger toxin from Ophiophagus hannah (king cobra) venom with beta-blocker activity. FASEB J. 2007 Nov;21(13):3685-95. doi: 10.1096/fj.07-8658com. Epub 2007 Jul 6.
Ref 22 The king cobra genome reveals dynamic gene evolution and adaptation in the snake venom system. Proc Natl Acad Sci U S A. 2013 Dec 17;110(51):20651-6. doi: 10.1073/pnas.1314702110. Epub 2013 Dec 2.
Ref 23 Structural and functional characterization of a novel homodimeric three-finger neurotoxin from the venom of Ophiophagus hannah (king cobra). J Biol Chem. 2010 Mar 12;285(11):8302-15. doi: 10.1074/jbc.M109.074161. Epub 2010 Jan 13.
Ref 24 A turripeptide from Polystira nobilis venom inhibits human 32 and 7 nicotinic acetylcholine receptors. Insect Biochem Mol Biol. 2020 Sep;124:103416. doi: 10.1016/j.ibmb.2020.103416. Epub 2020 Jun 24.
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