General Information of This Target
Target ID
BTDT10092
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-1-beta-1-delta-epsilon
Target Bioclass
Receptor
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N.A.
Species: Mammalian
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Alpha-conotoxin GI IC50
5.86 - 995 nM
[1- 18]
 Toxin Info    Conotoxin MIIIJ IC50
3 - 45 μM
[19]
References
Ref 1 Evolution of separate predation- and defence-evoked venoms in carnivorous cone snails. Nat Commun. 2014 Mar 24;5:3521. doi: 10.1038/ncomms4521.
Ref 2 Peptide toxins from Conus geographus venom. J Biol Chem. 1981 May 25;256(10):4734-40.
Ref 3 Primary and secondary structure of conotoxin GI, a neurotoxic tridecapeptide from a marine snail. FEBS Lett. 1982 Nov 8;148(2):260-2. doi: 10.1016/0014-5793(82)80820-x.
Ref 4 Conotoxin GI: disulfide bridges, synthesis, and preparation of iodinated derivatives. Biochemistry. 1984 Jun 5;23(12):2796-802. doi: 10.1021/bi00307a040.
Ref 5 The alpha-conotoxins GI and MI distinguish between the nicotinic acetylcholine receptor agonist sites while SI does not. Biochemistry. 1994 Nov 29;33(47):14058-63. doi: 10.1021/bi00251a014.
Ref 6 alpha-Conotoxins selectively inhibit one of the two acetylcholine binding sites of nicotinic receptors. Mol Pharmacol. 1995 Jul;48(1):105-11.
Ref 7 Determinants involved in the affinity of alpha-conotoxins GI and SI for the muscle subtype of nicotinic acetylcholine receptors. Biochemistry. 1997 May 27;36(21):6469-74. doi: 10.1021/bi970195w.
Ref 8 Role of hydroxyprolines in the in vitro oxidative folding and biological activity of conotoxins. Biochemistry. 2008 Feb 12;47(6):1741-51. doi: 10.1021/bi701934m. Epub 2008 Jan 12.
Ref 9 Modulation of conotoxin structure and function is achieved through a multienzyme complex in the venom glands of cone snails. J Biol Chem. 2012 Oct 5;287(41):34288-303. doi: 10.1074/jbc.M112.366781. Epub 2012 Aug 13.
Ref 10 Alanine-Scanning Mutagenesis of -Conotoxin GI Reveals the Residues Crucial for Activity at the Muscle Acetylcholine Receptor. Mar Drugs. 2018 Dec 13;16(12):507. doi: 10.3390/md16120507.
Ref 11 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 12 Cysteine-Rich -Conotoxin SII Displays Novel Interactions at the Muscle Nicotinic Acetylcholine Receptor. ACS Chem Neurosci. 2022 Apr 20;13(8):1245-1250. doi: 10.1021/acschemneuro.1c00857. Epub 2022 Mar 31.
Ref 13 Three-dimensional structure of the alpha-conotoxin GI at 1.2 A resolution. Biochemistry. 1996 Sep 3;35(35):11329-35. doi: 10.1021/bi960820h.
Ref 14 Solution conformation of conotoxin GI determined by 1H nuclear magnetic resonance spectroscopy and distance geometry calculations. Biochemistry. 1989 May 30;28(11):4853-60. doi: 10.1021/bi00437a050.
Ref 15 Solution structures of alpha-conotoxin G1 determined by two-dimensional NMR spectroscopy. Biochemistry. 1989 Jun 27;28(13):5494-501. doi: 10.1021/bi00439a026.
Ref 16 Two distinct structures of alpha-conotoxin GI in aqueous solution. Eur J Biochem. 1998 Jun 1;254(2):238-47. doi: 10.1046/j.1432-1327.1998.2540238.x.
Ref 17 Structure determination of the three disulfide bond isomers of alpha-conotoxin GI: a model for the role of disulfide bonds in structural stability. J Mol Biol. 1998 May 1;278(2):401-15. doi: 10.1006/jmbi.1998.1701.
Ref 18 NMR solution conformation of an antitoxic analogue of alpha-conotoxin GI: identification of a common nicotinic acetylcholine receptor alpha 1-subunit binding surface for small ligands and alpha-conotoxins. Biochemistry. 1999 Sep 14;38(37):11895-904. doi: 10.1021/bi990558n.
Ref 19 M-Conotoxin MIIIJ Blocks Nicotinic Acetylcholine Receptors at Neuromuscular Junctions of Frog and Fish. Toxins (Basel). 2020 Mar 21;12(3):197. doi: 10.3390/toxins12030197.
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