Target Information

General Information of This Target
Target ID
BTDT10122
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-3-beta-2
Target Bioclass
Receptor
Taxonomy ID
10116
        Click to Show/Hide the Complete Species Lineage
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    Alpha-conotoxin Mr1.1 Inhibition rate
50 - 70 %
 [1], [2], [3]
 Toxin Info    Alpha-conotoxin-like Qc1.2 Inhibition rate
63 %
 [1- 5]
 Toxin Info    Alpha-conotoxin AnIB IC50
0.2 nM
 [6], [7]
 Toxin Info    Alpha-conotoxin AnIB IC50
0.3 nM
 [6], [7]
 Toxin Info    Alpha-conotoxin TxIA IC50
3.5 nM
 [8], [9]
 Toxin Info    Alpha-conotoxin LvIA IC50
8.67 nM
 [10], [11], [12], [13]
 Toxin Info    Conotoxin Bt1.8 IC50
9.4 nM
 [14]
 Toxin Info    Alpha-conotoxin Lt1a IC50
9.8 - 22.95 nM
 [15], [16], [17]
 Toxin Info    Alpha-conotoxin LsIA IC50
10.3 nM
 [18], [19]
 Toxin Info    Alpha-conotoxin RegIIA IC50
10.7 - 33 nM
 [20- 26]
 Toxin Info    Alpha-conotoxin QcIA IC50
55.7 nM
 [4- 27]
 Toxin Info    Alpha-conotoxin CIB IC50
128.9 nM
 [28], [29]
 Toxin Info    Alpha-conotoxin GeXXA IC50
498 nM
 [4- 30]
 Toxin Info    Alpha-conotoxin Vt1.27 IC50
1.16 μM
 [31]
 Toxin Info    Alpha-conotoxin CIA IC50
2.06 μM
 [28], [29]
 Toxin Info    Neurotoxin Oh9-1 IC50
50.2 μM
 [32], [33]
References
Ref 1 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 2 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 3 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 4 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 5 Characterization of a novel alpha4/4-conotoxin, Qc1.2, from vermivorous Conus quercinus. Acta Biochim Biophys Sin (Shanghai). 2009 Oct;41(10):858-64. doi: 10.1093/abbs/gmp077.
Ref 6 Chemical and functional identification and characterization of novel sulfated alpha-conotoxins from the cone snail Conus anemone. J Med Chem. 2004 Feb 26;47(5):1234-41. doi: 10.1021/jm031010o.
Ref 7 Posttranslational modifications of -conotoxins: sulfotyrosine and C-terminal amidation stabilise structures and increase acetylcholine receptor binding. RSC Med Chem. 2021 Jul 26;12(9):1574-1584. doi: 10.1039/d1md00182e. eCollection 2021 Sep 23.
Ref 8 AChBP-targeted alpha-conotoxin correlates distinct binding orientations with nAChR subtype selectivity. EMBO J. 2007 Aug 22;26(16):3858-67. doi: 10.1038/sj.emboj.7601785. Epub 2007 Jul 26.
Ref 9 Secretion and maturation of conotoxins in the venom ducts of Conus textile. Toxicon. 2012 Dec 15;60(8):1370-9. doi: 10.1016/j.toxicon.2012.09.013. Epub 2012 Sep 29.
Ref 10 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 11 Recombinant Expression and Characterization of -Conotoxin LvIA in Escherichia coli. Mar Drugs. 2016 Jan 5;14(1):11. doi: 10.3390/md14010011.
Ref 12 -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 13 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 14 -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 15 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 16 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 17 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 18 Isolation and characterization of -conotoxin LsIA with potent activity at nicotinic acetylcholine receptors. Biochem Pharmacol. 2013 Sep 15;86(6):791-9. doi: 10.1016/j.bcp.2013.07.016. Epub 2013 Aug 4.
Ref 19 Rigidity of loop 1 contributes to equipotency of globular and ribbon isomers of -conotoxin AusIA. Sci Rep. 2021 Nov 9;11(1):21928. doi: 10.1038/s41598-021-01277-4.
Ref 20 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 21 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 22 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 23 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 24 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 25 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 26 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 27 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 28 Evolution of Conus peptide genes: duplication and positive selection in the A-superfamily. J Mol Evol. 2010 Feb;70(2):190-202. doi: 10.1007/s00239-010-9321-7. Epub 2010 Feb 9.
Ref 29 Synthesis, Structure and Biological Activity of CIA and CIB, Two -Conotoxins from the Predation-Evoked Venom of Conus catus. Toxins (Basel). 2018 Jun 1;10(6):222. doi: 10.3390/toxins10060222.
Ref 30 Conotoxin D-GeXXA utilizes a novel strategy to antagonize nicotinic acetylcholine receptors. Sci Rep. 2015 Sep 23;5:14261. doi: 10.1038/srep14261.
Ref 31 A 4/8 Subtype -Conotoxin Vt1.27 Inhibits N-Type Calcium Channels With Potent Anti-Allodynic Effect. Front Pharmacol. 2022 Apr 29;13:881732. doi: 10.3389/fphar.2022.881732. eCollection 2022.
Ref 32 Purification and characterization of a neurotoxin from the venom of Ophiophagus hannah (king cobra). Biochem Biophys Res Commun. 2002 Jun 14;294(3):574-8. doi: 10.1016/S0006-291X(02)00518-1.
Ref 33 A Distinct Functional Site in -Neurotoxins: Novel Antagonists of Nicotinic Acetylcholine Receptors from Snake Venom. ACS Chem Biol. 2015 Dec 18;10(12):2805-15. doi: 10.1021/acschembio.5b00492. Epub 2015 Oct 15.
Data Quality & Feedback

Help us maintain data quality by reporting any errors or inaccuracies you may find.

samedaypayday.com visits since 2024

If you find any error in data or bug in web service, please kindly report it to biodb_contact@163.com et al.