General Information of This Target
Target ID
BTDT10133
Target Name
Nicotinic acetylcholine receptor (nAChR) alpha-4-beta-2
Target Bioclass
Receptor
        Click to Show/Hide the Complete Species Lineage
N.A.
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Elevenin-Vc1 Effect . [1], [2], [3]
 Toxin Info    Alpha-conotoxin Pu14.1 Inhibition rate . [4]
 Toxin Info    Alpha-conotoxin TxIA Inhibition rate . [5], [6]
 Toxin Info    Alpha-conotoxin CIB Inhibition rate . [7], [8]
 Toxin Info    Alpha-conotoxin Lt28.1 Inhibition rate
18 %
[9]
 Toxin Info    Alpha-conotoxin GID IC50
128.6 - 390 nM
[10- 15]
 Toxin Info    Alpha-conotoxin MilIA IC50
>10 μM
[16]
 Toxin Info    Alpha-conotoxin Vc1a IC50
>30 μM
[17- 33]
 Toxin Info    Three-finger toxin 3b IC50
1.8 μM
[34]
 Toxin Info    Fulditoxin IC50
1.8 μM
[34], [35], [36]
References
Ref 1 Diversity of conotoxin gene superfamilies in the venomous snail, Conus victoriae. PLoS One. 2014 Feb 5;9(2):e87648. doi: 10.1371/journal.pone.0087648. eCollection 2014.
Ref 2 Hormone-like peptides in the venoms of marine cone snails. Gen Comp Endocrinol. 2017 Apr 1;244:11-18. doi: 10.1016/j.ygcen.2015.07.012. Epub 2015 Aug 22.
Ref 3 Characterisation of Elevenin-Vc1 from the Venom of Conus victoriae: A Structural Analogue of -Conotoxins. Mar Drugs. 2023 Jan 25;21(2):81. doi: 10.3390/md21020081.
Ref 4 A new subfamily of conotoxins belonging to the A-superfamily. Peptides. 2010 Nov;31(11):2009-16. doi: 10.1016/j.peptides.2010.07.011. Epub 2010 Aug 4.
Ref 5 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 6 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 7 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 8 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 9 Cloning, expression and functional characterization of a D-superfamily conotoxin Lt28.1 with previously undescribed cysteine pattern. Peptides. 2017 Aug;94:64-70. doi: 10.1016/j.peptides.2017.06.008. Epub 2017 Jun 27.
Ref 10 Evolution of separate predation- and defence-evoked venoms in carnivorous cone snails. Nat Commun. 2014 Mar 24;5:3521. doi: 10.1038/ncomms4521.
Ref 11 Isolation, structure, and activity of GID, a novel alpha 4/7-conotoxin with an extended N-terminal sequence. J Biol Chem. 2003 Jan 31;278(5):3137-44. doi: 10.1074/jbc.M210280200. Epub 2002 Nov 4.
Ref 12 Beta2 subunit contribution to 4/7 alpha-conotoxin binding to the nicotinic acetylcholine receptor. J Biol Chem. 2005 Aug 26;280(34):30460-8. doi: 10.1074/jbc.M504229200. Epub 2005 Jun 1.
Ref 13 Inhibition of neuronal nicotinic acetylcholine receptor subtypes by alpha-Conotoxin GID and analogues. J Biol Chem. 2009 Feb 20;284(8):4944-51. doi: 10.1074/jbc.M804950200. Epub 2008 Dec 19.
Ref 14 Design and synthesis of -conotoxin GID analogues as selective 42 nicotinic acetylcholine receptor antagonists. Biopolymers. 2014 Jan;102(1):78-87. doi: 10.1002/bip.22413.
Ref 15 Discovery of peptide ligands through docking and virtual screening at nicotinic acetylcholine receptor homology models. Proc Natl Acad Sci U S A. 2017 Sep 19;114(38):E8100-E8109. doi: 10.1073/pnas.1703952114. Epub 2017 Sep 5.
Ref 16 Structure-Function Elucidation of a New -Conotoxin, MilIA, from Conus milneedwardsi. Mar Drugs. 2019 Sep 16;17(9):535. doi: 10.3390/md17090535.
Ref 17 A novel alpha-conotoxin identified by gene sequencing is active in suppressing the vascular response to selective stimulation of sensory nerves in vivo. Biochemistry. 2003 Jun 10;42(22):6904-11. doi: 10.1021/bi034043e.
Ref 18 Determining sequences and post-translational modifications of novel conotoxins in Conus victoriae using cDNA sequencing and mass spectrometry. J Mass Spectrom. 2004 May;39(5):548-57. doi: 10.1002/jms.624.
Ref 19 A conus peptide blocks nicotinic receptors of unmyelinated axons in human nerves. Neuroreport. 2005 Apr 4;16(5):479-83. doi: 10.1097/00001756-200504040-00012.
Ref 20 Molecular mechanism for analgesia involving specific antagonism of alpha9alpha10 nicotinic acetylcholine receptors. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17880-4. doi: 10.1073/pnas.0608715103. Epub 2006 Nov 13.
Ref 21 Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?. Mol Pharmacol. 2007 Dec;72(6):1406-10. doi: 10.1124/mol.107.040568. Epub 2007 Sep 5.
Ref 22 Analgesic alpha-conotoxins Vc1.1 and Rg1A inhibit N-type calcium channels in rat sensory neurons via GABAB receptor activation. J Neurosci. 2008 Oct 22;28(43):10943-51. doi: 10.1523/JNEUROSCI.3594-08.2008.
Ref 23 Scanning mutagenesis of alpha-conotoxin Vc1.1 reveals residues crucial for activity at the alpha9alpha10 nicotinic acetylcholine receptor. J Biol Chem. 2009 Jul 24;284(30):20275-84. doi: 10.1074/jbc.M109.015339. Epub 2009 May 15.
Ref 24 Determination of the -conotoxin Vc1.1 binding site on the 910 nicotinic acetylcholine receptor. J Med Chem. 2013 May 9;56(9):3557-67. doi: 10.1021/jm400041h. Epub 2013 Apr 29.
Ref 25 Structure-Activity Studies of Cysteine-Rich -Conotoxins that Inhibit High-Voltage-Activated Calcium Channels via GABA(B) Receptor Activation Reveal a Minimal Functional Motif. Angew Chem Int Ed Engl. 2016 Apr 4;55(15):4692-6. doi: 10.1002/anie.201600297. Epub 2016 Mar 7.
Ref 26 Cyclic analogues of -conotoxin Vc1.1 inhibit colonic nociceptors and provide analgesia in a mouse model of chronic abdominal pain. Br J Pharmacol. 2018 Jun;175(12):2384-2398. doi: 10.1111/bph.14115. Epub 2018 Feb 13.
Ref 27 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 28 The synthesis, structural characterization, and receptor specificity of the alpha-conotoxin Vc1.1. J Biol Chem. 2006 Aug 11;281(32):23254-63. doi: 10.1074/jbc.M604550200. Epub 2006 Jun 5.
Ref 29 The engineering of an orally active conotoxin for the treatment of neuropathic pain. Angew Chem Int Ed Engl. 2010 Sep 3;49(37):6545-8. doi: 10.1002/anie.201000620.
Ref 30 Dicarba -conotoxin Vc1.1 analogues with differential selectivity for nicotinic acetylcholine and GABAB receptors. ACS Chem Biol. 2013 Aug 16;8(8):1815-21. doi: 10.1021/cb4002393. Epub 2013 Jun 17.
Ref 31 Racemic and quasi-racemic X-ray structures of cyclic disulfide-rich peptide drug scaffolds. Angew Chem Int Ed Engl. 2014 Oct 13;53(42):11236-41. doi: 10.1002/anie.201406563. Epub 2014 Aug 28.
Ref 32 Less is More: Design of a Highly Stable Disulfide-Deleted Mutant of Analgesic Cyclic -Conotoxin Vc1.1. Sci Rep. 2015 Aug 20;5:13264. doi: 10.1038/srep13264.
Ref 33 Structure-Activity Studies Reveal the Molecular Basis for GABA(B)-Receptor Mediated Inhibition of High Voltage-Activated Calcium Channels by -Conotoxin Vc1.1. ACS Chem Biol. 2018 Jun 15;13(6):1577-1587. doi: 10.1021/acschembio.8b00190. Epub 2018 May 25.
Ref 34 The venom-gland transcriptome of the eastern coral snake (Micrurus fulvius) reveals high venom complexity in the intragenomic evolution of venoms. BMC Genomics. 2013 Aug 2;14:531. doi: 10.1186/1471-2164-14-531.
Ref 35 Post-transcriptional Mechanisms Contribute Little to Phenotypic Variation in Snake Venoms. G3 (Bethesda). 2015 Sep 9;5(11):2375-82. doi: 10.1534/g3.115.020578.
Ref 36 Fulditoxin, representing a new class of dimeric snake toxins, defines novel pharmacology at nicotinic ACh receptors. Br J Pharmacol. 2020 Apr;177(8):1822-1840. doi: 10.1111/bph.14954. Epub 2020 Feb 9.
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.