Target Information

General Information of This Target
Target ID
BTDT00083
Target Name
Neuronal acetylcholine receptor subunit alpha-7 (CHRNA7)
Target Bioclass
Transporter and channel
Uniprot ID
P36544
3D Structure
Download
2D Sequence
3D Structure
Source
Predict by Alphafold2
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Alphafold Parameters: msa_mode: mmseqs2_uniref_env model_type: auto num_recycles: auto
Gene Name
CHRNA7
Gene ID
1139 ; 89832
Synonym
NACHRA7
Sequence
MRCSPGGVWLALAASLLHVSLQGEFQRKLYKELVKNYNPLERPVANDSQPLTVYFSLSLL
QIMDVDEKNQVLTTNIWLQMSWTDHYLQWNVSEYPGVKTVRFPDGQIWKPDILLYNSADE
RFDATFHTNVLVNSSGHCQYLPPGIFKSSCYIDVRWFPFDVQHCKLKFGSWSYGGWSLDL
QMQEADISGYIPNGEWDLVGIPGKRSERFYECCKEPYPDVTFTVTMRRRTLYYGLNLLIP
CVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFAST
MIIVGLSVVVTVIVLQYHHHDPDGGKMPKWTRVILLNWCAWFLRMKRPGEDKVRPACQHK
QRRCSLASVEMSAVAPPPASNGNLLYIGFRGLDGVHCVPTPDSGVVCGRMACSPTHDEHL
LHGGQPPEGDPDLAKILEEVRYIANRFRCQDESEAVCSEWKFAACVVDRLCLMAFSVFTI
ICTIGILMSAPNFVEAVSKDFA

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Family
the ligand-gated ion channel (TC 1.A.9) family
Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.

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Taxonomy ID
9606
TCDB ID
1.A.9.1.7
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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    Turritoxin F21-2 Inhibition rate
55 %
 [3]
 Toxin Info    Alpha-conotoxin LsIA IC50
0.3 - 10.1 nM
 [4], [5]
 Toxin Info    Toxin BMLCL IC50
42 nM
 [6], [7], [8]
 Toxin Info    Conotoxin Czon1107 IC50
77.2 nM
 [9], [10]
 Toxin Info    Alpha-conotoxin RegIIA IC50
103 - 210 nM
 [11- 17]
 Toxin Info    Alpha-conotoxin FrXXA IC50
125 nM
 [18]
 Toxin Info    Alpha-conotoxin FrXXA 2 IC50
125 nM
 [18]
 Toxin Info    Haditoxin IC50
180 nM
 [19], [20], [21]
 Toxin Info    Alpha-conotoxin GeXXA IC50
210 nM
 [22], [23]
 Toxin Info    Alpha-conotoxin OmIA IC50
290 nM
 [16- 26]
 Toxin Info    Conorfamide-As2 IC50
0.689 - 3.867 μM
 [27]
 Toxin Info    Conorfamide-As1 IC50
0.737 - 4.984 μM
 [27]
 Toxin Info    Alpha-conotoxin RgIA IC50
1.8 μM
 [28- 40]
 Toxin Info    Conorfamide-As1 IC50
2.029 - 8.464 μM
 [27]
 Toxin Info    Acidic phospholipase A2 CM-II IC50
3.2 μM
 [41], [42], [43], [44]
 Toxin Info    Basic phospholipase A2 vurtoxin IC50
14 μM
 [45], [44]
 Toxin Info    Conorfamide-As2 IC50
20.971 - 70.036 μM
 [27]
 Toxin Info    Azemiopsin IC50
22 μM
 [46]
 Toxin Info    Acidic phospholipase A2 Vur-PL2B IC50
29 μM
 [45], [44]
 Toxin Info    Conotoxin ArchIIIA IC50
45.7 μM
 [47]
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 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.
Ref 4 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 5 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 6 cDNA sequence analysis of a novel member of the three loop protein family from the Chinese continental banded krait. Biosci Biotechnol Biochem. 1999 May;63(5):940-2. doi: 10.1271/bbb.63.940.
Ref 7 Muscarinic toxin-like proteins from Taiwan banded krait (Bungarus multicinctus) venom: purification, characterization and gene organization. Biol Chem. 2002 Sep;383(9):1397-406. doi: 10.1515/BC.2002.158.
Ref 8 Nonconventional three-finger toxin BMLCL from krait Bungarus multicinctus venom with high affinity interacts with nicotinic acetylcholine receptors. Dokl Biochem Biophys. 2015;464:294-7. doi: 10.1134/S1607672915050099. Epub 2015 Oct 31.
Ref 9 Structure and allosteric activity of a single-disulfide conopeptide from Conus zonatus at human 34 and 7 nicotinic acetylcholine receptors. J Biol Chem. 2020 May 15;295(20):7096-7112. doi: 10.1074/jbc.RA119.012098. Epub 2020 Mar 31.
Ref 10 Single-Disulfide Conopeptide Czon1107, an Allosteric Antagonist of the Human 34 Nicotinic Acetylcholine Receptor. Mar Drugs. 2022 Jul 31;20(8):497. doi: 10.3390/md20080497.
Ref 11 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 12 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 13 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 14 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 15 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 16 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 17 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 18 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 19 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 20 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 21 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 22 Conotoxin D-GeXXA utilizes a novel strategy to antagonize nicotinic acetylcholine receptors. Sci Rep. 2015 Sep 23;5:14261. doi: 10.1038/srep14261.
Ref 23 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 24 Alpha-conotoxin OmIA is a potent ligand for the acetylcholine-binding protein as well as alpha3beta2 and alpha7 nicotinic acetylcholine receptors. J Biol Chem. 2006 Aug 25;281(34):24678-86. doi: 10.1074/jbc.M602969200. Epub 2006 Jun 27.
Ref 25 Unique Pharmacological Properties of -Conotoxin OmIA at 7 nAChRs. Front Pharmacol. 2021 Dec 8;12:803397. doi: 10.3389/fphar.2021.803397. eCollection 2021.
Ref 26 Solution conformation of a neuronal nicotinic acetylcholine receptor antagonist alpha-conotoxin OmIA that discriminates alpha3 vs. alpha6 nAChR subtypes. Biochem Biophys Res Commun. 2006 Jun 23;345(1):248-54. doi: 10.1016/j.bbrc.2006.04.099. Epub 2006 Apr 27.
Ref 27 Novel conorfamides from Conus austini venom modulate both nicotinic acetylcholine receptors and acid-sensing ion channels. Biochem Pharmacol. 2019 Jun;164:342-348. doi: 10.1016/j.bcp.2019.04.025. Epub 2019 Apr 24.
Ref 28 Alpha-RgIA: a novel conotoxin that specifically and potently blocks the alpha9alpha10 nAChR. Biochemistry. 2006 Feb 7;45(5):1511-7. doi: 10.1021/bi0520129.
Ref 29 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 30 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 31 Effects of cyclization on stability, structure, and activity of -conotoxin RgIA at the 910 nicotinic acetylcholine receptor and GABA(B) receptor. J Med Chem. 2011 Oct 13;54(19):6984-92. doi: 10.1021/jm201060r. Epub 2011 Sep 15.
Ref 32 Molecular basis for the differential sensitivity of rat and human 910 nAChRs to -conotoxin RgIA. J Neurochem. 2012 Sep;122(6):1137-44. doi: 10.1111/j.1471-4159.2012.07867.x. Epub 2012 Aug 3.
Ref 33 -conotoxin RgIA protects against the development of nerve injury-induced chronic pain and prevents both neuronal and glial derangement. Pain. 2014 Oct;155(10):1986-95. doi: 10.1016/j.pain.2014.06.023. Epub 2014 Jul 5.
Ref 34 Molecular interaction of -conotoxin RgIA with the rat 910 nicotinic acetylcholine receptor. Mol Pharmacol. 2015 May;87(5):855-64. doi: 10.1124/mol.114.096511. Epub 2015 Mar 4.
Ref 35 Corrections to "Molecular interaction of -conotoxin RgIA with the rat 910 nicotinic acetylcholine receptor". Mol Pharmacol. 2016 Oct;90(4):415-7. doi: 10.1124/mol.114.096511err.
Ref 36 Inhibition of 910 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain. Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):E1825-E1832. doi: 10.1073/pnas.1621433114. Epub 2017 Feb 21.
Ref 37 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 38 The three-dimensional structure of the analgesic alpha-conotoxin, RgIA. FEBS Lett. 2008 Mar 5;582(5):597-602. doi: 10.1016/j.febslet.2008.01.027. Epub 2008 Jan 31.
Ref 39 Alpha-RgIA, a novel conotoxin that blocks the alpha9alpha10 nAChR: structure and identification of key receptor-binding residues. J Mol Biol. 2008 Apr 4;377(4):1216-27. doi: 10.1016/j.jmb.2008.01.082. Epub 2008 Feb 4.
Ref 40 Dicarba analogues of -conotoxin RgIA. Structure, stability, and activity at potential pain targets. J Med Chem. 2014 Dec 11;57(23):9933-44. doi: 10.1021/jm501126u. Epub 2014 Dec 1.
Ref 41 Regional and accelerated molecular evolution in group I snake venom gland phospholipase A2 isozymes. Toxicon. 2000 Mar;38(3):449-62. doi: 10.1016/s0041-0101(99)00165-8.
Ref 42 Purification, some properties and amino-acid sequences of two phospholipases A (CM-II and CM-III) from Naja naja kaouthia venom. Eur J Biochem. 1980 Dec;112(3):493-9. doi: 10.1111/j.1432-1033.1980.tb06112.x.
Ref 43 A new type of thrombin inhibitor, noncytotoxic phospholipase A2, from the Naja haje cobra venom. Toxicon. 2010 Feb-Mar;55(2-3):186-94. doi: 10.1016/j.toxicon.2009.07.011. Epub 2009 Jul 19.
Ref 44 Inhibition of nicotinic acetylcholine receptors, a novel facet in the pleiotropic activities of snake venom phospholipases A2. PLoS One. 2014 Dec 18;9(12):e115428. doi: 10.1371/journal.pone.0115428. eCollection 2014.
Ref 45 cDNA cloning, structural, and functional analyses of venom phospholipases A? and a Kunitz-type protease inhibitor from steppe viper Vipera ursinii renardi. Toxicon. 2011 Feb;57(2):332-41. doi: 10.1016/j.toxicon.2010.12.012. Epub 2010 Dec 23.
Ref 46 Azemiopsin from Azemiops feae viper venom, a novel polypeptide ligand of nicotinic acetylcholine receptor. J Biol Chem. 2012 Aug 3;287(32):27079-86. doi: 10.1074/jbc.M112.363051. Epub 2012 May 21.
Ref 47 A short framework-III (mini-M-2) conotoxin from the venom of a vermivorous species, Conus archon, inhibits human neuronal nicotinic acetylcholine receptors. Peptides. 2022 Jul;153:170785. doi: 10.1016/j.peptides.2022.170785. Epub 2022 Mar 17.
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