Target Information

General Information of This Target
Target ID
BTDT00234
Target Name
Neuronal acetylcholine receptor subunit alpha-9 (CHRNA9);Neuronal acetylcholine receptor subunit alpha-10 (CHRNA10)
Target Bioclass
Transporter and channel
Uniprot ID
Q9UGM1 ; Q9GZZ6
3D Structure
Download
2D Sequence
3D Structure
Source
Predict by Alphafold2
?
Alphafold Parameters: msa_mode: mmseqs2_uniref_env model_type: auto num_recycles: auto
Gene Name
CHRNA9;CHRNA10
Gene ID
55584 ; 57053
Synonym 1
Nicotinic acetylcholine receptor subunit alpha-9
Synonym 2
Nicotinic acetylcholine receptor subunit alpha-10
Sequence 1
MNWSHSCISFCWIYFAASRLRAAETADGKYAQKLFNDLFEDYSNALRPVEDTDKVLNVTL
QITLSQIKDMDERNQILTAYLWIRQIWHDAYLTWDRDQYDGLDSIRIPSDLVWRPDIVLY
NKADDESSEPVNTNVVLRYDGLITWDAPAITKSSCVVDVTYFPFDNQQCNLTFGSWTYNG
NQVDIFNALDSGDLSDFIEDVEWEVHGMPAVKNVISYGCCSEPYPDVTFTLLLKRRSSFY
IVNLLIPCVLISFLAPLSFYLPAASGEKVSLGVTILLAMTVFQLMVAEIMPASENVPLIG
KYYIATMALITASTALTIMVMNIHFCGAEARPVPHWARVVILKYMSRVLFVYDVGESCLS
PHHSRERDHLTKVYSKLPESNLKAARNKDLSRKKDMNKRLKNDLGCQGKNPQEAESYCAQ
YKVLTRNIEYIAKCLKDHKATNSKGSEWKKVAKVIDRFFMWIFFIMVFVMTILIIARAD

    Click to Show/Hide
Sequence 2
MGLRSHHLSLGLLLLFLLPAECLGAEGRLALKLFRDLFANYTSALRPVADTDQTLNVTLE
VTLSQIIDMDERNQVLTLYLWIRQEWTDAYLRWDPNAYGGLDAIRIPSSLVWRPDIVLYN
KADAQPPGSASTNVVLRHDGAVRWDAPAITRSSCRVDVAAFPFDAQHCGLTFGSWTHGGH
QLDVRPRGAAASLADFVENVEWRVLGMPARRRVLTYGCCSEPYPDVTFTLLLRRRAAAYV
CNLLLPCVLISLLAPLAFHLPADSGEKVSLGVTVLLALTVFQLLLAESMPPAESVPLIGK
YYMATMTMVTFSTALTILIMNLHYCGPSVRPVPAWARALLLGHLARGLCVRERGEPCGQS
RPPELSPSPQSPEGGAGPPAGPCHEPRCLCRQEALLHHVATIANTFRSHRAAQRCHEDWK
RLARVMDRFFLAIFFSMALVMSLLVLVQAL

    Click to Show/Hide
Family1
the ligand-gated ion channel (TC 1.A.9) family
Family2
the ligand-gated ion channel (TC 1.A.9) family
Function 1
Ionotropic receptor with a probable role in the modulation of; auditory stimuli. Agonist binding induces a conformation change that; leads to the opening of an ion-conducting channel across the plasma; membraneThe channel is permeable; to a range of divalent cations including calcium, the influx of which; may activate a potassium current which hyperpolarizes the cell membrane;In the ear, this may lead to a; reduction in basilar membrane motion, altering the activity of auditory; nerve fibers and reducing the range of dynamic hearing. This may; protect against acoustic trauma. May also regulate keratinocyte; adhesion.

    Click to Show/Hide
Function 2
Ionotropic receptor with a probable role in the modulation of; auditory stimuli. Agonist binding may induce 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 permeable; to a range of divalent cations including calcium, the influx of which; may activate a potassium current which hyperpolarizes the cell; membrane. In the ear, this may lead to a reduction in basilar membrane; motion, altering the activity of auditory nerve fibers and reducing the; range of dynamic hearing. This may protect against acoustic trauma.

    Click to Show/Hide
Taxonomy ID
9606
TCDB ID
1.A.9.1.22 ; 1.A.9.1.22
        Click to Show/Hide the Complete Species Lineage
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    Alpha-conotoxin RgIA IC50
1.5 nM
 [1- 13]
References
Ref 1 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 2 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 3 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 4 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 5 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 6 -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 7 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 8 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 9 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 10 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 11 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 12 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 13 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.
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.