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nicotinic acetylcholine receptor α10 subunit

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Target not currently curated in GtoImmuPdb

Target id: 470

Nomenclature: nicotinic acetylcholine receptor α10 subunit

Family: Nicotinic acetylcholine receptors (nACh)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 450 11p15.4 CHRNA10 cholinergic receptor nicotinic alpha 10 subunit 2
Mouse 4 447 7 E3 Chrna10 cholinergic receptor, nicotinic, alpha polypeptide 10
Rat 4 447 1q32 Chrna10 cholinergic receptor nicotinic alpha 10 subunit 1
Previous and Unofficial Names Click here for help
NACHR alpha 10 | nicotinic acetylcholine receptor subunit alpha 10 | cholinergic receptor, nicotinic, alpha 10 (neuronal) | cholinergic receptor, nicotinic alpha 10 | cholinergic receptor
Database Links Click here for help
Alphafold Q9GZZ6 (Hs), Q9JLB5 (Rn)
CATH/Gene3D 2.70.170.10
ChEMBL Target CHEMBL2109238 (Hs), CHEMBL3461 (Rn)
DrugBank Target Q9GZZ6 (Hs)
Ensembl Gene ENSG00000129749 (Hs), ENSMUSG00000066279 (Mm), ENSRNOG00000020293 (Rn)
Entrez Gene 57053 (Hs), 504186 (Mm), 64574 (Rn)
Human Protein Atlas ENSG00000129749 (Hs)
KEGG Gene hsa:57053 (Hs), mmu:504186 (Mm), rno:64574 (Rn)
OMIM 606372 (Hs)
Pharos Q9GZZ6 (Hs)
RefSeq Nucleotide NM_020402 (Hs), NM_001081424 (Mm), NM_022639 (Rn)
RefSeq Protein NP_065135 (Hs), NP_001074893 (Mm), NP_072161 (Rn)
UniProtKB Q9GZZ6 (Hs), Q9JLB5 (Rn)
Wikipedia CHRNA10 (Hs)
Functional Characteristics Click here for help
α9α10: PCa/PNa = 9, Pf = 22%
Natural/Endogenous Ligands Click here for help
acetylcholine
Commonly used antagonists
α9α10: α-bungarotoxin > tropisetron = strychnine > tubocurarine

Download all structure-activity data for this target as a CSV file go icon to follow link

Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]methyllycaconitine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 8.1 pKd
⤷ pKd 8.1 (Kd 7.5x10-9 M) α9α10
RgIA4 Peptide Click here for species-specific activity table Rn Antagonist 9.1 pIC50 3
⤷ pIC50 9.1 (IC50 9x10-10 M) α9α10 [3]
RgIA4 Peptide Click here for species-specific activity table Hs Antagonist 8.8 pIC50 3
⤷ pIC50 8.8 (IC50 1.5x10-9 M) α9α10 [3]
strychnine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
⤷ α9α10
nicotine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
⤷ α9α10
α-bungarotoxin Peptide Click here for species-specific activity table Hs Antagonist - -
⤷ α9α10
muscarine Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
⤷ α9α10
α-conotoxin RgIA Peptide Click here for species-specific activity table Hs Antagonist - -
⤷ α9α10
View species-specific antagonist tables
Tissue Distribution Click here for help
Pituitary gland, keratinocytes
Species:  Human
Technique:  RT-PCR
References:  4
Pituitary gland (pars tuberalis region), cochlear, vestibular hair cells
Species:  Rat
Technique:  In situ hybridisation, RT-PCR
References:  1,4
Physiological Consequences of Altering Gene Expression Click here for help
Knockout mice have abnormal innervation, synaptic function and morphology of the cochlear.
Species:  Mouse
Tissue:  in vivo
Technique:  Knockout
References:  5

References

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1. Elgoyhen AB, Vetter DE, Katz E, Rothlin CV, Heinemann SF, Boulter J. (2001) alpha10: a determinant of nicotinic cholinergic receptor function in mammalian vestibular and cochlear mechanosensory hair cells. Proc Natl Acad Sci USA, 98 (6): 3501-6. [PMID:11248107]

2. Lustig LR, Peng H, Hiel H, Yamamoto T, Fuchs PA. (2001) Molecular cloning and mapping of the human nicotinic acetylcholine receptor alpha10 (CHRNA10). Genomics, 73 (3): 272-83. [PMID:11350119]

3. Romero HK, Christensen SB, Di Cesare Mannelli L, Gajewiak J, Ramachandra R, Elmslie KS, Vetter DE, Ghelardini C, Iadonato SP, Mercado JL et al.. (2017) Inhibition of α9α10 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain. Proc Natl Acad Sci USA, 114 (10): E1825-E1832. [PMID:28223528]

4. Sgard F, Charpantier E, Bertrand S, Walker N, Caput D, Graham D, Bertrand D, Besnard F. (2002) A novel human nicotinic receptor subunit, alpha10, that confers functionality to the alpha9-subunit. Mol Pharmacol, 61 (1): 150-9. [PMID:11752216]

5. Vetter DE, Katz E, Maison SF, Taranda J, Turcan S, Ballestero J, Liberman MC, Elgoyhen AB, Boulter J. (2007) The alpha10 nicotinic acetylcholine receptor subunit is required for normal synaptic function and integrity of the olivocochlear system. Proc Natl Acad Sci USA, 104 (51): 20594-9. [PMID:18077337]

Contributors

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