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ASIC2

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 685

Nomenclature: ASIC2

Family: Acid-sensing (proton-gated) ion channels (ASICs)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 512 17q11.2-q12 ASIC2 acid sensing ion channel subunit 2
Mouse 2 512 11 48.43 cM Asic2 acid-sensing ion channel 2
Rat 2 512 10q26 Asic2 acid sensing ion channel subunit 2
Previous and Unofficial Names Click here for help
ACCN | ACCN1 | acid-sensing ion channel 2 | acid-sensing (proton-gated) ion channel 2 | acid sensing (proton gated) ion channel 2 | amiloride-sensitive brain sodium channel 2 | amiloride-sensitive cation channel 1 | amiloride-sensitive cation channel 1, neuronal | ASIC2a | BNaC1 | BNaC1a | BNC1 | BNC1k | brain sodium channel 1 | degenerin | MDEG
Database Links Click here for help
Alphafold Q16515 (Hs), Q925H0 (Mm), Q62962 (Rn)
ChEMBL Target CHEMBL3232695 (Mm), CHEMBL3562171 (Rn)
Ensembl Gene ENSG00000108684 (Hs), ENSMUSG00000020704 (Mm), ENSRNOG00000058308 (Rn)
Entrez Gene 40 (Hs), 11418 (Mm), 25364 (Rn)
Human Protein Atlas ENSG00000108684 (Hs)
KEGG Gene hsa:40 (Hs), mmu:11418 (Mm), rno:25364 (Rn)
OMIM 601784 (Hs)
Pharos Q16515 (Hs)
UniProtKB Q16515 (Hs), Q925H0 (Mm), Q62962 (Rn)
Wikipedia ASIC2 (Hs)
Functional Characteristics Click here for help
γ=10.4-13.4 pS
PNa/PK =10, PNa/PCa = 20
rapid activation rate, moderate inactivation rate (3.3-5.5 s) @ pH 5
Natural/Endogenous Ligands Click here for help
H+

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Activators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
Extracellular H+ Click here for species-specific activity table Ligand is endogenous in the given species Hs - ~4.1 – 5.0 pEC50 - no
⤷ pEC50 ~4.1 – 5.0 (EC50 ~8x10-5 – 1x10-5 M)
Not voltage dependent
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
diminazene Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs - no ~6.1 pIC50 - no 4
⤷ pIC50 ~6.1 [4]
Not voltage dependent
amiloride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs - no 4.6 pIC50 - no 9
⤷ pIC50 4.6 (IC50 2.8x10-5 M) [9]
Not voltage dependent
A-317567 Small molecule or natural product Click here for species-specific activity table Hs - no ~4.5 pIC50 - no 3
⤷ pIC50 ~4.5 (IC50 ~3x10-5 M) [3]
Not voltage dependent
nafamostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs - no ~4.2 pIC50 - no 8
⤷ pIC50 ~4.2 (IC50 ~7x10-5 M) [8]
Not voltage dependent
Cd2+ Click here for species-specific activity table Hs - no ~3.0 pIC50 - no 7
⤷ pIC50 ~3.0 (IC50 ~1x10-3 M) Partial inhibition [7]
Not voltage dependent
Immunopharmacology Comments
Non-steroidal anti-inflammatory drugs (NSAIDs) are direct inhibitors of ASIC currents (reviewed in [1]). Inflammatory conditions and particular pro-inflammatory mediators such as arachidonic acid induce overexpression of ASIC-encoding genes and enhance ASIC currents [2,5-6]. The sustained current component mediated by ASIC3 is potentiated by hypertonic solutions in a manner that is synergistic with the effect of arachidonic acid [2].

References

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1. Baron A, Lingueglia E. (2015) Pharmacology of acid-sensing ion channels - Physiological and therapeutical perspectives. Neuropharmacology, 94: 19-35. [PMID:25613302]

2. Deval E, Noël J, Lay N, Alloui A, Diochot S, Friend V, Jodar M, Lazdunski M, Lingueglia E. (2008) ASIC3, a sensor of acidic and primary inflammatory pain. EMBO J, 27 (22): 3047-55. [PMID:18923424]

3. Dubé GR, Lehto SG, Breese NM, Baker SJ, Wang X, Matulenko MA, Honoré P, Stewart AO, Moreland RB, Brioni JD. (2005) Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. Pain, 117 (1-2): 88-96. [PMID:16061325]

4. Lee JYP, Saez NJ, Cristofori-Armstrong B, Anangi R, King GF, Smith MT, Rash LD. (2018) Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain. Br J Pharmacol, 175 (12): 2204-2218. [PMID:29134638]

5. Mamet J, Baron A, Lazdunski M, Voilley N. (2002) Proinflammatory mediators, stimulators of sensory neuron excitability via the expression of acid-sensing ion channels. J Neurosci, 22 (24): 10662-70. [PMID:12486159]

6. Smith ES, Cadiou H, McNaughton PA. (2007) Arachidonic acid potentiates acid-sensing ion channels in rat sensory neurons by a direct action. Neuroscience, 145 (2): 686-98. [PMID:17258862]

7. Staruschenko A, Dorofeeva NA, Bolshakov KV, Stockand JD. (2007) Subunit-dependent cadmium and nickel inhibition of acid-sensing ion channels. Dev Neurobiol, 67 (1): 97-107. [PMID:17443775]

8. Ugawa S, Ishida Y, Ueda T, Inoue K, Nagao M, Shimada S. (2007) Nafamostat mesilate reversibly blocks acid-sensing ion channel currents. Biochem Biophys Res Commun, 363 (1): 203-8. [PMID:17826743]

9. Waldmann R, Champigny G, Voilley N, Lauritzen I, Lazdunski M. (1996) The mammalian degenerin MDEG, an amiloride-sensitive cation channel activated by mutations causing neurodegeneration in Caenorhabditis elegans. J Biol Chem, 271 (18): 10433-6. [PMID:8631835]

Contributors

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