Target Information

Target General Infomation
Target ID
T55094
Former ID
TTDR01256
Target Name
Acid-sensing ion channel ASIC1a/ASIC1b
Gene Name
ASIC1
Synonyms
ACCN2; Acid-sensing ion channel 1; Amiloride-sensitive cation channel 2, neuronal; BNaC2; Brain sodium channel 2; ASIC1
Target Type
Successful
Disease Congestive heart failure; Hypertension [ICD9: 428; ICD10: I50]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
Isoform 1 does not display proton-gated cation channel activity.
BioChemical Class
Amiloride-sensitive sodium channel
UniProt ID
P78348
Sequence
MELKAEEEEVGGVQPVSIQAFASSSTLHGLAHIFSYERLSLKRALWALCFLGSLAVLLCV
CTERVQYYFHYHHVTKLDEVAASQLTFPAVTLCNLNEFRFSQVSKNDLYHAGELLALLNN
RYEIPDTQMADEKQLEILQDKANFRSFKPKPFNMREFYDRAGHDIRDMLLSCHFRGEVCS
AEDFKVVFTRYGKCYTFNSGRDGRPRLKTMKGGTGNGLEIMLDIQQDEYLPVWGETDETS
FEAGIKVQIHSQDEPPFIDQLGFGVAPGFQTFVACQEQRLIYLPPPWGTCKAVTMDSDLD
FFDSYSITACRIDCETRYLVENCNCRMVHMPGDAPYCTPEQYKECADPALDFLVEKDQEY
CVCEMPCNLTRYGKELSMVKIPSKASAKYLAKKFNKSEQYIGENILVLDIFFEVLNYETI
EQKKAYEIAGLLGDIGGQMGLFIGASILTVLELFDYAYEVIKHKLCRRGKCQKEAKRSSA
DKGVALSLDDVKRHNPCESLRGHPAGMTYAANILPHHPARGTFEDFTC
Drugs and Mode of Action
Drug(s) Amiloride Drug Info Approved Congestive heart failure; Hypertension [538224], [539551]
PPC-5650 Drug Info Phase 1 Pain [523653]
Modulator Amiloride Drug Info [556264]
PPC-5650 Drug Info [523653]
Blocker PcTx1 Drug Info [536309], [537642]
Pathways
KEGG Pathway Inflammatory mediator regulation of TRP channels
Reactome Stimuli-sensing channels
WikiPathways Iron uptake and transport
References
Ref 523653ClinicalTrials.gov (NCT01449487) Investigation of Efficacy and Safety of PPC-5650 to Experimental Induced Sensation and Pain in the Rectosigmoid. U.S. National Institutes of Health.
Ref 538224FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070346.
Ref 539551(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2421).
Ref 523653ClinicalTrials.gov (NCT01449487) Investigation of Efficacy and Safety of PPC-5650 to Experimental Induced Sensation and Pain in the Rectosigmoid. U.S. National Institutes of Health.
Ref 536309Peptides inhibitors of acid-sensing ion channels. Toxicon. 2007 Feb;49(2):271-84.
Ref 537642Challenges in Analgesic Drug Development. Clin Pharmacol Ther. 2009 Aug 12.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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