Target Information

Target General Infomation
Target ID
T51666
Former ID
TTDS00044
Target Name
Potassium-transporting ATPase alpha chain 1
Gene Name
ATP4A
Synonyms
Gastric H(+)/K(+)-ATPase; Gastric H+/K+ ATPase alpha subunit; Proton pump; ATP4A
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Cardiovascular disorder [ICD10: I00-I99]
Erosive esophagitis; Non-erosive gastro-esophageal reflux disease [ICD9: 530; ICD10: K20, K21]
Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21]
Helicobacter pylori infection [ICD9: 41.86; ICD10: B96.81]
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27]
Stomach ulcer [ICD10: K25-K27]
Ulcerative colitis [ICD9: 556; ICD10: K51]
Function
Catalyzes the hydrolysis of ATP coupled with the exchange of H(+) and K(+) ions across the plasma membrane. Responsible for acid production in the stomach.
BioChemical Class
Acid anhydrides hydrolase
Target Validation
T51666
UniProt ID
P20648
EC Number
EC 3.6.3.10
Sequence
MGKAENYELYSVELGPGPGGDMAAKMSKKKKAGGGGGKRKEKLENMKKEMEINDHQLSVA
ELEQKYQTSATKGLSASLAAELLLRDGPNALRPPRGTPEYVKFARQLAGGLQCLMWVAAA
ICLIAFAIQASEGDLTTDDNLYLAIALIAVVVVTGCFGYYQEFKSTNIIASFKNLVPQQA
TVIRDGDKFQINADQLVVGDLVEMKGGDRVPADIRILAAQGCKVDNSSLTGESEPQTRSP
ECTHESPLETRNIAFFSTMCLEGTVQGLVVNTGDRTIIGRIASLASGVENEKTPIAIEIE
HFVDIIAGLAILFGATFFIVAMCIGYTFLRAMVFFMAIVVAYVPEGLLATVTVCLSLTAK
RLASKNCVVKNLEAVETLGSTSVICSDKTGTLTQNRMTVSHLWFDNHIHTADTTEDQSGQ
TFDQSSETWRALCRVLTLCNRAAFKSGQDAVPVPKRIVIGDASETALLKFSELTLGNAMG
YRDRFPKVCEIPFNSTNKFQLSIHTLEDPRDPRHLLVMKGAPERVLERCSSILIKGQELP
LDEQWREAFQTAYLSLGGLGERVLGFCQLYLNEKDYPPGYAFDVEAMNFPSSGLCFAGLV
SMIDPPRATVPDAVLKCRTAGIRVIMVTGDHPITAKAIAASVGIISEGSETVEDIAARLR
VPVDQVNRKDARACVINGMQLKDMDPSELVEALRTHPEMVFARTSPQQKLVIVESCQRLG
AIVAVTGDGVNDSPALKKADIGVAMGIAGSDAAKNAADMILLDDNFASIVTGVEQGRLIF
DNLKKSIAYTLTKNIPELTPYLIYITVSVPLPLGCITILFIELCTDIFPSVSLAYEKAES
DIMHLRPRNPKRDRLVNEPLAAYSYFQIGAIQSFAGFTDYFTAMAQEGWFPLLCVGLRAQ
WEDHHLQDLQDSYGQEWTFGQRLYQQYTCYTVFFISIEVCQIADVLIRKTRRLSAFQQGF
FRNKILVIAIVFQVCIGCFLCYCPGMPNIFNFMPIRFQWWLVPLPYGILIFVYDEIRKLG
VRCCPGSWWDQELYY
Drugs and Mode of Action
Drug(s) Dexlansoprazole Drug Info Approved Erosive esophagitis; Non-erosive gastro-esophageal reflux disease [538589]
Rabeprazole Drug Info Approved Bacterial infections [535862], [542311]
AG-SPT201 Drug Info Phase 3 Ulcerative colitis [523556]
Esomeprazole magnesium + Aspirin Drug Info Phase 3 Peptic ulcer [535862]
API-023 Drug Info Phase 1 Gastroesophageal reflux disease [521830]
Modulator AG-SPT201 Drug Info [525464]
ARH-1029 Drug Info [543965]
CA-50040 Drug Info [543965]
OPC-22575 Drug Info [543965]
PA-10040 Drug Info [543965]
Inhibitor API-023 Drug Info [543965]
CDRI-85/92 Drug Info [543965]
Dexlansoprazole Drug Info [551717]
Esomeprazole magnesium + Aspirin Drug Info [550288]
Rabeprazole Drug Info [534917], [534918]
Saliphenylhalamide Drug Info [543965]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Oxidative phosphorylation
Collecting duct acid secretion
Gastric acid secretion
PathWhiz Pathway Gastric Acid Production
Reactome Ion transport by P-type ATPases
WikiPathways Iron uptake and transport
Secretion of Hydrochloric Acid in Parietal Cells
References
Ref 521830ClinicalTrials.gov (NCT00325715) AGN 201904 Versus Esomeprazole in the Prevention of Aspirin-induced Stomach or Upper Intestinal Damage in Healthy Volunteers. U.S. National Institutes of Health.
Ref 523556ClinicalTrials.gov (NCT01400945) Efficacy Study of AGSPT201 Tablet to Treat Gastroesophageal Reflux Disease. U.S. National Institutes of Health.
Ref 535862An overview of proton pump inhibitors. Gastroenterol Nurs. 2003 Sep-Oct;26(5):182-90.
Ref 538589FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022287.
Ref 542311(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: 7290).
Ref 525464Effects of pantoprazole, a novel H+/K+-ATPase inhibitor, on duodenal ulcerogenic and healing responses in rats: a comparative study with omeprazole and lansoprazole. J Gastroenterol Hepatol. 1999 Mar;14(3):251-7.
Ref 534917Review article: pharmacokinetic concerns in the selection of anti-ulcer therapy. Aliment Pharmacol Ther. 1999 Oct;13 Suppl 5:11-6.
Ref 534918Review article: rabeprazole's tolerability profile in clinical trials. Aliment Pharmacol Ther. 1999 Oct;13 Suppl 5:17-23.
Ref 543965(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. (Target id: 849).
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 551717Clinical pipeline report, company report or official report of Takeda (2009).

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