Target Information
| Target General Information | Top | |||||
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| Target ID |
T51666
(Former ID: TTDS00044)
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| Target Name |
Gastric H(+)/K(+) ATPase alpha (ATP4A)
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| Synonyms |
Gastric H+/K+ ATPase alpha subunit; Gastric H(+)/K(+)-ATPase; ATP4A
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| Gene Name |
ATP4A
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
| 2 | Gastro-oesophageal reflux disease [ICD-11: DA22] | |||||
| 3 | Oesophageal ulcer [ICD-11: DA25] | |||||
| 4 | Peptic ulcer [ICD-11: DA61] | |||||
| 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.
Click to Show/Hide
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| BioChemical Class |
Acid anhydrides hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 7.2.2.19
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| Sequence |
MGKAENYELYSVELGPGPGGDMAAKMSKKKKAGGGGGKRKEKLENMKKEMEINDHQLSVA
ELEQKYQTSATKGLSASLAAELLLRDGPNALRPPRGTPEYVKFARQLAGGLQCLMWVAAA ICLIAFAIQASEGDLTTDDNLYLAIALIAVVVVTGCFGYYQEFKSTNIIASFKNLVPQQA TVIRDGDKFQINADQLVVGDLVEMKGGDRVPADIRILAAQGCKVDNSSLTGESEPQTRSP ECTHESPLETRNIAFFSTMCLEGTVQGLVVNTGDRTIIGRIASLASGVENEKTPIAIEIE HFVDIIAGLAILFGATFFIVAMCIGYTFLRAMVFFMAIVVAYVPEGLLATVTVCLSLTAK RLASKNCVVKNLEAVETLGSTSVICSDKTGTLTQNRMTVSHLWFDNHIHTADTTEDQSGQ TFDQSSETWRALCRVLTLCNRAAFKSGQDAVPVPKRIVIGDASETALLKFSELTLGNAMG YRDRFPKVCEIPFNSTNKFQLSIHTLEDPRDPRHLLVMKGAPERVLERCSSILIKGQELP LDEQWREAFQTAYLSLGGLGERVLGFCQLYLNEKDYPPGYAFDVEAMNFPSSGLCFAGLV SMIDPPRATVPDAVLKCRTAGIRVIMVTGDHPITAKAIAASVGIISEGSETVEDIAARLR VPVDQVNRKDARACVINGMQLKDMDPSELVEALRTHPEMVFARTSPQQKLVIVESCQRLG AIVAVTGDGVNDSPALKKADIGVAMGIAGSDAAKNAADMILLDDNFASIVTGVEQGRLIF DNLKKSIAYTLTKNIPELTPYLIYITVSVPLPLGCITILFIELCTDIFPSVSLAYEKAES DIMHLRPRNPKRDRLVNEPLAAYSYFQIGAIQSFAGFTDYFTAMAQEGWFPLLCVGLRAQ WEDHHLQDLQDSYGQEWTFGQRLYQQYTCYTVFFISIEVCQIADVLIRKTRRLSAFQQGF FRNKILVIAIVFQVCIGCFLCYCPGMPNIFNFMPIRFQWWLVPLPYGILIFVYDEIRKLG VRCCPGSWWDQELYY Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T68J49 | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Dexlansoprazole | Drug Info | Approved | Non-erosive gastro-esophageal reflux disease | [2] | |
| 2 | Rabeprazole | Drug Info | Approved | Bacterial infection | [3], [4] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | AG-SPT201 | Drug Info | Phase 3 | Ulcerative colitis | [5] | |
| 2 | Esomeprazole magnesium + Aspirin | Drug Info | Phase 3 | Peptic ulcer | [4] | |
| 3 | API-023 | Drug Info | Phase 1 | Gastroesophageal reflux disease | [6] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | Saliphenylhalamide | Drug Info | Preclinical | Solid tumour/cancer | [7] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | Dexlansoprazole | Drug Info | [8] | |||
| 2 | Rabeprazole | Drug Info | [1], [9] | |||
| 3 | Esomeprazole magnesium + Aspirin | Drug Info | [11] | |||
| 4 | API-023 | Drug Info | [12] | |||
| 5 | Saliphenylhalamide | Drug Info | [12] | |||
| 6 | CDRI-85/92 | Drug Info | [12] | |||
| Modulator | [+] 5 Modulator drugs | + | ||||
| 1 | AG-SPT201 | Drug Info | [10] | |||
| 2 | ARH-1029 | Drug Info | [12] | |||
| 3 | CA-50040 | Drug Info | [12] | |||
| 4 | OPC-22575 | Drug Info | [12] | |||
| 5 | PA-10040 | Drug Info | [12] | |||
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Oxidative phosphorylation | |||||
| 2 | Collecting duct acid secretion | |||||
| 3 | Gastric acid secretion | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Gastric Acid Production | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Ion transport by P-type ATPases | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | Iron uptake and transport | |||||
| 2 | Secretion of Hydrochloric Acid in Parietal Cells | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Review article: rabeprazole's tolerability profile in clinical trials. Aliment Pharmacol Ther. 1999 Oct;13 Suppl 5:17-23. | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022287. | |||||
| REF 3 | URL: 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 4 | An overview of proton pump inhibitors. Gastroenterol Nurs. 2003 Sep-Oct;26(5):182-90. | |||||
| REF 5 | ClinicalTrials.gov (NCT01400945) Efficacy Study of AGSPT201 Tablet to Treat Gastroesophageal Reflux Disease. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.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 7 | Lysosomes as a therapeutic target. Nat Rev Drug Discov. 2019 Dec;18(12):923-948. | |||||
| REF 8 | Clinical pipeline report, company report or official report of Takeda (2009). | |||||
| REF 9 | Review article: pharmacokinetic concerns in the selection of anti-ulcer therapy. Aliment Pharmacol Ther. 1999 Oct;13 Suppl 5:11-6. | |||||
| REF 10 | Effects 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 11 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
| REF 12 | URL: 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). | |||||
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