Target Information
| Target General Information | Top | |||||
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| Target ID |
T40800
(Former ID: TTDS00045)
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| Target Name |
Sodium pump subunit alpha-1 (ATP1A1)
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| Synonyms |
Sodium/potassium-transporting ATPase alpha1; Sodium pump 1; Na+/K+ ATPase 1; ATP1A1
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| Gene Name |
ATP1A1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 7 Target-related Diseases | + | ||||
| 1 | Cardiac arrhythmia [ICD-11: BC9Z] | |||||
| 2 | Chronic obstructive pulmonary disease [ICD-11: CA22] | |||||
| 3 | Corneal disease [ICD-11: 9A76-9A78] | |||||
| 4 | Heart failure [ICD-11: BD10-BD1Z] | |||||
| 5 | Hyperhidrosis [ICD-11: EE00] | |||||
| 6 | Malaria [ICD-11: 1F40-1F45] | |||||
| 7 | Supraventricular tachyarrhythmia [ICD-11: BC81] | |||||
| Function |
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of atp coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions.
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| BioChemical Class |
Acid anhydrides hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 7.2.2.13
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| Sequence |
MGKGVGRDKYEPAAVSEQGDKKGKKGKKDRDMDELKKEVSMDDHKLSLDELHRKYGTDLS
RGLTSARAAEILARDGPNALTPPPTTPEWIKFCRQLFGGFSMLLWIGAILCFLAYSIQAA TEEEPQNDNLYLGVVLSAVVIITGCFSYYQEAKSSKIMESFKNMVPQQALVIRNGEKMSI NAEEVVVGDLVEVKGGDRIPADLRIISANGCKVDNSSLTGESEPQTRSPDFTNENPLETR NIAFFSTNCVEGTARGIVVYTGDRTVMGRIATLASGLEGGQTPIAAEIEHFIHIITGVAV FLGVSFFILSLILEYTWLEAVIFLIGIIVANVPEGLLATVTVCLTLTAKRMARKNCLVKN LEAVETLGSTSTICSDKTGTLTQNRMTVAHMWFDNQIHEADTTENQSGVSFDKTSATWLA LSRIAGLCNRAVFQANQENLPILKRAVAGDASESALLKCIELCCGSVKEMRERYAKIVEI PFNSTNKYQLSIHKNPNTSEPQHLLVMKGAPERILDRCSSILLHGKEQPLDEELKDAFQN AYLELGGLGERVLGFCHLFLPDEQFPEGFQFDTDDVNFPIDNLCFVGLISMIDPPRAAVP DAVGKCRSAGIKVIMVTGDHPITAKAIAKGVGIISEGNETVEDIAARLNIPVSQVNPRDA KACVVHGSDLKDMTSEQLDDILKYHTEIVFARTSPQQKLIIVEGCQRQGAIVAVTGDGVN DSPALKKADIGVAMGIAGSDVSKQAADMILLDDNFASIVTGVEEGRLIFDNLKKSIAYTL TSNIPEITPFLIFIIANIPLPLGTVTILCIDLGTDMVPAISLAYEQAESDIMKRQPRNPK TDKLVNERLISMAYGQIGMIQALGGFFTYFVILAENGFLPIHLLGLRVDWDDRWINDVED SYGQQWTYEQRKIVEFTCHTAFFVSIVVVQWADLVICKTRRNSVFQQGMKNKILIFGLFE ETALAAFLSYCPGMGVALRMYPLKPTWWFCAFPYSLLIFVYDEVRKLIIRRRPGGWVEKE TYY Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A01671 ; BADD_A02409 ; BADD_A02982 ; BADD_A04410 | |||||
| HIT2.0 ID | T70OGQ | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 8 Approved Drugs | + | ||||
| 1 | Acetyldigitoxin | Drug Info | Approved | Congestive heart failure | [2], [3] | |
| 2 | Acocantherin | Drug Info | Approved | Heart failure | [4], [5] | |
| 3 | Almitrine | Drug Info | Approved | Chronic obstructive pulmonary disease | [6] | |
| 4 | Aluminium | Drug Info | Approved | Hyperhidrosis | [7] | |
| 5 | Artemether | Drug Info | Approved | Malaria | [8] | |
| 6 | Chloroprocaine | Drug Info | Approved | Anaesthesia | [9], [10] | |
| 7 | Deslanoside | Drug Info | Approved | Heart failure | [11], [12], [13] | |
| 8 | Lumefantrine | Drug Info | Approved | Malaria | [12] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | UNBS-1450 | Drug Info | Phase 1 | Solid tumour/cancer | [14] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Acetyldigitoxin | Drug Info | [15] | |||
| Binder | [+] 6 Binder drugs | + | ||||
| 1 | Acocantherin | Drug Info | [1] | |||
| 2 | Almitrine | Drug Info | [16], [17] | |||
| 3 | Aluminium | Drug Info | [18], [19] | |||
| 4 | Artemether | Drug Info | [8] | |||
| 5 | Deslanoside | Drug Info | [1] | |||
| 6 | Lumefantrine | Drug Info | [8] | |||
| Blocker | [+] 1 Blocker drugs | + | ||||
| 1 | Chloroprocaine | Drug Info | [20] | |||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | UNBS-1450 | Drug Info | [21] | |||
| 2 | DIGITOXIGENIN | Drug Info | [22] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| 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 Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 17 KEGG Pathways | + | ||||
| 1 | cGMP-PKG signaling pathway | |||||
| 2 | cAMP signaling pathway | |||||
| 3 | Cardiac muscle contraction | |||||
| 4 | Adrenergic signaling in cardiomyocytes | |||||
| 5 | Insulin secretion | |||||
| 6 | Thyroid hormone synthesis | |||||
| 7 | Thyroid hormone signaling pathway | |||||
| 8 | Aldosterone-regulated sodium reabsorption | |||||
| 9 | Endocrine and other factor-regulated calcium reabsorption | |||||
| 10 | Proximal tubule bicarbonate reclamation | |||||
| 11 | Salivary secretion | |||||
| 12 | Gastric acid secretion | |||||
| 13 | Pancreatic secretion | |||||
| 14 | Carbohydrate digestion and absorption | |||||
| 15 | Protein digestion and absorption | |||||
| 16 | Bile secretion | |||||
| 17 | Mineral absorption | |||||
| Pathwhiz Pathway | [+] 4 Pathwhiz Pathways | + | ||||
| 1 | Kidney Function | |||||
| 2 | Lactose Degradation | |||||
| 3 | Trehalose Degradation | |||||
| 4 | Muscle/Heart Contraction | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Ion transport by P-type ATPases | |||||
| WikiPathways | [+] 1 WikiPathways | + | ||||
| 1 | Iron uptake and transport | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 2 | 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: 6794). | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009436. | |||||
| REF 4 | 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: 4826). | |||||
| REF 5 | Drug information of Ouabain, 2008. eduDrugs. | |||||
| REF 6 | Improving oxygenation during bronchopulmonary lavage using nitric oxide inhalation and almitrine infusion. Anesth Analg. 1999 Aug;89(2):302-4. | |||||
| REF 7 | Drug information of Cocculin, 2008. eduDrugs. | |||||
| REF 8 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | |||||
| REF 9 | 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: 7145). | |||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040273. | |||||
| REF 11 | 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: 6806). | |||||
| REF 12 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009282. | |||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029692) | |||||
| REF 15 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 16 | Almitrine, a new kind of energy-transduction inhibitor acting on mitochondrial ATP synthase. Biochim Biophys Acta. 1989 Aug 3;975(3):325-9. | |||||
| REF 17 | Flux-dependent increase in the stoichiometry of charge translocation by mitochondrial ATPase/ATP synthase induced by almitrine. Biochim Biophys Acta. 1990 Jul 17;1018(1):91-7. | |||||
| REF 18 | The inhibitory effect of aluminium on the (Na+/K+)ATPase activity of rat brain cortex synaptosomes. J Inorg Biochem. 2003 Sep 15;97(1):143-50. | |||||
| REF 19 | Effects of aluminium and lead on ATPase activity of knockout +/- mouse cerebral synaptosomes in vitro. Altern Lab Anim. 2004 Oct;32(4):361-7. | |||||
| REF 20 | Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics. Pharmacol Res. 2001 Apr;43(4):399-403. | |||||
| REF 21 | Early downregulation of Mcl-1 regulates apoptosis triggered by cardiac glycoside UNBS1450. Cell Death Dis. 2015 Jun 11;6:e1782. | |||||
| REF 22 | 17beta-O-Aminoalkyloximes of 5beta-androstane-3beta,14beta-diol with digitalis-like activity: synthesis, cardiotonic activity, structure-activity r... J Med Chem. 2000 Jun 15;43(12):2332-49. | |||||
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