Details of the Target

General Information of Target

Target ID LDTP03062
Target Name Potassium-transporting ATPase alpha chain 1 (ATP4A)
Gene Name ATP4A
Gene ID 495
Synonyms
Potassium-transporting ATPase alpha chain 1; EC 7.2.2.19; Gastric H(+)/K(+) ATPase subunit alpha; Proton pump
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGKAENYELYSVELGPGPGGDMAAKMSKKKKAGGGGGKRKEKLENMKKEMEINDHQLSVA
ELEQKYQTSATKGLSASLAAELLLRDGPNALRPPRGTPEYVKFARQLAGGLQCLMWVAAA
ICLIAFAIQASEGDLTTDDNLYLAIALIAVVVVTGCFGYYQEFKSTNIIASFKNLVPQQA
TVIRDGDKFQINADQLVVGDLVEMKGGDRVPADIRILAAQGCKVDNSSLTGESEPQTRSP
ECTHESPLETRNIAFFSTMCLEGTVQGLVVNTGDRTIIGRIASLASGVENEKTPIAIEIE
HFVDIIAGLAILFGATFFIVAMCIGYTFLRAMVFFMAIVVAYVPEGLLATVTVCLSLTAK
RLASKNCVVKNLEAVETLGSTSVICSDKTGTLTQNRMTVSHLWFDNHIHTADTTEDQSGQ
TFDQSSETWRALCRVLTLCNRAAFKSGQDAVPVPKRIVIGDASETALLKFSELTLGNAMG
YRDRFPKVCEIPFNSTNKFQLSIHTLEDPRDPRHLLVMKGAPERVLERCSSILIKGQELP
LDEQWREAFQTAYLSLGGLGERVLGFCQLYLNEKDYPPGYAFDVEAMNFPSSGLCFAGLV
SMIDPPRATVPDAVLKCRTAGIRVIMVTGDHPITAKAIAASVGIISEGSETVEDIAARLR
VPVDQVNRKDARACVINGMQLKDMDPSELVEALRTHPEMVFARTSPQQKLVIVESCQRLG
AIVAVTGDGVNDSPALKKADIGVAMGIAGSDAAKNAADMILLDDNFASIVTGVEQGRLIF
DNLKKSIAYTLTKNIPELTPYLIYITVSVPLPLGCITILFIELCTDIFPSVSLAYEKAES
DIMHLRPRNPKRDRLVNEPLAAYSYFQIGAIQSFAGFTDYFTAMAQEGWFPLLCVGLRAQ
WEDHHLQDLQDSYGQEWTFGQRLYQQYTCYTVFFISIEVCQIADVLIRKTRRLSAFQQGF
FRNKILVIAIVFQVCIGCFLCYCPGMPNIFNFMPIRFQWWLVPLPYGILIFVYDEIRKLG
VRCCPGSWWDQELYY
Target Type
Successful
Target Bioclass
Enzyme
Family
Cation transport ATPase (P-type) (TC 3.A.3) family, Type IIC subfamily
Subcellular location
Apical cell membrane
Function
The catalytic subunit of the gastric H(+)/K(+) ATPase pump which transports H(+) ions in exchange for K(+) ions across the apical membrane of parietal cells. Uses ATP as an energy source to pump H(+) ions to the gastric lumen while transporting K(+) ion from the lumen into the cell. Remarkably generates a million-fold proton gradient across the gastric parietal cell membrane, acidifying the gastric juice down to pH 1. Within a transport cycle, the transfer of a H(+) ion across the membrane is coupled to ATP hydrolysis and is associated with a transient phosphorylation that shifts the pump conformation from inward-facing (E1) to outward-facing state (E2). The release of the H(+) ion in the stomach lumen is followed by binding of K(+) ion converting the pump conformation back to the E1 state.
TTD ID
T51666
Uniprot ID
P20648
DrugMap ID
TTF1QVM
Ensemble ID
ENST00000262623.4
HGNC ID
HGNC:819
ChEMBL ID
CHEMBL2095173

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C385(1.47)  LDD2182  [1]
Acrolein
 Probe Info  		N.A.  LDD0217  [2]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info  		N.A.  LDD0136  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [2]
 LDCM0625  F8 Ramos C385(1.30)  LDD2187  [1]
 LDCM0572  Fragment10 Ramos C385(1.22)  LDD2189  [1]
 LDCM0573  Fragment11 Ramos C385(1.37)  LDD2190  [1]
 LDCM0574  Fragment12 Ramos C385(1.31)  LDD2191  [1]
 LDCM0575  Fragment13 Ramos C385(0.91)  LDD2192  [1]
 LDCM0576  Fragment14 Ramos C385(1.10)  LDD2193  [1]
 LDCM0579  Fragment20 Ramos C385(2.30)  LDD2194  [1]
 LDCM0580  Fragment21 Ramos C385(1.19)  LDD2195  [1]
 LDCM0582  Fragment23 Ramos C385(1.01)  LDD2196  [1]
 LDCM0578  Fragment27 Ramos C385(0.81)  LDD2197  [1]
 LDCM0588  Fragment30 Ramos C385(1.00)  LDD2199  [1]
 LDCM0589  Fragment31 Ramos C385(1.08)  LDD2200  [1]
 LDCM0590  Fragment32 Ramos C385(1.23)  LDD2201  [1]
 LDCM0468  Fragment33 Ramos C385(0.72)  LDD2202  [1]
 LDCM0596  Fragment38 Ramos C385(0.81)  LDD2203  [1]
 LDCM0566  Fragment4 Ramos C385(1.73)  LDD2184  [1]
 LDCM0610  Fragment52 Ramos C385(0.62)  LDD2204  [1]
 LDCM0614  Fragment56 Ramos C385(0.82)  LDD2205  [1]
 LDCM0569  Fragment7 Ramos C385(1.53)  LDD2186  [1]
 LDCM0571  Fragment9 Ramos C385(1.99)  LDD2188  [1]
 LDCM0022  KB02 Ramos C385(1.47)  LDD2182  [1]
 LDCM0023  KB03 Ramos C385(1.76)  LDD2183  [1]
 LDCM0024  KB05 Ramos C385(1.89)  LDD2185  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dexlansoprazole Small molecular drug D06YYD
Esomeprazole Small molecular drug DB00736
Lansoprazole Small molecular drug DB00448
Omeprazole Small molecular drug DB00338
Pantoprazole Small molecular drug DB00213
Rabeprazole Small molecular drug D0KL4J
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ag-spt201 . D0V3ZN
Esomeprazole Magnesium + Aspirin . D0B2ZZ
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Api-023 . D0Z9NY
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Saliphenylhalamide Small molecular drug D0K1UF
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Arh-1029 . D0E2MI
Ca-50040 . D06ZAK
Cdri-85/92 . D0N0KG
Opc-22575 . D0K6LA
Pa-10040 . D03SSG

References

1 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
2 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
3 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.