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Literature summary for 7.2.2.19 extracted from

  • Shin, J.M.; Munson, K.; Vagin, O.; Sachs, G.
    The gastric HK-ATPase: structure, function, and inhibition (2009), Pflugers Arch., 457, 609-622.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
K791S the mutation greatly reduces enzyme activity as well as increases the Ki for 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile Homo sapiens
K791S the mutation greatly reduces enzyme activity as well as increases the Ki for 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile Rattus norvegicus
K791S the mutation greatly reduces enzyme activity as well as increases the Ki for 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile Oryctolagus cuniculus
K791S the mutation greatly reduces enzyme activity as well as increases the Ki for 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile Canis lupus familiaris
K791S the mutation greatly reduces enzyme activity as well as increases the Ki for SCH28080 Sus scrofa
additional information mutations towards the exoplasmic surface of TM4, TM5, TM6, the loop between TM5 and TM6, and one site at the end of TM8 altered either the Ki or change the nature of inhibition from strictly competitive to mixed or even non-competitive without affecting ion affinity Homo sapiens
additional information mutations towards the exoplasmic surface of TM4, TM5, TM6, the loop between TM5 and TM6, and one site at the end of TM8 altered either the Ki or change the nature of inhibition from strictly competitive to mixed or even non-competitive without affecting ion affinity Rattus norvegicus
additional information mutations towards the exoplasmic surface of TM4, TM5, TM6, the loop between TM5 and TM6, and one site at the end of TM8 altered either the Ki or change the nature of inhibition from strictly competitive to mixed or even non-competitive without affecting ion affinity Sus scrofa
additional information mutations towards the exoplasmic surface of TM4, TM5, TM6, the loop between TM5 and TM6, and one site at the end of TM8 altered either the Ki or change the nature of inhibition from strictly competitive to mixed or even non-competitive without affecting ion affinity Oryctolagus cuniculus
additional information mutations towards the exoplasmic surface of TM4, TM5, TM6, the loop between TM5 and TM6, and one site at the end of TM8 altered either the Ki or change the nature of inhibition from strictly competitive to mixed or even non-competitive without affecting ion affinity Canis lupus familiaris

Inhibitors

Inhibitors Comment Organism Structure
2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile i.e. SCH28080 Canis lupus familiaris
2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile i.e. SCH28080 Homo sapiens
2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile i.e. SCH28080 Oryctolagus cuniculus
2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile i.e. SCH28080 Rattus norvegicus
2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile i.e. SCH28080 Sus scrofa
BYK36399
-
Canis lupus familiaris
BYK36399
-
Homo sapiens
BYK36399
-
Oryctolagus cuniculus
BYK36399
-
Rattus norvegicus
BYK36399
-
Sus scrofa
esomeprazole
-
Canis lupus familiaris
esomeprazole
-
Homo sapiens
esomeprazole
-
Oryctolagus cuniculus
esomeprazole
-
Rattus norvegicus
esomeprazole
-
Sus scrofa
lansoprazole
-
Canis lupus familiaris
lansoprazole
-
Homo sapiens
lansoprazole
-
Oryctolagus cuniculus
lansoprazole
-
Rattus norvegicus
lansoprazole
-
Sus scrofa
additional information inhibitor binding and inhibition kinetics Canis lupus familiaris
additional information inhibitor binding and inhibition kinetics Homo sapiens
additional information inhibitor binding and inhibition kinetics Oryctolagus cuniculus
additional information inhibitor binding and inhibition kinetics Rattus norvegicus
additional information inhibitor binding and inhibition kinetics Sus scrofa
N-methyl-BYK36399
-
Canis lupus familiaris
N-methyl-BYK36399
-
Homo sapiens
N-methyl-BYK36399
-
Oryctolagus cuniculus
N-methyl-BYK36399
-
Rattus norvegicus
N-methyl-BYK36399
-
Sus scrofa
Omeprazole
-
Canis lupus familiaris
Omeprazole
-
Homo sapiens
Omeprazole
-
Oryctolagus cuniculus
Omeprazole
-
Rattus norvegicus
Omeprazole
-
Sus scrofa
pantoprazole
-
Canis lupus familiaris
pantoprazole
-
Homo sapiens
pantoprazole
-
Oryctolagus cuniculus
pantoprazole
-
Rattus norvegicus
pantoprazole
-
Sus scrofa
rabeprazole
-
Canis lupus familiaris
rabeprazole
-
Homo sapiens
rabeprazole
-
Oryctolagus cuniculus
rabeprazole
-
Rattus norvegicus
rabeprazole
-
Sus scrofa
timoprazole
-
Canis lupus familiaris
timoprazole
-
Homo sapiens
timoprazole
-
Oryctolagus cuniculus
timoprazole
-
Rattus norvegicus
timoprazole
-
Sus scrofa

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane apical membrane Sus scrofa 16020
-
membrane apical membrane Oryctolagus cuniculus 16020
-
membrane apical membrane Canis lupus familiaris 16020
-
membrane apical membrane, cytoplasmic tubular membranes in the resting state Homo sapiens 16020
-
membrane apical membrane, cytoplasmic tubular membranes in the resting state Rattus norvegicus 16020
-
microsome relatively ion tight vesicles Sus scrofa
-
-
microvillus microvilli of the expanded secretory canaliculus in the stimulated state of the parietal cell Homo sapiens 5902
-
microvillus microvilli of the expanded secretory canaliculus in the stimulated state of the parietal cell Rattus norvegicus 5902
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens
Mg2+ required Rattus norvegicus
Mg2+ required Sus scrofa
Mg2+ required Oryctolagus cuniculus
Mg2+ required Canis lupus familiaris

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + H+/in + K+/out Homo sapiens the H,K-ATPase is the final step of acid secretion ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out Rattus norvegicus the H,K-ATPase is the final step of acid secretion ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out Sus scrofa the H,K-ATPase is the final step of acid secretion ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out Oryctolagus cuniculus the H,K-ATPase is the final step of acid secretion ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out Canis lupus familiaris the H,K-ATPase is the final step of acid secretion ADP + phosphate + H+/out + K+/in
-
?
additional information Homo sapiens a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion ?
-
?
additional information Rattus norvegicus a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion ?
-
?
additional information Sus scrofa a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion ?
-
?
additional information Oryctolagus cuniculus a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion ?
-
?
additional information Canis lupus familiaris a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion ?
-
?

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-
Oryctolagus cuniculus
-
-
-
Rattus norvegicus
-
-
-
Sus scrofa
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein N-glycosylation of the beta subunit Homo sapiens
glycoprotein N-glycosylation of the beta subunit Rattus norvegicus
glycoprotein N-glycosylation of the beta subunit Sus scrofa
glycoprotein N-glycosylation of the beta subunit Oryctolagus cuniculus
glycoprotein N-glycosylation of the beta subunit Canis lupus familiaris

Reaction

Reaction Comment Organism Reaction ID
ATP + H2O + H+[side 1] + K+[side 2] = ADP + phosphate + H+[side 2] + K+[side 1] orientation of the subunits in the membrane towards cytoplasmic and periplasmic sides and reaction mechanism, detailed overview Homo sapiens
ATP + H2O + H+[side 1] + K+[side 2] = ADP + phosphate + H+[side 2] + K+[side 1] orientation of the subunits in the membrane towards cytoplasmic and periplasmic sides and reaction mechanism, detailed overview Rattus norvegicus
ATP + H2O + H+[side 1] + K+[side 2] = ADP + phosphate + H+[side 2] + K+[side 1] orientation of the subunits in the membrane towards cytoplasmic and periplasmic sides and reaction mechanism, detailed overview Sus scrofa
ATP + H2O + H+[side 1] + K+[side 2] = ADP + phosphate + H+[side 2] + K+[side 1] orientation of the subunits in the membrane towards cytoplasmic and periplasmic sides and reaction mechanism, detailed overview Oryctolagus cuniculus
ATP + H2O + H+[side 1] + K+[side 2] = ADP + phosphate + H+[side 2] + K+[side 1] orientation of the subunits in the membrane towards cytoplasmic and periplasmic sides and reaction mechanism, detailed overview Canis lupus familiaris

Source Tissue

Source Tissue Comment Organism Textmining
oxyntic cell
-
Homo sapiens
-
oxyntic cell
-
Rattus norvegicus
-
oxyntic cell
-
Sus scrofa
-
oxyntic cell
-
Oryctolagus cuniculus
-
oxyntic cell
-
Canis lupus familiaris
-
renal medulla
-
Homo sapiens
-
renal medulla
-
Rattus norvegicus
-
renal medulla
-
Sus scrofa
-
renal medulla
-
Oryctolagus cuniculus
-
renal medulla
-
Canis lupus familiaris
-
stomach
-
Homo sapiens
-
stomach
-
Rattus norvegicus
-
stomach
-
Sus scrofa
-
stomach
-
Oryctolagus cuniculus
-
stomach
-
Canis lupus familiaris
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + H+/in + K+/out
-
Homo sapiens ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out
-
Rattus norvegicus ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out
-
Sus scrofa ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out
-
Oryctolagus cuniculus ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out
-
Canis lupus familiaris ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out the H,K-ATPase is the final step of acid secretion Homo sapiens ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out the H,K-ATPase is the final step of acid secretion Rattus norvegicus ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out the H,K-ATPase is the final step of acid secretion Sus scrofa ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out the H,K-ATPase is the final step of acid secretion Oryctolagus cuniculus ADP + phosphate + H+/out + K+/in
-
?
ATP + H2O + H+/in + K+/out the H,K-ATPase is the final step of acid secretion Canis lupus familiaris ADP + phosphate + H+/out + K+/in
-
?
additional information a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion Homo sapiens ?
-
?
additional information a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion Rattus norvegicus ?
-
?
additional information a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion Sus scrofa ?
-
?
additional information a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion Oryctolagus cuniculus ?
-
?
additional information a K+ efflux channel is associated with the gastric H,K-ATPase, KCNQ1-KCNE2 appears to be the K+ efflux channel that is essential for gastric acid secretion Canis lupus familiaris ?
-
?

Subunits

Subunits Comment Organism
heterodimer alphabeta structure, determination of the primary structure of the gastric H,K-ATPase alpha subunit containing the catalytic site, sequence comparison Homo sapiens
heterodimer alphabeta structure, determination of the primary structure of the gastric H,K-ATPase alpha subunit containing the catalytic site, sequence comparison Rattus norvegicus
heterodimer alphabeta structure, determination of the primary structure of the gastric H,K-ATPase alpha subunit containing the catalytic site, sequence comparison Sus scrofa
heterodimer alphabeta structure, determination of the primary structure of the gastric H,K-ATPase alpha subunit containing the catalytic site, sequence comparison Oryctolagus cuniculus
heterodimer alphabeta structure, determination of the primary structure of the gastric H,K-ATPase alpha subunit containing the catalytic site, sequence comparison Canis lupus familiaris
More a cluster of intramembranal carboxylic amino acids is located in the middle of the transmembrane segments TM4, TM5,TM6, and TM8 of the alpha-subunit that contains the ion binding domain in this enzyme and the ATPase Homo sapiens
More a cluster of intramembranal carboxylic amino acids is located in the middle of the transmembrane segments TM4, TM5,TM6, and TM8 of the alpha-subunit that contains the ion binding domain in this enzyme and the ATPase Rattus norvegicus
More a cluster of intramembranal carboxylic amino acids is located in the middle of the transmembrane segments TM4, TM5,TM6, and TM8 of the alpha-subunit that contains the ion binding domain in this enzyme and the ATPase Sus scrofa
More a cluster of intramembranal carboxylic amino acids is located in the middle of the transmembrane segments TM4, TM5,TM6, and TM8 of the alpha-subunit that contains the ion binding domain in this enzyme and the ATPase Oryctolagus cuniculus
More a cluster of intramembranal carboxylic amino acids is located in the middle of the transmembrane segments TM4, TM5,TM6, and TM8 of the alpha-subunit that contains the ion binding domain in this enzyme and the ATPase Canis lupus familiaris

Synonyms

Synonyms Comment Organism
gastric HK-ATPase
-
Homo sapiens
gastric HK-ATPase
-
Rattus norvegicus
gastric HK-ATPase
-
Sus scrofa
gastric HK-ATPase
-
Oryctolagus cuniculus
gastric HK-ATPase
-
Canis lupus familiaris
More the enzyme is a member of the P2-type ATPase family Homo sapiens
More the enzyme is a member of the P2-type ATPase family Rattus norvegicus
More the enzyme is a member of the P2-type ATPase family Sus scrofa
More the enzyme is a member of the P2-type ATPase family Oryctolagus cuniculus
More the enzyme is a member of the P2-type ATPase family Canis lupus familiaris

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens
ATP
-
Rattus norvegicus
ATP
-
Sus scrofa
ATP
-
Oryctolagus cuniculus
ATP
-
Canis lupus familiaris