[H+, K+ -ATPase, H+ -ATPase]. 1996

N Takeguchi, and S Asano, and M Morii
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.

Gastric H+, K+ -ATPase comprised of alpha- and beta-subunits was functionally expressed in an animal cell-line. When glutamic acid (345) of the alpha-subunit was mutated to glutamine, the affinity of K+ decreased 10-fold, indicating that this residue in the 4th transmembrane domain engages in the determination of the K+ affinity. The roles of other residues are also discussed. The number of the binding site of proton pump inhibitors such as omeprazole and E3810 (rabeprazole) is 1, which is contrary to the proposal of 2 or 3 by other researchers. The reason of this discrepancy is explained. The interaction between 2 or 4 alpha-subunits was shown to be necessary for the function of this pump. Finally, recent topics about H+ -ATPase are discussed.

UI MeSH Term Description Entries
D009853 Omeprazole A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. H 168-68,Omeprazole Magnesium,Omeprazole Sodium,Prilosec,H 168 68,H 16868,Magnesium, Omeprazole,Sodium, Omeprazole
D011506 Proteins Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein. Gene Products, Protein,Gene Proteins,Protein,Protein Gene Products,Proteins, Gene
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000596 Amino Acids Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. Twenty alpha-amino acids are the subunits which are polymerized to form proteins. Amino Acid,Acid, Amino,Acids, Amino
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001562 Benzimidazoles Compounds with a BENZENE fused to IMIDAZOLES.
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D013270 Stomach An organ of digestion situated in the left upper quadrant of the abdomen between the termination of the ESOPHAGUS and the beginning of the DUODENUM. Stomachs
D017506 H(+)-K(+)-Exchanging ATPase An enzyme isolated from the GASTRIC MUCOSA that catalyzes the hydrolysis of ATP coupled with the exchange of hydrogen and potassium ions across the cell wall. This enzyme was formerly listed as EC 3.6.1.36. ATPase, Hydrogen, Potassium,Adenosinetriphosphatase, Hydrogen, Potassium,H(+)-K(+)-Transporting ATPase,Hydrogen, Potassium ATPase,Hydrogen, Potassium, Adenosinetriphosphatase,Adenosine Triphosphatase, Hydrogen, Potassium,Gastric H(+) K(+) ATPase,Hydrogen, Potassium, Adenosine Triphosphatase,Hydrogen-Potassium-Exchanging ATPase,Potassium Hydrogen ATPase,ATPase Hydrogen, Potassium,ATPase, Hydrogen-Potassium-Exchanging,ATPase, Potassium Hydrogen,Hydrogen Potassium Exchanging ATPase
D053799 2-Pyridinylmethylsulfinylbenzimidazoles Compounds that contain benzimidazole joined to a 2-methylpyridine via a sulfoxide linkage. Several of the compounds in this class are ANTI-ULCER AGENTS that act by inhibiting the POTASSIUM HYDROGEN ATPASE found in the PROTON PUMP of GASTRIC PARIETAL CELLS. 2-Methylpyridine 2-Benzimidazole Sulfoxides,2-Pyridinylmethylsulfinyl-2-Benzimidazoles,Benzimidazole Methylpyridine Sulfoxides,Timoprazole Derivatives,Timoprazoles,2 Methylpyridine 2 Benzimidazole Sulfoxides,2 Pyridinylmethylsulfinyl 2 Benzimidazoles,2 Pyridinylmethylsulfinylbenzimidazoles,2-Benzimidazole Sulfoxides, 2-Methylpyridine,Methylpyridine Sulfoxides, Benzimidazole,Sulfoxides, 2-Methylpyridine 2-Benzimidazole,Sulfoxides, Benzimidazole Methylpyridine

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