2xzb

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Pig Gastric H,K-ATPase with bound BeF and SCH28080

Structural highlights

2xzb is a 2 chain structure with sequence from Sus scrofa. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:Electron crystallography, Resolution 7Å
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

ATP4A_PIG 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.

Publication Abstract from PubMed

Acid-related gastric diseases are associated with disorder of digestive tract acidification. The gastric proton pump, H(+),K(+)-ATPase, exports H(+) in exchange for luminal K(+) to generate a highly acidic environment in the stomach, and is a main target for acid suppressants. Here, we report the three-dimensional structure of gastric H(+),K(+)-ATPase with bound SCH28080, a representative K(+)-competitive acid blocker, at 7 A resolution based on electron crystallography of two-dimensional crystals. The density of the bound SCH28080 is found near transmembrane (TM) helices 4, 5 and 6, in the luminal cavity. The SCH28080-binding site is formed by the rearrangement of TM helices, which is in turn transmitted to the cytoplasmic domains, resulting in a luminal-open conformation. These results represent the first structural evidence for a binding site of an acid suppressant on H(+),K(+)-ATPase, and the conformational change induced by this class of drugs.

Conformational rearrangement of gastric H(+),K(+)-ATPase induced by an acid suppressant.,Abe K, Tani K, Fujiyoshi Y Nat Commun. 2011 Jan;2(1):155. PMID:21224846[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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Citations
11 reviews cite this structure
Gastric acid, calcium absorption, and their impact on bone health.
Kopic et al. (2013)
10 more
21 other articles
No citations found

See Also

References

  1. ↑ Abe K, Tani K, Fujiyoshi Y. Conformational rearrangement of gastric H(+),K(+)-ATPase induced by an acid suppressant. Nat Commun. 2011 Jan;2(1):155. PMID:21224846 doi:10.1038/ncomms1154

Contents


PDB ID 2xzb

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OCA

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