絞り込み

16555

広告

Crystal structures of the gastric proton pump.

著者 Abe K , Irie K , Nakanishi H , Suzuki H , Fujiyoshi Y
Nature.2018 Apr 04 ; ():.
この記事をPubMed上で見るPubMedで表示
この記事をGoogle翻訳上で見る Google翻訳で開く

スターを付ける スターを付ける     (124view , 0users)

Full Text Sources

Miscellaneous

Other Literature Sources

The gastric proton pump-the H, K-ATPase-is a P-type ATPase responsible for acidifying the gastric juice down to pH 1. This corresponds to a million-fold proton gradient across the membrane of the parietal cell, the steepest known cation gradient of any mammalian tissue. The H, K-ATPase is an important target for drugs that treat gastric acid-related diseases. Here we present crystal structures of the H, K-ATPase in complex with two blockers, vonoprazan and SCH28080, in the luminal-open state, at 2.8 Å resolution. The drugs have partially overlapping but clearly distinct binding modes in the middle of a conduit running from the gastric lumen to the cation-binding site. The crystal structures suggest that the tight configuration at the cation-binding site lowers the pKvalue of Glu820 sufficiently to enable the release of a proton even into the pH 1 environment of the stomach.
PMID: 29618813 [PubMed - as supplied by publisher]
印刷用ページを開く Endnote用テキストダウンロード