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May 24, 2022
Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump.
(PubMed, J Med Chem)
- "We show crystal and cryo-EM structures of the gastric proton pump in complex with four different P-CABs, tegoprazan, soraprazan, PF-03716556 and revaprazan, at resolutions reaching 2.8 Å. We reveal that revaprazan has a novel binding mode in which its tetrahydroisoquinoline moiety binds deep in the cation transport conduit. The mechanism of action of these P-CABs can now be evaluated at the molecular level, which will facilitate the rational development and improvement of currently available P-CABs to provide better treatment of acid-related gastrointestinal diseases."
Journal • Gastroenterology • Gastrointestinal Disorder
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