RQ-00000774 / RaQualia - LARVOL DELTA

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