Cryo-EM structure of the gastric proton pump complexed with revaprazan
Ontology highlight
ABSTRACT:
SUBMITTER: Kazuhiro Abe
PROVIDER: EMPIAR-11057 | biostudies-other |
REPOSITORIES: biostudies-other
Publications
Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump.
Tanaka Saki S Morita Mikio M Yamagishi Tatsuya T Madapally Hridya Valia HV Hayashida Kenichi K Khandelia Himanshu H Gerle Christoph C Shigematsu Hideki H Oshima Atsunori A Abe Kazuhiro K
Journal of medicinal chemistry 20220523 11
As specific inhibitors of the gastric proton pump, responsible for gastric acidification, K<sup>+</sup>-competitive acid blockers (P-CABs) have recently been utilized in the clinical treatment of gastric acid-related diseases in Asia. However, as these compounds have been developed based on phenotypic screening, their detailed binding poses are unknown. We show crystal and cryo-EM structures of the gastric proton pump in complex with four different P-CABs, tegoprazan, soraprazan, PF-03716556 and ...[more]
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