How ligands modulate the gastric H,K-ATPase activity and its inhibition by tegoprazan.

ABSTRACT: The introduction of potassium-competitive acid blockers (P-CABs) has been a major innovation in gastric H,K-ATPase inhibition and many laboratories are actively engaged in the development of novel molecules within this class. This work investigates the interaction between H,K-ATPase and tegoprazan, a representative of the P-CABs group, in terms of K⁺ and H⁺ binding, through functional and structural analyses. First, by studying the H,K-ATPase activity, we found a model to describe the non-Michaelis-Menten kinetics through a "ping-pong" mechanism that explains a stoichiometry of 1 H⁺, 1 K⁺, and 1 ATP molecule, but also considering the influence of H⁺ on the ionization states of the protein. A kinetic evaluation of the inhibition of tego

SUBMITTER: Cerf NT 

PROVIDER: S-EPMC11697777 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature