Acid pump antagonists

Proton Pump Inhibitors and Acid Pump Antagonists... 

Proton Pump Inhibitors and Acid Pump Antagonists retinoid X receptor (RXR) and is also activated by various lipophilic compounds produced by the body such as bile acids and steroids. PXR heterodimerized with RXR stimulates the transcription of cytochrome P450 3A monooxygenases (CYP3A) and other genes involved in the detoxification and elimination of the... 

Proton Pump Inhibitors and Acid Pump Antagonists. Figure 1 Irreversible proton pump inhibitors (PPIs). 

Proton Pump Inhibitors and Acid Pump Antagonists. Figure 2 Chemical mechanism of irreversible PPIs. PPIs are accumulated in acidic lumen and converted to active sulfenic acid and/or sulfenamide by acid catalysis. These active forms bind to extracytoplasmic cysteines of the gastric H.K-ATPase [3]. 

Whereas the PPIs have a unique targeting and covalent inhibitory action on the proton pump based on their chemistry and the biology of the parietal cell, another class of compounds-acid pump antagonists-have a structural specificity... 

BY 841, an acid pump antagonist that has been shown to be an effective antisecretory agent in humans, providing an intragastn c pH of approximately 6.0, 1 hour after administration. 

An Illustration of the binding site of acid pump antagonists such as the imidazopyridine, SCH28080, with the transmembrane segments numbered and the amino acids to which this compound binds emphasized as ball-and-stick forms and named. By comparing this to the binding site for PPIs, it can be seen that there is overlap of this binding site with that of omeprazole and other PPIs. 

Wurst W, Hartmann M (1996) Current status of acid pump antagonists (reversible PPIs). Yale J Biol Med 69 233-243... 

Yoon YA, Park CS, Cha MH, Choi H, Sim JY, Kim JG (2010) Novel pyrimidines as acid pump antagonists (APAs). Bioorg Med Chem Lett 20 5735-5738... 

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