Intestinal Farnesoid X Receptor Activation by Pharmacologic Inhibition of the Organic Solute Transporter α-β.

Sandra M W van de Wiel,D Rudi de Waart,Ronald P J Oude Elferink,Stan F J van de Graaf

Cellular and Molecular Gastroenterology and Hepatology（2018）

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摘要

This study identifies clofazimine as an inhibitor of OSTα-OSTβ in vitro and in vivo, validates OSTα-OSTβ as a drug target to enhance intestinal bile acid signaling, and confirmed the applicability of the Förster Resonance Energy Transfer-bile acid sensor to screen for inhibitors of bile acid efflux pathways.

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关键词

Fluorescence Resonance Energy Transfer (FRET),FXR,OSTα-OSTβ,Bile Acids

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