2021
DOI: 10.1021/acs.jmedchem.0c02201 View full text |Buy / Rent full text
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Abstract: Pregnane X receptor (PXR) plays roles in detoxification and other physiological processes. PXR activation may enhance drug metabolism (leading to adverse drug reactions) or inhibit inflammation. Therefore, PXR agonists, antagonists, and inverse agonists may serve as research tools and drug candidates. However, a specific PXR modulator with an associated structure–activity relationship is lacking. Based on the scaffold of specific human PXR (hPXR) antagonist SPA70 (10), we developed 81 SPA70 analogs and evaluat… Show more

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