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Bazedoxifene scaffold-based mimetics of solomonsterols A and B as novel pregnane X receptor antagonistsHodnik, Žiga, farmacevt ...Pregnane X receptor (PXR), a member of the NR1I nuclear receptor family, acts as a xenobiotic sensor and a paramount transcriptional regulator of drug metabolising enzymes and transporters. The ... overexpression of PXR in various cancer cells indicates the importance of PXR as a drug target for countering multi drug resistance in anticancer treatments. We describe the discovery of novel, bazedoxifene scaffold-based PXR antagonists, inspired by the marine sulphated steroids, solomonsterols A and B, as natural leads. Luciferase reporter assay on a PXR transfected HepG2 cell line identified compounds 19-24 as promising PXR antagonists. Further structure-activity relationship study of the most active PXR antagonist from the series (compound 20, IC50 = 11 [micro]M revealed the importance of hydroxy groups as hydrogen bond donors for PXR antagonistic activity. PXR antagonists 20 and 24 (IC50 = 14 [micro]M), in addition to the down-regulation of PXR expression, exhibited an inhibition of PXR-induced CYP3A4 expression, which illustrates their potential to suppress PXR-regulated phase I drug metabolism.Source: Journal of medicinal chemistry. - ISSN 0022-2623 (Vol. 57, no. 11, 2014, str. 4819-4833)Type of material - article, component partPublish date - 2014Language - englishCOBISS.SI-ID - 3647601
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Database name | Field | Year |
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Hodnik, Žiga, farmacevt | 33052 |
Peterlin-Mašič, Lucija | 19317 |
Tomašič, Tihomir | 28334 |
Smodiš, Domen, farmacevt | 54098 |
D'Amore, Claudio | |
Fiorucci, Stefano | |
Kikelj, Danijel | 01463 |
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