Abstract
The human cytochrome P450 enzyme CYP8B1 is a crucial regulator of the balance of cholic acid (CA) and chenodeoxycholic acid (CDCA) in the liver. It was previously shown to catalyze the conversion of 7α-hydroxycholest-4-en-3-one, a CDCA precursor, to 7α,12α-dihydroxycholest-4-en-3-one, which is an intermediate of CA biosynthesis. In this study we demonstrate that CYP8B1 can also convert CDCA itself to CA. We also show that five derivatives of luciferin are metabolized by CYP8B1 and established a rapid and convenient inhibitor test system. In this way we were able to identify four new CYP8B1 inhibitors, which are aminobenzotriazole, exemestane, ketoconazole and letrozole.
Acknowledgments
We thank Dr. Youcai Zhang for helpful discussions.
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Supplementary Material
The online version of this article offers supplementary material (https://doi.org/10.1515/hsz-2018-0379).
©2019 Walter de Gruyter GmbH, Berlin/Boston
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- Frontmatter
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- Oxidative stress and antioxidants in the pathophysiology of malignant melanoma
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- Molecular Medicine
- The comparative biochemistry of viruses and humans: an evolutionary path towards autoimmunity
- MiR-23a-3p-regulated abnormal acetylation of FOXP3 induces regulatory T cell function defect in Graves’ disease
- Cell Biology and Signaling
- Evidence for a protective role of the CX3CL1/CX3CR1 axis in a model of amyotrophic lateral sclerosis
- LncRNA TINCR/microRNA-107/CD36 regulates cell proliferation and apoptosis in colorectal cancer via PPAR signaling pathway based on bioinformatics analysis
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