Startseite Lebenswissenschaften Conversion of chenodeoxycholic acid to cholic acid by human CYP8B1
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Conversion of chenodeoxycholic acid to cholic acid by human CYP8B1

  • Linbing Fan , Jan Felix Joseph , Pradeepraj Durairaj , Maria Kristina Parr und Matthias Bureik EMAIL logo
Veröffentlicht/Copyright: 18. Dezember 2018

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).


Received: 2018-09-19
Accepted: 2018-11-13
Published Online: 2018-12-18
Published in Print: 2019-05-27

©2019 Walter de Gruyter GmbH, Berlin/Boston

Heruntergeladen am 29.1.2026 von https://www.degruyterbrill.com/document/doi/10.1515/hsz-2018-0379/pdf
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