Conversion of chenodeoxycholic acid to cholic acid by human CYP8B1
| Autor: | Matthias Bureik, Linbing Fan, Jan Felix Joseph, Pradeepraj Durairaj, Maria Kristina Parr |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
medicine.drug_class Clinical Biochemistry Cholic Acid Chenodeoxycholic Acid Biochemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Biosynthesis Chenodeoxycholic acid medicine Humans Steroid 12-alpha-Hydroxylase Enzyme Inhibitors Molecular Biology Fluorescent Dyes chemistry.chemical_classification Molecular Structure biology Bile acid Cholic acid Cytochrome P450 Luciferin 030104 developmental biology Enzyme chemistry 030220 oncology & carcinogenesis Biocatalysis biology.protein CYP8B1 |
| Zdroj: | Biological Chemistry. 400:625-628 |
| ISSN: | 1437-4315 1431-6730 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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