Abstract:
:CYP20A1 is a well-conserved member of the human cytochrome P450 enzyme family for which no endogenous or xenobiotic substrate is known. We have recently shown that this enzyme has moderate activity towards two proluciferin probe substrates. In order to facilitate the search for physiological substrates we have tested nine additional proluciferins in this study and identified three such probe substrates that give much higher product yields. Using one of these probes, we demonstrate inhibition of CYP20A1 activity by 1-benzylimidazole, ketoconazole and letrozole. Finally, we show that the combination of two common single nucleotide polymorphisms (SNPs) of CYP20A1 leads to an enzyme (CYP20A1Leu97Phe346) with reduced activity.
journal_name
Biol Chemjournal_title
Biological chemistryauthors
Durairaj P,Fan L,Sharma SS,Jie Z,Bureik Mdoi
10.1515/hsz-2019-0307subject
Has Abstractpub_date
2020-02-25 00:00:00pages
361-365issue
3eissn
1431-6730issn
1437-4315pii
/j/bchm.ahead-of-print/hsz-2019-0307/hsz-2019-0307journal_volume
401pub_type
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