Title : Steroid bioconjugation to a CYP3A4 allosteric site and its effect on substrate binding and coupling efficiency.

Pub. Date : 2018 Sep 1

PMID : 29958895






2 Functional Relationships(s)
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1 Recently, we demonstrated that steroid bioconjugation at the allosteric site results in an increase in activity of CYP3A4 toward testosterone and 7-benzyloxy-4-trifluoromethylcoumarin oxidation. Testosterone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Here, using the established bioconjugation methodology, we show how steroid bioconjugation at the allosteric site affects the heme spin state, the binding affinity (KS) of CYP3A4 for testosterone, as well as the enzyme coupling efficiency. Testosterone cytochrome P450 family 3 subfamily A member 4 Homo sapiens