Title : Inhibition of human cytochrome P450 3A4 activity by zinc(II) ion.

Pub. Date : 2005 Apr 28

PMID : 15763633






6 Functional Relationships(s)
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1 Effects of Zn2+ on the activity and conformation of cytochorome P450 3A4 (CYP3A4) were investigated. Zinc cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Effects of Zn2+ on the activity and conformation of cytochorome P450 3A4 (CYP3A4) were investigated. Zinc cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Zn2+ specifically inhibited the testosterone 6beta-hydroxylation activity of CYP3A4 with an IC50 value of 27 microM. Zinc cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 Zn2+ inhibited the CO-binding spectra of CYP3A4 reduced by NADPH-cytochrome P450 reductase (CPR) and NADPH only in the presence of b5. Zinc cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 Zn2+-induced conformational changes of CYP3A4 were monitored by CD and intrinsic fluorescence. Zinc cytochrome P450 family 3 subfamily A member 4 Homo sapiens
6 These results suggest that the inhibitory effects of Zn2+ come from preventing the stimulation of b5 on CYP3A4 activity. Zinc cytochrome P450 family 3 subfamily A member 4 Homo sapiens