Pub. Date : 2002 Aug
PMID : 12207635
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | The influence of CYP2B6, CYP2C9 and CYP2D6 genotypes on the formation of the potent antioestrogen Z-4-hydroxy-tamoxifen in human liver. | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 2 | AIMS: To investigate in a large panel of 50 human liver samples the contribution of CYP2C9, CYP2D6, and CYP3A4 to the overall formation of the potent antioestrogen Z-4-hydroxy-tamoxifen, and how various genotypes affect its formation from tamoxifen. | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 3 | METHODS: The formation of Z-4-hydroxy-tamoxifen from 10 microm tamoxifen was studied in human liver microsomes (n=50), characterized for CYP2B6, CYP2C9, CYP2D6 and CYP3A4 expression, and CYP2B6, CYP2C9 and CYP2D6 genotype. | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 4 | RESULTS: Z-4-hydroxy-tamoxifen was formed by supersomes expressing CYP2B6, CYP2C9, CYP2C19 and CYP2D6, but not CYP3A4. | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 5 | Furthermore, Z-4-hydroxy-tamoxifen formation significantly correlated with both CYP2C9 expression (r(s)=0.256, P<0.05) and CYP2D6 expression (r(s)=0.309, P<0.05). | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 6 | CYP2D6 and CYP2C9 contribute on average 45 and 46%, respectively, to the overall formation of Z-4-hydroxy-tamoxifen. | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 7 | CONCLUSIONS: CYP2B6, CYP2C9 and CYP2D6 genotypes all affected Z-4-hydroxy-tamoxifen formation and can predict individual ability to catalyse this reaction. | z-4-hydroxy-tamoxifen | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |