Title : Pharmacogenomics of tamoxifen: roles of drug metabolizing enzymes and transporters.

Pub. Date : 2012

PMID : 22041137






4 Functional Relationships(s)
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1 Tamoxifen requires metabolic activation by cytochrome P450 (CYP) enzymes for formation of active metabolites, 4-hydroxytamoxifen and endoxifen, which have 30- to 100-fold greater affinity to the estrogen receptor and the potency to suppress estrogen-dependent breast cancer cell proliferation. Tamoxifen cytochrome P450 family 4 subfamily F member 3 Homo sapiens
2 Tamoxifen requires metabolic activation by cytochrome P450 (CYP) enzymes for formation of active metabolites, 4-hydroxytamoxifen and endoxifen, which have 30- to 100-fold greater affinity to the estrogen receptor and the potency to suppress estrogen-dependent breast cancer cell proliferation. Tamoxifen cytochrome P450 family 4 subfamily F member 3 Homo sapiens
3 The genetic polymorphisms in the other drug-metabolizing enzymes, including other CYP isoforms, sulfotransferases and UDP-glucuronosyltransferases might contribute to individual differences in the tamoxifen metabolism and clinical outcome of tamoxifen therapy although their contributions would be small. Tamoxifen cytochrome P450 family 4 subfamily F member 3 Homo sapiens
4 The genetic polymorphisms in the other drug-metabolizing enzymes, including other CYP isoforms, sulfotransferases and UDP-glucuronosyltransferases might contribute to individual differences in the tamoxifen metabolism and clinical outcome of tamoxifen therapy although their contributions would be small. Tamoxifen cytochrome P450 family 4 subfamily F member 3 Homo sapiens