Quantitative metabolomics services for biomarker discovery and validation.
Specializing in ready to use metabolomics kits.
Your source for quantitative metabolomics technologies and bioinformatics.
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Nuclear receptor coactivator 1 Endoxifen Transporter ADP/ATP translocase 1 4- Hydroxytamoxifen Transporter ADP/ATP translocase 1 Dimethylaniline monooxygenase [N-oxide- forming] 3 Dimethylaniline monooxygenase [N-oxide- forming] 1 Cytochrome P450 3A4 Cytochrome P450 2D6 Cytochrome P450 3A4 Cytochrome P450 3A5 Cytochrome P450 3A4 Cytochrome P450 3A5 Cytochrome P450 2D6 UDP- glucuronosyltransferase 1-10 Heat shock 70 kDa protein 1A/1B Steroid hormone receptor ERR1 Steroid hormone receptor ERR1 Steroid hormone receptor ERR1 Heat shock 70 kDa protein 1A/1B Endoxifen Endoxifen Endoxifen 4-Hydroxytamoxifen 4-Hydroxytamoxifen 4-Hydroxytamoxifen Tamoxifen Tamoxifen Tamoxifen NADPH H+ O2 Tamoxifen N-oxide NADP H2O H2O NADP O2 NADPH H+ NADPH H+ O2 NADP H2O O2 NADPH H+ N-Desmethyltamoxifen H2O Formaldehyde NADP O2 NADPH H+ H2O Formaldehyde NADP NADPH H+ O2 H2O NADP Uridine diphosphate glucuronic acid Endoxifen O-glucuronide Uridine 5'-diphosphate Estradiol FAD FAD Heme Heme Heme Heme Heme Heme Endoxifen Endoxifen Promoter ER Target Gene Heme Hepatocyte Breast Cancer Cell Tamoxifen is absorbed through the GI tract into the bloodstream after being administered orally. Tamoxifen travels through the bloodstream to the liver where it is metabolized via multiple liver enzymes. Endoxifen and 4-Hydroxytamoxifen are metabolites from Tamoxifen that act as active metabolites. They are released back into the blood after being synthesized in the liver. Endoxifen binds to estrogen receptors, displacing heat shock proteins. This forms the estrogen receptor complex. Endoxifen prevents the binding of estradiol to the estrogen receptors. Estradiol is unable to bind the receptor due to endoxifen The receptor complex with endoxifen translocates to the nucleus where it binds to the promoter region of estrogen target genes. The complex after binding the promoter region requires a co-activator protein in order to start transcription. Due to endoxifen binding to the receptor instead of estradiol, the co-activator protein cannot bind to the complex. With no activation from the co-activator, transcription of the target gene cannot occur leading to cellular death/apoptosis killing the cancer cell. Liver Breast Nucleus
Nucleus Endoplasmic Reticulum NCOA1 Unknown SLC25A4 Unknown SLC25A4 FMO3 FMO1 CYP3A4 CYP2D6 CYP3A4 CYP3A5 CYP3A4 CYP3A5 CYP2D6 UGT1A10 HSPA1A ESRRA ESRRA ESRRA HSPA1A Endoxifen Endoxifen Endoxifen 4- Hydroxytamoxifen 4- Hydroxytamoxifen 4- Hydroxytamoxifen Tamoxifen Tamoxifen Tamoxifen NADPH Hydrogen Ion Oxygen Tamoxifen N-oxide NADP Water Water NADP Oxygen NADPH Hydrogen Ion NADPH Hydrogen Ion Oxygen NADP Water Oxygen NADPH Hydrogen Ion N- Desmethyltamoxifen Water Formaldehyde NADP Oxygen NADPH Hydrogen Ion Water Formaldehyde NADP NADPH Hydrogen Ion Oxygen Water NADP Uridine diphosphate glucuronic acid Endoxifen O-glucuronide Uridine 5'-diphosphate Estradiol Endoxifen Endoxifen Promoter ER Target Gene