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In addition, isomerization of 4-hydroxytamoxifen is catalyzed by CYP1B1,2B6, and 2C19 (7).
O-glucuronidation of 4-hydroxytamoxifen is mainly mediated by UDP-glucuronosyltransferases (UGTs) UGT1A4, 2B15, 2B7, 1A8, and various others to produce 4-hydroxytamoxifen-O-glucuronide (33-35).
We possess a genetic "switch" that controls expression of telomerase, but, unlike the mice that were altered to respond to 4-hydroxytamoxifen, we don't know exactly what chemical turns telomerase on in our bodies.
At steady state, achieved after 2 weeks of therapy, mean plasma 4-hydroxytamoxifen levels were just 1/18 of those measured in 19 healthy controls taking 20 mg/day of oral tamoxifen.
TamoGel(TM) is a percutaneously applied gel formulation of the anti-estrogen 4-hydroxytamoxifen (4-OHT), the most active metabolite of tamoxifen.
17[beta]-Estradiol, genistein and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the G protein-coupled receptor GPR30.
TamoGel(TM) is a percutaneously applied gel formulation of 4-Hydroxytamoxifen (4- OHT) that is currently under investigation in a variety of benign and malignant estrogen-dependent conditions by ASCEND Therapeutics.
Estrogen receptor alpha mediated induction of the transforming growth factor alpha gene by estradiol and 4-hydroxytamoxifen in MDA-MB-231 breast cancer cells.