Esterase estradiol

Katz J, Levitz M, Kadner SS, Finlay TH (1991) Estradiol esters can replace 17b-estradiol in the stimulation of DNA and esterase synthesis by MCF-7 cells a possible role for the estrogen-sensitive MCF-7 cell esterase. J Steroid Biochem Mol Biol 38 17-26... 

The inhibition by other organophosphate compounds of the carboxylesterase which hydrolyzes malathion is a further example of xenobiotic interaction resulting from irreversible inhibition because, in this case, the enzyme is phosphorylated by the inhibitor. A second type of inhibition involving organophosphorus insecticides involves those containing the P=S moiety. During CYP activation to the esterase-inhibiting oxon, reactive sulfur is released that inhibits CYP isoforms by an irreversible interaction with the heme iron. As a result, these chemicals are inhibitors of the metabolism of other xenobiotics, such as carbaryl and fipronil, and are potent inhibitors of the metabolism of steroid hormones such as testosterone and estradiol. 

When the transdermal penetration of a drug is inadequate to achieve and maintain a plasma concentration above the minimum therapeutic concentration required to produce the desired effect, a lipophilic prodrug that will be metabolized in the epidermis to the active drug could be used in the development of a controlled-release transdermal delivery system. This approach has been applied to estradiol esters (diacetate and valerate) which are rapidly converted by esterases in the skin tissue to estradiol (Chien et al, 1985). The prodrug serves to increase the transdermal bioavailability of the active drug to which it is converted by metabolism (generally ester hydrolysis) during the percutaneous absorption process. 

Estafiatin, 3079 Esterases, 2346 Ester hydrolysis, 370 Esters, 361, 3371,3373 Estradiol, 2385, 2448 Estradiol receptor P (ERP), 2413 Estradiol receptors (ERs), 2385, 2413 Estragole, 2976 Estrogen, 1374, 1829, 3752 Estrogen-dependant human breast cancer, 3478 Estrogenic, 2419, 2447 activity, 2291, 2466 anti-estrogenic, 2652 effect, 2412... 

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