Influence of endometrial 17 beta-hydroxysteroid dehydrogenase activity on the binding of estradiol to receptors. 1981

E Gurpide, and C Marks

Specimens of proliferative and secretory endometrium which differ in the levels of 17 beta-estradiol dehydrogenase activity, were superfused with mixtures of [3H]estradiol ([3H]E2) and [3H]ethynyl estradiol ([3H]EE) in the presence and absence of diethylstilbestrol. Concentrations of labeled E2, EE, and estrone were measured in homogenates and in nuclei isolated from the superfused tissues. The relative proportions of [3H]EE and [3H]E2 bound to nuclear receptor were much higher in secretory than in proliferative endometrium. Since EE binds to the estrogen receptor but is not a substrate for 17 beta-estradiol dehydrogenase, these results demonstrate the influence of metabolism on the binding of E2 to the receptor. The elevated enzymatic activity present in secretory endometrium also accounts for the relatively lower concentration of [3H]E2 and the increased [3H]estrone to [3H]E2 ratio in the superfused tissue.

UI MeSH Term Description Entries
D011960 Receptors, Estrogen Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important. Estrogen Receptor,Estrogen Receptors,Estrogen Nuclear Receptor,Estrogen Receptor Type I,Estrogen Receptor Type II,Estrogen Receptors Type I,Estrogen Receptors Type II,Receptor, Estrogen Nuclear,Receptors, Estrogen, Type I,Receptors, Estrogen, Type II,Nuclear Receptor, Estrogen,Receptor, Estrogen
D002467 Cell Nucleus Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed) Cell Nuclei,Nuclei, Cell,Nucleus, Cell
D004054 Diethylstilbestrol A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed) Stilbestrol,Agostilben,Apstil,Diethylstilbestrol, (Z)-Isomer,Diethylstilbestrol, Disodium Salt,Distilbène,Stilbene Estrogen,Tampovagan,Estrogen, Stilbene
D004717 Endometrium The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo. Endometria
D004958 Estradiol The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. 17 beta-Estradiol,Estradiol-17 beta,Oestradiol,17 beta-Oestradiol,Aerodiol,Delestrogen,Estrace,Estraderm TTS,Estradiol Anhydrous,Estradiol Hemihydrate,Estradiol Hemihydrate, (17 alpha)-Isomer,Estradiol Monohydrate,Estradiol Valerate,Estradiol Valeriante,Estradiol, (+-)-Isomer,Estradiol, (-)-Isomer,Estradiol, (16 alpha,17 alpha)-Isomer,Estradiol, (16 alpha,17 beta)-Isomer,Estradiol, (17-alpha)-Isomer,Estradiol, (8 alpha,17 beta)-(+-)-Isomer,Estradiol, (8 alpha,17 beta)-Isomer,Estradiol, (9 beta,17 alpha)-Isomer,Estradiol, (9 beta,17 beta)-Isomer,Estradiol, Monosodium Salt,Estradiol, Sodium Salt,Estradiol-17 alpha,Estradiol-17beta,Ovocyclin,Progynon-Depot,Progynova,Vivelle,17 beta Estradiol,17 beta Oestradiol,Estradiol 17 alpha,Estradiol 17 beta,Estradiol 17beta,Progynon Depot
D004960 Estradiol Dehydrogenases Enzymes that catalyze the oxidation of estradiol at the 17-hydroxyl group in the presence of NAD+ or NADP+ to yield estrone and NADH or NADPH. The 17-hydroxyl group can be in the alpha- or beta-configuration. EC 1.1.1.62 17 beta-Estradiol Dehydrogenase,Estradiol 17 alpha-Dehydrogenase,Estradiol 17 beta-Dehydrogenase,Estradiol Dehydrogenase,17 alpha-Dehydrogenase, Estradiol,17 beta Estradiol Dehydrogenase,17 beta-Dehydrogenase, Estradiol,Dehydrogenase, 17 beta-Estradiol,Dehydrogenase, Estradiol,Dehydrogenases, Estradiol,Estradiol 17 alpha Dehydrogenase,Estradiol 17 beta Dehydrogenase
D004970 Estrone An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women. Folliculin (Hormone),Estrone, (+-)-Isomer,Estrone, (8 alpha)-Isomer,Estrone, (9 beta)-Isomer,Estrovarin,Kestrone,Unigen,Wehgen
D004997 Ethinyl Estradiol A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES. 19-Norpregna-1,3,5(10)-trien-20-yne-3,17-diol, (17alpha)-,Ethynyl Estradiol,Estinyl,Ethinyl Estradiol Hemihydrate,Ethinyl Estradiol, (8 alpha)-Isomer,Ethinyl Estradiol, (8 alpha,17 alpha)-Isomer,Ethinyl Estradiol, (8 alpha,9 beta,13 alpha,14 beta)-Isomer,Ethinyl Estradiol, (9 beta,17 alpha)-Isomer,Ethinyl-Oestradiol Effik,Ethinylestradiol Jenapharm,Ethinyloestradiol,Lynoral,Microfollin,Microfollin Forte,Progynon C,Estradiol, Ethinyl,Estradiol, Ethynyl,Ethinyl Oestradiol Effik,Hemihydrate, Ethinyl Estradiol,Jenapharm, Ethinylestradiol
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

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