Studies on the mechanism of estrogen biosynthesis in the rat ovary–I

Brodie, Angela; Schwarzel, William C.; Brodie, Harry J.

doi:10.1016/0022-4731(76)90180-1

Cited by 109 publications

(21 citation statements)

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“…Py, reflux; c H 2 , 10% Pd/C, CH 2 Cl 2 , CH 3 OH, and RT Anti-aromatase assay was carried out in purpose of screening potential inhibitory effect of the newly synthesized compounds. The assay was run in the denucleated ovarian fraction from PMSG-pretreated female rats (Penov Gaši et al, 2001;Brodie et al, 1976). The compounds were tested in two concentrations (10 and 50 lL).…”

Section: Resultsmentioning

confidence: 99%

“…In brief, in the final volume of 0.25 ml, the incubation mixture contained testosterone as substrate, 1 mM NADPH, 0.1 M phosphate buffer (pH 7.4), tested compound and 0.125 ml of denucleated ovarian fraction (0.33 mg of protein, prepared by known procedure; Brodie et al, 1976). Parallel incubations without tested compounds were also run as control samples.…”

Section: Animals Treatment and Assaymentioning

confidence: 99%

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Evaluation of biological activity of new hemiesters of 17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile

Јovanović-Šanta

Andrić

et al. 2010

Med Chem Res

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In uterotrophic assay newly synthesized compounds 2-5 showed a complete loss of estrogenic activity, whereas derivatives 2-4 exhibited slight, and compound 5 higher antiestrogenic effects. On the other hand, anti-aromatase assay showed that compounds 2, 3, and 4 possess inhibition potency, although lower than standard aromatase inhibitor aminoglutethimide. Cytotoxicity of compounds 2-5, estradiol and tamoxifen against several human tumor or healthy cell lines (MCF-7, MDA-MB-231, HT-29, and MRC-5) was evaluated after short-time treatment.

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Section: Resultsmentioning

confidence: 99%

Section: Animals Treatment and Assaymentioning

confidence: 99%

Evaluation of biological activity of new hemiesters of 17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile

Јovanović-Šanta

Andrić

et al. 2010

Med Chem Res

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“…In addition, using the method of Brodie et al [23] we determined the aromatase activity in the ovarian microsome fraction of the test animals and did not find a significant change. Accordingly, meso-3-PtSO 4 did not inhibit the transformation of testosterone into E 1 in a microsomal fraction of human placenta (for the method see [24]; data not given).…”

Section: Reduction Of the E 2 Plasma Level By Meso-3-ptsomentioning

confidence: 99%

“…The preparation of the microsomes was performed according to the method of Brodie et al [23]. The tissue was homogenized in 8.0 mL ice-cold phosphate/sucrose buffer.…”

Section: Preparation Of Ovarian Microsomesmentioning

confidence: 99%

[1, 2‐Bis(2, 6‐difluoro‐3‐hydroxyphenyl)ethylene‐diamine]platinum(II) Complexes, Compounds for the Endocrine Therapy of Breast Cancer ‐ Mode of Action I: Antitumor Activity Due to the Reduction of the Endogenous Estrogen Level

Schertl

Hartmann

Batzl‐Hartmann

et al. 2004

Archiv der Pharmazie

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Aqua[meso-1, 2-bis(2, 6-difluoro-3-hydroxyphenyl)ethylenediamine]sulfatoplatinum(II) (meso-3-PtSO(4)) and its racemate (rac-3-PtSO(4)) are highly active on the hormone-sensitive MXT-M-3, 2 breast cancer of the mouse. In vitro, on the MXT(+) cell culture derived from this tumor, however, they are inactive (meso-3-PtSO(4)) or moderately active (rac-3-PtSO(4)) in concentrations corresponding to levels of these drugs in animal experiments. The in vivo effect is mainly caused by a reduction of the endogenous estrogen level in the host animals due to an interference with the ovarian steroid biosynthesis as demonstrated for meso-3-PtSO(4). Therefore, a reversal of the breast cancer inhibiting effect of meso-3-PtSO(4) can be achieved by simultaneous estrone administration. Histological results on ovaries, uterus, and tumor of meso-3-PtSO(4)-treated mice also favor such a mode of action. However, especially for rac-3-PtSO(4) cytotoxic effects contributing to the anti-breast cancer activity cannot be excluded. Considerations on the mode of action of Pt-complexes which inhibit breast cancer by interference with estrogen receptor mediated processes of growth control and with DNA replication are presented.

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“…These compounds were substrate analogs and exhibited properties typical of competitive inhibitors. They included l,4,6-androstatriene-3,17-dione [47] 4-hydroxyandrostenedione (4-OHA) [48] and 4-acetoxyandrostenedione [49]. Interestingly, some of these inhibitors were later found to cause inactivation of the enzyme [28] and appear to be functioning as mechanism-based inhibitors.…”

Section: Steroidal Aromatase Inhibitorsmentioning

confidence: 99%

Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer

Jordan¹,

Brodie²

2007

Steroids

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183

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The enthusiasm with which the clinical community has embraced the use of antiestrogenic therapy to treat breast cancer is based upon the proven record of success that first the nonsteroidal antiestrogen tamoxifen and then the aromatase inhibitor have demonstrated in clinical trial. The reasons for the enthusiasm are obvious. Antihormonal therapy, particularly aromatase inhibition to create a "no estrogen state" in the postmenopausal breast cancer patient is effective, saves women's lives, is contributing successfully to reducing the national mortality from breast cancer, is relatively cheap and has fewer side effects and easy administration (oral) than any other anticancer strategy. However, the successful application of a therapeutic strategy to block the known growth stimulation property of estrogen in breast cancer was not greeted with such enthusiasm 40 years ago.Estrogen is essential for life. Without the critical role of estrogenic steroids, reproduction would not be possible. Based on emerging knowledge from laboratory studies, the value of modulating the steroid environment during the menstrual cycle was advanced to clinical testing during the 1950's as a means of oral contraception. The results of these studies were to change society forever.The Worcester Foundation for Experimental Biology is the place where Gregory Pincus established the scientific principles necessary to propose clinical testing of the oral contraceptive and M.C. Chang subsequently established the first protocols to perform in vitro fertilization. Simply stated, the Worcester Foundation was, at that time, the world center for steroid endocrinology and reproductive biology. Over the years, hundreds of scientists have trained at the Foundation and subsequently spread their knowledge throughout the world [1]. However, fashions in research change and new opportunities emerge.In 1971, President Nixon made a national commitment to seek a cure for cancer by signing the National Cancer Act. Mahlon Hoagland, the President of the Worcester Foundation, responded to the initiative by appointing Professor Elwood V. Jensen, Director of the Ben May Cancer Research Laboratory at the University of Chicago, to be a member of the Foundation's Scientific Advisory Board. Jensen had discovered the estrogen receptor (ER) as the putative mechanism of estrogen action in its target tissues [2]. The known link between estrogen and breast cancer suggested that "antiestrogenic strategies" might have potential as therapeutic Correspondence to: V. Craig Jordan, v.craig.jordan@fccc.edu. Present Address: Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA 19111-2497 Publisher's Disclaimer: This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final citable form. Please note that during the production process errors may be d...

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Studies on the mechanism of estrogen biosynthesis in the rat ovary–I

Cited by 109 publications

References 14 publications

Evaluation of biological activity of new hemiesters of 17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile

Evaluation of biological activity of new hemiesters of 17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile

[1, 2‐Bis(2, 6‐difluoro‐3‐hydroxyphenyl)ethylene‐diamine]platinum(II) Complexes, Compounds for the Endocrine Therapy of Breast Cancer ‐ Mode of Action I: Antitumor Activity Due to the Reduction of the Endogenous Estrogen Level

Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer

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