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Inhibition of estrone sulfatase enzyme in human placenta and human breast carcinoma

Evans, T.R.Jeffry ; Rowlands, Martin G. ; Jarman, Michael ; Coombes, R.Charles

The Journal of steroid biochemistry and molecular biology, 1991-10, Vol.39 (4), p.493-499 [Periódico revisado por pares]

Oxford: Elsevier Ltd

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Título:
Inhibition of estrone sulfatase enzyme in human placenta and human breast carcinoma
Autor: Evans, T.R.Jeffry ; Rowlands, Martin G. ; Jarman, Michael ; Coombes, R.Charles
Assuntos: Analytical, structural and metabolic biochemistry ; Androgens - pharmacology ; Biological and medical sciences ; Breast Neoplasms - enzymology ; Cell Nucleus - enzymology ; Danazol - pharmacology ; Enzymes and enzyme inhibitors ; Estrogen Antagonists - pharmacology ; Estrogens - pharmacology ; Female ; Fundamental and applied biological sciences. Psychology ; Humans ; Hydrolases ; Kinetics ; Microsomes - enzymology ; Mitochondria - enzymology ; Placenta - enzymology ; Pregnancy ; Substrate Specificity ; Sulfatases - antagonists & inhibitors
É parte de: The Journal of steroid biochemistry and molecular biology, 1991-10, Vol.39 (4), p.493-499
Notas: ObjectType-Article-2
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Descrição: Estrone sulfatase is an important mechanism of local synthesis of biologically active estrogens in human breast cancer. The human placental microsome and breast carcinoma mitochondrial/microsomal estrone sulfatase activity were characterized and inhibition studies performed. The K m of the placental tissue enzyme was 6.83 μM, V max 0.015 nmol/min/mg, and for the breast carcinoma tissue K m was 8.91 μM and V max 0.022 nmol/min/mg. Danazol produced a significant inhibition of estrone sulfatase (20% with 50 μM danazol). No significant inhibition was seen in the presence of aminoglutethimide, rogletimide, tamoxifen, 4-hydroxyandrostenedione, stilboestrol, or any metabolites of danazol or tamoxifen. Studies with synthetic and naturally occuring steroids demonstrated that the presence of a sulfate group at the 3 position to be the most important factor in determining inhibition, and the most potent inhibitor was 5α-androstene-3β, 17β-diol-3-sulfate ( K i of 2.0 μM). The naturally occuring 3-sulfated steroids all demonstrated competitive inhibition. These studies could form the basis for the design of a potent estrone sulfatase inhibitor which would have potential therapeutic activity in the management of breast cancer.
Editor: Oxford: Elsevier Ltd
Idioma: Inglês

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Inhibition of estrone sulfatase enzyme in human placenta and human breast carcinoma

Evans, T.R.Jeffry ; Rowlands, Martin G. ; Jarman, Michael ; Coombes, R.Charles

Oxford: Elsevier Ltd

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