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Direct antiproliferative effect of nonsteroidal 17β-hydroxysteroid dehydrogenase type 1 inhibitors in vitro.
Berényi, Agnes Frotscher, Martin Marchais-Oberwinkler, Sandrine Hartmann, Rolf W Minorics, Renáta Ocsovszki, Imre Falkay, George Zupkó, István
Berényi, Agnes
Frotscher, Martin
Marchais-Oberwinkler, Sandrine
Hartmann, Rolf W
Minorics, Renáta
Ocsovszki, Imre
Falkay, George
Zupkó, István
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2013-08
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Abstract
Inhibition of the local formation of estrogens seems to be an attractive strategy for pharmacological intervention in hormone-dependent disorders. The direct antiproliferative properties of ten nonsteroidal 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitors were investigated on human cancer cell lines of gynecological origin. The mechanism of the antiproliferative action was approximated by cell cycle analysis, fluorescent microscopy, BrdU assay, determination of caspase-3 activity and quantification of the expression of cell cycle regulators at mRNA level. Treatment of HeLa cells with some of the compounds resulted in a concentration-dependent inhibition of the G1-S transition and an increase in the apoptotic population. The most effective agents increased the expression of tumor suppressors p21 and p53, while CDK2 and Rb were down-regulated. The reported anticancer actions of the tested compounds are independent of the 17β-HSD1-inhibiting capacity. These results indicate that it is possible to combine direct antiproliferative activity and 17β-HSD1 inhibition resulting in novel agents with dual mode of action.
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Direct antiproliferative effect of nonsteroidal 17β-hydroxysteroid dehydrogenase type 1 inhibitors in vitro. 2013, 28 (4):695-703 J Enzyme Inhib Med Chem
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en
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1475-6374
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Archived with thanks to Journal of enzyme inhibition and medicinal chemistry