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Inhibition of growth by the antihormone RU486 in different hepatoma cell lines

Authors
Journal
Molecular and Cellular Endocrinology
0303-7207
Publisher
Elsevier
Publication Date
Volume
82
Identifiers
DOI: 10.1016/0303-7207(91)90026-o
Keywords
  • Antiglucocorticoid
  • Metabolization
  • Antiproliferative Effect
  • Glucocorticoid Receptor

Abstract

Abstract The synthetic steroid RU486 (17)β-hydroxy-11β-(4-dimethylaminophenyl)-17α-(1-propynyl)-estra-4, 9-dien-3-one), which has been shown to display antiprogestin and antiglucocorticoid properties in different systems, exerts antiglucocorticoid effects and inhibits the cell growth in a concentration-dependent manner on Reuber rat hepatoma cell variants. This effect can be observed on glucocorticoid-sensitive cells, containing glucocorticoid receptors, and on glucocorticoid-resistant cells displaying a very low level of dexamethasone binding. Metabolization of RU486 occurs in different glucocorticoid-resistant hepatoma variants; these cells are less sensitive to the growth inhibitory effect of the antihormone than the steroid-sensitive cells which do not metabolize RU486. Thus, metabolization of RU486 must also be taken into account for the efficacy of this antagonist on cell growth.

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