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Human Reproduction, Vol. 9, No. suppl_1, pp. 7-11, 1994
© 1994 European Society of Human Reproduction and Embryology

The progesterone receptor. Biological effects of progestins and antiprogestins

J.F. Savouret, A. Chauchereau, M. Misrahi, P. Lescop, A. Mantel, A. Bailly and E. Milgrom1

Institut National de la Santé et de la Recherche Médicale Unité 135, Hormones et Reproduction, Hôpital de Bicêtre, 94276 Bicêtre Cedex, France

Correspondence: 1To whom correspondence should be addressed

The progesterone receptor displays the typical three-domains structure of the steroid–thyroid receptor family. The central domain contains two ‘zinc finger’ structures responsible for the specific recognition of the cognate DNA sequences. The carboxy-terminal domain contains the hormone and anti-hormone binding site. Progesterone and synthetic progestins (R5020, Org 2058) activate the receptor, provoke its phosphorylation and DNA-binding ability and induce its regulatory activities. The antagonist RU38486 elicits the same sequence of events but leads to an abortive conclusion without specific gene transactivation. The progesterone receptor is down-regulated by its own ligand at the transcriptional level through inhibition of oestrogen receptor-mediated induction through protein–protein interactions. This mechanism is also inhibited by RU38486.

Key words: anti-hormones/gene regulation/phosphorylation/progesterone receptor/progestins


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