The antisteroid RU486 its cellular and molecular mode of action

EE Baulieu - Trends in Endocrinology & Metabolism, 1991 - Elsevier
EE Baulieu
Trends in Endocrinology & Metabolism, 1991Elsevier
RU486 is a very powerful antisteroid hormone compound, with antiprogestin and
antiglucocorticosteroid clinical applications. High-affinity binding to the receptor ligand-
binding domain results in essentially antagonistic function; however, some agonistlike
effects have been observed. This review discusses the implications of recent discoveries
concerning hsp90 (heat-shock protein M r≈ 90,000)-receptor interaction, receptor-DNA
binding, and the involvement of transcription factors in the mechanism of action of RU486.
Abstract
RU486 is a very powerful antisteroid hormone compound, with antiprogestin and antiglucocorticosteroid clinical applications. High-affinity binding to the receptor ligand-binding domain results in essentially antagonistic function; however, some agonistlike effects have been observed. This review discusses the implications of recent discoveries concerning hsp90 (heat-shock protein Mr≈90,000)-receptor interaction, receptor-DNA binding, and the involvement of transcription factors in the mechanism of action of RU486.
Elsevier