Methods for screening for progesterone receptor isoform-specific ligands and tissue-selective progesterone receptor ligands

摘要

The present invention provides a method for screening for progesterone receptor isoform specific ligands as well as a first method for screening for tissue-selective progesterone receptor ligands, both methods comprising selecting progesterone receptor isoform A or progesterone receptor isoform B selective ligands by means of an assay involving cells stably transfected with plasmids expressing the progesterone receptor isoform A or B. Furthermore, the present invention provides a second method for screening for tissue-selective progesterone receptor ligands, comprising in vivo tests in desired target tissues. The present invention also relates to the progesterone receptor isoform specific and/or tissue-selective ligands identified through the methods according to the present invention. The present invention further relates to cell lines suitable for this transactivation assay, a respective assay kit and medical uses of the isoform-specific and/or tissue-selective progesterone receptor ligands according to the present invention.