The progesterone receptor (PR) is a ligand-activated steroid receptor in the nuclear
receptor (NR) superfamily of transcription factor. Besides gynecological and obstetrical
indications, the involvement/mechanism of PR in many other diseases, such as oncology,
neurology, immunology, etc. has been revealed and studied in recent decades. Therapeutic agents
that selectively activate or inhibit PR have been developed. PR agonists have generally been used
in oral contraception and postmenopausal hormone replacement therapy (HRT), typically in
combination with estrogens. PR antagonists and selective PR modulators (SPRMs) can be useful
therapies for hormone dependent breast and prostate cancers, nonmalignant chronic conditions
such as fibroids, and endometriosis. This review provides an overview and detailed discussions
about the recent development of chemical structures of the PR ligands, their structural
characteristics (particularly those contributing to their activity and selectivity), in vitro/in vivo
studies and clinical trial outcomes, and the synthetic methodologies.
Keywords: Agonist, Antagonist, Ligand, Modulator, Nonsteroid, Progesterone receptor, Steroid.
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