Current Progresses and Trends in the Development of Progesterone Receptor Modulators

Keywords: Agonist, Antagonist, Ligand, Modulator, Nonsteroid, Progesterone receptor, Steroid. Current Medicinal Chemistry Title:Current Progresses and Trends in the Development of Progesterone Receptor Modulators Volume: 23 Issue: 23 Author(s): Wenlu Li, Xi Li, Bin Zhang, Chunmei Gao, Yuzong Chen and Yuyang Jiang Affiliation:

Agonist, Antagonist, Ligand, Modulator, Nonsteroid, Progesterone receptor, Steroid.

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. Export Options About this article Cite this article as: Li Wenlu, Li Xi, Zhang Bin, Gao Chunmei, Chen Yuzong and Jiang Yuyang, Current Progresses and Trends in the Development of Progesterone Receptor Modulators, Current Medicinal Chemistry 2016; 23 (23) . https://dx.doi.org/10.2174/0929867323666160428105310 | DOI https://dx.doi.org/10.2174/0929867323666160428105310 | Print ISSN 0929-8673 | | Publisher Name Bentham Science Publishers | Online ISSN 1875-533X | Call for Papers in Thematic Issues Advance in Novel Drug and combined Therapies for Chronic Diseases Chronic diseases such as malignant tumors and rheumatoid arthritis have long plagued a large number of patients. 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