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Updated: Jun 21, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Non-steroidal ligands for steroid hormone receptors
1Chiron Corporation, Small Molecule Drug Discovery, Emeryville, CA 94608, USA. xiaodong_lin@cc.chiron.com
Abstract:
Nuclear hormone receptors play important roles in many physiological events. Small molecules, ie, ligands, can regulate these physiological effects by binding to the receptors forming a ligand-receptor complex, which in turn triggers a cascade of transcriptional events. Over the years, non-steroidal ligands for steroid receptors have been developed and have found extensive clinical use in cancer treatment, fertility regulation and hormone replacement therapy. This review summarizes the recent progress in the identification of pharmacologically relevant non-steroidal ligands for steroid receptors, focusing on the estrogen receptor (ER), the progesterone receptor (PR) and the androgen receptor (AR). The ligands are selected for discussion based on their clinical status, pharmacological profile and structural novelty, and range from compounds launched extensively to those in the early discovery stage.
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