Curr Opin Drug Discov Devel. 2000 Jul;3(4):383-98.
Current opinion in drug discovery & development
X Lin, V Huebner
PMID: 19649870
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.
