Recent advances in estrogen receptor modulators.
Modulation of estrogen action is an effective treatment for alleviating the symptoms associated with menopause, and also provides an alternative to ablative surgery for the treatment of breast cancer. The side effects associated with the currently used estrogen receptor-modulating drugs have resulted in the pursuit of agents with an improved therapeutic profile. Recent advances in understanding the molecular determinants of estrogen receptor signaling have contributed to the continued discovery and development of novel chemical compounds designed to exploit this knowledge. This review focuses on the recent clinical and preclinical development of novel classes of ligands that modulate the two estrogen receptor subtypes.
Henke
Brad R
BR
GlaxoSmithKline Inc, Metabolic and Viral Diseases Drug Discovery, Research Triangle Park, PO Box 13398, NC 27705, USA. brad.r.henke@gsk.com
Heyer
Dennis
D
D000818:Animals; D006801:Humans; D008024:Ligands; D011960:Receptors, Estrogen / Q000819:agonists / Q000037:antagonists & inhibitors / Q000187:drug effects; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology* / Q000627:therapeutic use
D008024:Ligands; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators