 | SELECTIVE ESTROGEN RECEPTOR MODULATORS (SERMs)
Copyright © 2001 by the New York Academy of Sciences
description
Annals of the New York Academy of Sciences 949:16-35 (2001)
© 2001 New York Academy of Sciences
Capitalizing on the Complexities of Estrogen Receptor Pharmacology in the Quest for the Perfect SERM
DONALD P. McDONNELL,
CHING-YI CHANG AND
JOHN D. NORRIS
Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
Address for correspondence: Dr. Donald P. McDonnell, Department of Pharmacology and Cancer Biology, Duke University Medical Center, Box 3813, Durham, NC 27710. Voice: 919-684-6035; fax: 919-681-7139.
donald.mcdonnell{at}duke.edu
The term Selective Estrogen Receptor Modulators (SERMs) has been used of late to describe a group of pharmaceuticals that manifest estrogen receptor (ER) agonist activity in some tissues, but that oppose estrogen action in others. Whereas the name describing this class of drugs is new, the concept is not. Indeed, compounds exhibiting tissue-selective ER agonist/antagonist properties have been around for nearly 40 years. What is new is the idea that it may be possible to capitalize on the paradoxical activities of these drugs and develop them as treatments for estrogenopathies where it is desirable to direct therapy to a specific estrogen-responsive target organ. This realization has provided the impetus for research in this area and has pushed the development and clinical use of this class of drugs. The objective of this review is to describe how the medical need for SERMs arose and how recent studies of the mechanism of action of the currently available drugs are paving the way for the development of novel drugs with improved selectivity.
Key Words: ER  • ERß • SERMs • tamoxifen • LXXLL-containing peptides
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