Related Experiment Video
Updated: Sep 30, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Elucidation of the molecular mechanism of action of selective estrogen receptor modulators
Donald P McDonnell1, Ashini Wijayaratne, Ching-yi Chang
1Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina 27710, USA. mcdonnell@duke.edu
Abstract:
The term selective estrogen receptor modulator (SERM) describes a group of pharmaceuticals that manifest estrogen receptor (ER) agonist activity in some tissues but opposes estrogen action in others. Although the name describing this class of drugs is new, the concept is not, as compounds exhibiting tissue-selective ER agonist/antagonist properties have been available for nearly 40 years. What is new is the idea that it may be possible to capitalize on the paradoxical activities of SERMs and develop them as target organ-selective ER agonists for the treatment of osteoporosis and other estrogenopathies. This realization has provided the impetus for research in this area, the progress of which is described in this review.
Related Concept Videos
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
E2 Reaction: Stereochemistry and Regiochemistry
When a substrate with two different β hydrogens undergoes an E2 elimination, the presence of a strong base can yield two regioisomeric alkenes. The more-substituted alkene is the major product and...
E1 Reaction: Stereochemistry and Regiochemistry

