Selective Estrogen-Receptor Modulators — Mechanisms of Action and Application to Clinical Practice

2003/02/13 by B. Lawrence Riggs, Lynn C. Hartmann · 4 citations
Biochemistry, Genetics and Molecular Biology · Medicine · #Estrogen and related hormone effects #Menopause: Health Impacts and Treatments #Inflammatory mediators and NSAID effects

paper · doi:10.1056/nejmra022219

openalex publication_date 2003/02/13 · openalex created_date 2025/10/10 · openalex updated_date 2026/08/01

Abstract

The selective estrogen-receptor modulators, or SERMs, chemically diverse nonsteroid compounds, have tertiary structures that permit binding to the estrogen receptor. These compounds have either selective agonist or antagonist effects, depending on the target tissue. This article reviews current information concerning the molecular basis of SERM action and the tissue-selective agonist–antagonist effects of this class of medication. The article also offers a perspective on the therapeutic uses of SERMs and compares the SERMs with estrogen and nonestrogen alternatives.

Citations

• Molecular Determinants for the Tissue Specificity of SERMs
• Estrogen Receptor Null Mice: What Have We Learned and Where Will They Lead Us?
• Structural Insights into the Mode of Action of a Pure Antiestrogen
• Comparison of the Ligand Binding Specificity and Transcript Tissue Distribution of Estrogen Receptors α and β
• Molecular basis of agonism and antagonism in the oestrogen receptor
• The Structural Basis of Estrogen Receptor/Coactivator Recognition and the Antagonism of This Interaction by Tamoxifen
• Estrogen Receptor (ER)-β Reduces ERα-Regulated Gene Transcription, Supporting a “Ying Yang” Relationship between ERα and ERβ in Mice

Cited by

• Estrogen and selective estrogen receptor modulators (SERMs) for the treatment of acromegaly: a meta-analysis of published observational studies
• New insights into the molecular mechanisms underlying effects of estrogen on cholesterol gallstone formation
• Preclinical Characterization of a Novel Diphenyl Benzamide Selective ERα Agonist for Hormone Therapy in Prostate Cancer
• Selective estrogen receptor modulator [wikipedia]