Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators

2011/03/01 by Camillo Rosano, Emilia Stec‐Martyna, Rosamaria Lappano +1 · 2 citations
Biochemistry, Genetics and Molecular Biology · Computer Science · #Estrogen and related hormone effects #Computational Drug Discovery Methods #Steroid Chemistry and Biochemistry

paper · doi:10.2174/092986711795029645

openalex publication_date 2011/03/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/31

Abstract

In the last twenty years the efforts to design and optimize new drugs have been based on the three dimensional structure of the selected target proteins. In this regard, useful information has been achieved mainly by protein crystallography, which has recently turned from a low into a high-throughput process thanks to the improvement in robot technologies, automation procedure and the use of synchrotron radiation facilities [1-3]. This review examines the impact of Structure Based Drug Design (SBDD) on the discovery of ligands as the selective estrogen receptor modulators (SERMs) of the Estrogen Receptor (ER)α, which is involved in the regulation of several physiological and pathological processes. Keywords: Structure based drug design, estrogen, estrogen receptor, lasofoxifene, raloxifene, tamoxifen, SERMs, ADME, DNA, ligand binding domain

Citations

• Structure–function relationship of estrogen receptor α and β: Impact on human health
• Estrogen receptors and human disease
• Cloning of a novel receptor expressed in rat prostate and ovary.
• Comparison of the Ligand Binding Specificity and Transcript Tissue Distribution of Estrogen Receptors α and β
• The crystal structure of the estrogen receptor DNA-binding domain bound to DNA: How receptors discriminate between their response elements

Cited by

• The Discovery and Development of Selective Estrogen Receptor Modulators (SERMs) for Clinical Practice
• Selective estrogen receptor modulator [wikipedia]