Tissue-Specific Estrogen Action: Novel Mechanisms, Novel Ligands, Novel Therapies(2006/1 Ernst Schering Foundation Symposium Proceedings)

Nuclear hormone receptors are not only important drug targets, but have also been the focus of decades of active and highly insightful research. Ten years ago, a review on nuclear receptors was entitled “The Second Decade” and a special issue of Molecular Endocrinology in 2005 dealt with the results of these research efforts. The consensus from nuclear receptor research was of course that the signaling pathways mediated by these receptors warrant further research, even though in principle they appeared to represent the most immediate, seemingly simple signaling pathway from hormone (ligand) binding to gene expression changes. In nuclear receptor molecular biology, estrogen receptor research has additional unique facets: since the discovery of ethinyl estradiol by Inhoffen and Hohlweg in the laboratories of Schering AG in the 1930s—and therefore several decades longer than nuclear receptor - searchitself—estrogenreceptorshavebeentargetsofwidelyused,orally administered drugs. Thus, accumulating clinical experience on estrogen action in vivo helps to support the progress in molecular biological research.

Table of Contents:
Interfering with the Dynamics of Estrogen Receptor-Regulated Transcription.- Actions of Estrogen and Estrogen Receptors in Nonclassical Target Tissues.- Genetic Dissection of Estrogen Receptor Signaling In Vivo.- Of Mice and Men: The Many Guises of Estrogens.- Estradiol Action in Atherosclerosis and Reendothelialization.- Functional Effects and Molecular Mechanisms of Subtype-Selective ER? and ER? Agonists in the Cardiovascular System.- Pathogenesis and Therapy of Rheumatoid Arthritis.- The Role of ER? and ER? in theProstate: Insights from Genetic Models and Isoform-Selective Ligands.- Preclinical Characterization of Selective Estrogen Receptor ? Agonists: New Insights into Their Therapeutic Potential.- Exploiting Nongenomic Estrogen Receptor-Mediated Signaling for the Development of Pathway-Selective Estrogen Receptor Ligands.

Review :
From the reviews: "This summation of a symposium discusses some of the new research developments and estrogen-receptor based therapies that are being tested in the laboratory and in current use. ... It is written for researchers, physician scientists, and those interested in estrogen receptor interactions at a molecular level. Hopefully, it can also stimulate interest in and future research by graduate students or clinical/basic researchers." (Amber R. Cooper, Doody's Review Service, January 2008)