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Review
. 2006;6(2):103-11.
doi: 10.2174/156802606775270279.

Control of Chronic Inflammation With Pathway Selective Estrogen Receptor Ligands

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Review

Control of Chronic Inflammation With Pathway Selective Estrogen Receptor Ligands

Robert J Steffan et al. Curr Top Med Chem. .

Abstract

The discovery of novel intervention points in the inflammatory pathway has been a focus of drug development in recent years. We have identified pathway selective ligands for the estrogen receptor (ER) that inhibit NF-kappaB mediated inflammatory gene expression causing a reduction of cytokines, chemokines, adhesion molecules and inflammatory enzymes. SAR development of a series of 4-(Indazol-3-yl)-phenols has led to the identification of WAY-169916 an orally active non-steroidal ligand with the potential use in the treatment of inflammatory diseases without the classical proliferative effects associated with non-selective estrogens.

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