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Identification of pathway-selective estrogen receptor ligands that inhibit NF-kappaB transcriptional activity. 2005
Christopher C Chadwick, and
Susan Chippari, and
Edward Matelan, and
Lisa Borges-Marcucci, and
Amy M Eckert, and
James C Keith, and
Leo M Albert, and
Yelena Leathurby, and
Heather A Harris, and
Ramesh A Bhat, and
Mark Ashwell, and
Eugene Trybulski, and
Richard C Winneker, and
Steven J Adelman, and
Robert J Steffan, and
Douglas C Harnish
Women's Health Research Institute and Departmens of Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
Inflammation is now recognized as a key component in a number of diseases such as atherosclerosis, rheumatoid arthritis, and inflammatory bowel disease. The transcription factor NF-kappaB has been shown to be involved in both the early and late stages of the inflammatory-proliferative process. In this report, we describe the identification of the pathway-selective estrogen receptor (ER) ligand, WAY-169916, that inhibits NF-kappaB transcriptional activity but is devoid of conventional estrogenic activity. This pathway-selective ligand does not promote the classic actions of estrogens such as stimulation of uterine proliferation or ER-mediated gene expression, but is a potent antiinflammatory agent, as demonstrated in the HLA-B27 transgenic rat model of inflammatory bowel disease. Our results indicate the potential utility of pathway-selective ER ligands such as WAY-169916 in the treatment of chronic inflammatory diseases.
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