| Autor: |
Chadwick CC; Women's Health Research Institute and Departmens of Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA., Chippari S, Matelan E, Borges-Marcucci L, Eckert AM, Keith JC Jr, Albert LM, Leathurby Y, Harris HA, Bhat RA, Ashwell M, Trybulski E, Winneker RC, Adelman SJ, Steffan RJ, Harnish DC |
| Jazyk: |
angličtina |
| Zdroj: |
Proceedings of the National Academy of Sciences of the United States of America [Proc Natl Acad Sci U S A] 2005 Feb 15; Vol. 102 (7), pp. 2543-8. Date of Electronic Publication: 2005 Feb 07. |
| DOI: |
10.1073/pnas.0405841102 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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