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Submitted on May 17, 2005
Accepted on October 26, 2005
selective agonist ERB-041
Biological Technologies, Wyeth Research, Cambridge MA 02140. Caprion Pharmaceuticals, Montreal, Quebec H4S 2C8. Cardiovascular and Metabolic Diseases, Wyeth Research, Cambridge MA 02140. Women's Health Research Institute, Wyeth Research, Collegeville PA 19426
* To whom correspondence should be addressed. E-mail: harrish{at}wyeth.com.
Two receptors (ER
and ER
) mediate the manifold effects of estrogens throughout the body. Although a clear role has been established for ER in mediation of the classical effects of estrogen activity, the physiological role of ER is less well understood. A small molecule ER selective agonist, ERB-041, has potent anti-inflammatory activity in the Lewis rat model of adjuvant-induced arthritis (AIA). To characterize the response of target organs and pathways responsible for this anti-inflammatory effect, mRNA expression profiling of the spleen, lymph node and liver was performed, in conjunction with a global analysis of the plasma proteome. We find that the expression of a large number of genes and proteins are altered in the disease model and the majority of these are partially or fully reversed by ERB-041 treatment. Regulated pathways include the acute phase response, eicosinoid synthesis, fatty acid metabolism and iron metabolism. In addition, many of the regulated genes and proteins are known to be dysregulated in human rheumatoid arthritis, providing further evidence that the manifestations of the Lewis rat AIA model bear similarity to the human disease.
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