Estrogen receptor ligands in the control of pathogenic inflammation.
Inflammation is recognized as a key component in a number of diseases, including rheumatoid arthritis, inflammatory bowel disease and atherosclerosis. Although well known for their classic effects on the reproductive tract and action by means of estrogen response elements in gene promoters, estrogens are also known to possess anti-inflammatory activity. This was originally highlighted with the observation that pregnancy ameliorates symptoms of rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease. Furthermore, the antagonistic cross talk between nuclear factor kappaB and estrogen receptor signaling pathways has been well documented. Recently, novel estrogen receptor ligands, pathway-selective ligands and estrogen receptor beta-selective ligands have been identified which demonstrate potent anti-inflammatory activity; these ligands are being analyzed for their therapeutic potential in pathogenic inflammation.
Harnish
Douglas C
DC
Cardiovascular and Metabolic Disease Research, Wyeth Research, 500 Arcola Rd, Collegeville, PA 19246, USA. harnisd@wyeth.com
D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D004967:Estrogens / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D006801:Humans; D007249:Inflammation / Q000378:metabolism / Q000517:prevention & control*; D008024:Ligands; D015394:Molecular Structure; D016328:NF-kappa B / Q000378:metabolism; D016032:Randomized Controlled Trials as Topic; D011960:Receptors, Estrogen / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D004967:Estrogens; D008024:Ligands; D016328:NF-kappa B; D011960:Receptors, Estrogen