RGD Reference Report - Evaluation of an estrogen receptor-beta agonist in animal models of human disease. - Rat Genome Database

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Evaluation of an estrogen receptor-beta agonist in animal models of human disease.

Authors: Harris, HA  Albert, LM  Leathurby, Y  Malamas, MS  Mewshaw, RE  Miller, CP  Kharode, YP  Marzolf, J  Komm, BS  Winneker, RC  Frail, DE  Henderson, RA  Zhu, Y  Keith JC, JR 
Citation: Harris HA, etal., Endocrinology. 2003 Oct;144(10):4241-9.
RGD ID: 5509042
Pubmed: PMID:14500559   (View Abstract at PubMed)
DOI: DOI:10.1210/en.2003-0550   (Journal Full-text)

The discovery of a second estrogen receptor (ER), called ERbeta, in 1996 sparked intense interest within the scientific community to discover its role in mediating estrogen action. However, despite more than 6 yr of research into the function of this receptor, its physiological role in mediating estrogen action remains unclear and controversial. We have developed a series of highly selective agonists for ERbeta and have characterized their activity in several clinically relevant rodent models of human disease. The activity of one such compound, ERB-041, is reported here. We conclude from these studies that ERbeta does not mediate the bone-sparing activity of estrogen on the rat skeleton and that it does not affect ovulation or ovariectomy-induced weight gain. In addition, these compounds are nonuterotrophic and nonmammotrophic. However, ERB-041 has a dramatic beneficial effect in the HLA-B27 transgenic rat model of inflammatory bowel disease and the Lewis rat adjuvant-induced arthritis model. Daily oral doses as low as 1 mg/kg reverse the chronic diarrhea of HLA-B27 transgenic rats and dramatically improve histological disease scores in the colon. The same dosing regimen in the therapeutic adjuvant-induced arthritis model reduces joint scores from 12 (maximal inflammation) to 1 over a period of 10 d. Synovitis and Mankin (articular cartilage) histological scores are also significantly lowered (50-75%). These data suggest that one function of ERbeta may be to modulate the immune response, and that ERbeta-selective ligands may be therapeutically useful agents to treat chronic intestinal and joint inflammation.




  
Object Symbol
Species
Term
Qualifier
Evidence
With
Notes
Source
Original Reference(s)
ESR2Humaninflammatory bowel disease  ISOEsr2 (Rattus norvegicus) RGD 
Esr2Ratinflammatory bowel disease  IDA  RGD 
Esr2Mouseinflammatory bowel disease  ISOEsr2 (Rattus norvegicus) RGD 


Genes (Rattus norvegicus)
Esr2  (estrogen receptor 2)

Genes (Mus musculus)
Esr2  (estrogen receptor 2 (beta))

Genes (Homo sapiens)
ESR2  (estrogen receptor 2)