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New agents display selectivity for estrogen receptor beta.(Brief Article)
2003 FEB 6 - (NewsRx.com & NewsRx.net) -- Researchers at a major drug firm have reported on a new line of estrogen receptor modulators with selectivity for estrogen receptor beta.
The scientists described "a series of 1,3,5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ER-beta subtype.
"Compound 1, which displayed modest potency and selectivity for ER-beta vs. ER-alpha, was identified via high-throughput screening utilizing an ER-beta SPA-based binding assay. Subsequent analogue preparation resulted in the identification of compounds such as 21 and 43 that display 25- to 30-fold selectivity for ER-beta with potencies in the 10-30 nM range," stated B.R. Henke and coauthors, GlaxoSmithKline.
"These compounds profile as full antagonists at ER-beta and weak partial agonists at ER-alpha in a cell-based reporter gene assay. In addition, the x-ray crystal structure of compound 15 complexed with the ...
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Source: HighBeam Research, New agents display selectivity for estrogen receptor beta.(Brief...