Journal article

Drug and Cell Type-Specific Regulation of Genes with Different Classes of Estrogen Receptor beta-Selective Agonists

Sreenivasan Paruthiyil, Aleksandra Cvoro, Xiaoyue Zhao, Zhijin Wu, Yunxia Sui, Richard E Staub, Scott Baggett, Candice B Herber, Chandi Griffin, Mary Tagliaferri, Heather A Harris, Isaac Cohen, Leonard F Bjeldanes, Terence P Speed, Fred Schaufele, Dale C Leitman



Estrogens produce biological effects by interacting with two estrogen receptors, ERalpha and ERbeta. Drugs that selectively target ERalpha or ERbeta might be safer for conditions that have been traditionally treated with non-selective estrogens. Several synthetic and natural ERbeta-selective compounds have been identified. One class of ERbeta-selective agonists is represented by ERB-041 (WAY-202041) which binds to ERbeta much greater than ERalpha. A second class of ERbeta-selective agonists derived from plants include MF101, nyasol and liquiritigenin that bind similarly to both ERs, but only activate transcription with ERbeta. Diarylpropionitrile represents a third class of ERbeta-selective ..

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University of Melbourne Researchers