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Bionovo's Estrogen Receptor Beta Selective Drugs Have Unique Gene Expression and Cell Type Specificity Article Tools

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Bionovo, Inc. announced that a study of the gene regulation in multiple cell lines by several of their estrogen receptor beta (ERb) candidates will be published in Public Library of Science One.

"In this study we show that plant-derived ERb compounds are as selective as synthetic compounds, but regulate different genes. Specifically, we have discovered that these compounds do not promote breast or endometrial cancer in animal models, unlike many estrogen therapies. This suggests that these plant-derived ERb-selective compounds could lead to safer, more attractive alternative therapies for menopausal symptoms," said Dr. Dale Liftman, the Principal Investigator of the study.

The publication describes the analyses of three distinct classes of ERb selective drugs. The study determines the relative ER selectivity and pattern of gene expression of the three classes of ERb selective compounds compared to the natural hormone estradiol, which non-selectively regulates both ERa and ERb.

The most significant finding in the study was that the ERb-selective compounds regulate a number of genes differently than estradiol, a hormone therapy commonly used to treat women's health issues. This discovery indicates that ERb agonists might be safer than current estrogens used in hormone therapy.

The study also demonstrates the cell type selectivity of Menerba (MF101) and Liquiritigenin, two of Bionovo's ERb selective drugs, in different cell types. These compelling findings will serve as a strong impetus for Bionovo, Inc. to continue investigating the unique abilities of their drugs to safely and effectively treat menopausal symptoms.

"It is essential that new drug candidates demonstrate drug selectivity and tissue specificity in order to minimize adverse effects, particularly when the drug is being developed for the treatment of common, recurring symptoms associated with menopause, such as hot flashes. This is particularly important when developing drugs that mediate their effects through estrogen receptors, which are responsible for many functions in the body and are present in a range of different tissues. Bionovo stands alone in its dedication to identifying novel pathways in estrogen receptor signaling as drug targets for the treatment of women's conditions," said Isaac Cohen, Chairman and CEO of Bionovo, Inc.

"We have been endeavoring to develop more selective drugs in women's health, and Dr. Leitman's study highlights the solid scientific underpinnings of our ER beta selective drugs and underlines the deep biological understanding we have of the mechanisms through which they work."