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National Institute of Environmental Health Sciences

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Publication Detail

Title: Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G.

Authors: Zhao, Zibo; Wang, Lu; James, Taryn; Jung, Youngeun; Kim, Ikyon; Tan, Renxiang; Hoffmann, F Michael; Xu, Wei

Published In Chem Biol, (2015 Dec 17)

Abstract: ERβ is regarded as a "tumor suppressor" in breast cancer due to its anti-proliferative effects. However, unlike ERα, ERβ has not been developed as a therapeutic target in breast cancer due to loss of ERβ in aggressive cancers. In a small-molecule library screen for ERβ stabilizers, we identified Diptoindonesin G (Dip G), which significantly increases ERβ protein stability while decreasing ERα protein levels. Dip G enhances the transcription and anti-proliferative activities of ERβ, while attenuating the transcription and proliferative effects of ERα. Further investigation revealed that instead of targeting ER, Dip G targets the CHIP E3 ubiquitin ligase shared by ERα and ERβ. Thus, Dip G is a dual-functional moiety that reciprocally controls ERα and ERβ protein stability and activities via an indirect mechanism. The ERβ stabilization effects of Dip G may enable the development of ERβ-targeted therapies for human breast cancers.

PubMed ID: 26670079 Exiting the NIEHS site

MeSH Terms: No MeSH terms associated with this publication

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