Reciprocal Regulation of ER? and ER? Stability and Activity by Diptoindonesin G.
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ABSTRACT:
SUBMITTER: Zhao Z
PROVIDER: S-EPMC4767166 | biostudies-literature | 2015 Dec
REPOSITORIES: biostudies-literature
Publications
Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G.
Zhao Zibo Z Wang Lu L James Taryn T Jung Youngeun Y Kim Ikyon I Tan Renxiang R Hoffmann F Michael FM Xu Wei W
Chemistry & biology 20151203 12
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 attenua ...[more]
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