ArticleChemistry & biology2015
Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G.
Article in Chemistry & biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
18 citing papers in PubMed, 36 citations in OpenAlex.
- Estrogen-mediated NF-κB blockade enables breast cancer sensitivity to oncolytic VSV virotherapy.Molecular therapy : the journal of the American Society of Gene Therapy · 2026Article
- Article
- Diptoindonesin G antagonizes AR signaling and enhances the efficacy of antiandrogen therapy in prostate cancer.The Prostate · 2022Article
- Steroid sulfatase deficiency causes cellular senescence and abnormal differentiation by inducing Yippee-like 3 expression in human keratinocytes.Scientific reports · 2021Article
- Triggering a switch from basal- to luminal-like breast cancer subtype by the small-molecule diptoindonesin G via induction of GABARAPL1.Cell death & disease · 2020Article
- The Relationship between Estrogen-Related Signaling and Human Papillomavirus Positive Cancers.Pathogens (Basel, Switzerland) · 2020Review
- Estrogen Receptor Beta (ERβ): A Ligand Activated Tumor Suppressor.Frontiers in oncology · 2020Review
- BAG2-Mediated Inhibition of CHIP Expression and Overexpression of MDM2 Contribute to the Initiation of Endometriosis by Modulating Estrogen Receptor Status.Frontiers in cell and developmental biology · 2020Article
- Overexpression Of ERβ Participates In The Progression Of Liver Cancer Via Inhibiting The Notch Signaling Pathway.OncoTargets and therapy · 2019Article
- Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation.Molecules (Basel, Switzerland) · 2018Review
- Concomitant high expression of ERα36, EGFR and HER2 is associated with aggressive behaviors of papillary thyroid carcinomas.Scientific reports · 2017Article
- Diptoindonesin G promotes ERK-mediated nuclear translocation of p-STAT1 (Ser727) and cell differentiation in AML cells.Cell death & disease · 2017Article
- Musashi RNA-binding protein 2 regulates estrogen receptor 1 function in breast cancer.Oncogene · 2017Article
- Targeted Protein Degradation by Small Molecules.Annual review of pharmacology and toxicology · 2017Review
- Total Synthesis of Viniferifuran, Resveratrol-Piceatannol Hybrid, Anigopreissin A and Analogues - Investigation of Demethylation Strategies.Advanced synthesis & catalysis · 2016Article
- Differential Impacts of Alternative Splicing Networks on Apoptosis.International journal of molecular sciences · 2016Review
- Total synthesis of diptoindonesin G and its analogues as selective modulators of estrogen receptors.Organic & biomolecular chemistry · 2016Article
- Symmetry-based approach to oligostilbenoids: Rapid entry to viniferifuran, shoreaphenol, malibatol A, and diptoindonesin G.Beilstein journal of organic chemistry · 2016Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 3 countries.
Funding
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.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.