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Updated: Jul 28, 2025

Reconstitution Of β-catenin Degradation In Xenopus Egg Extract
Published on: June 17, 2014
E7386 is not a Specific CBP/β-Catenin Antagonist
Yusuke Higuchi1, Cu Nguyen1, Nyam-Osor Chimge1
1Department of Cancer Biology and Molecular Medicine, Beckman Research Institute of City of Hope, Duarte, CA 91010, USA.
E7386 is not a specific CBP/β-catenin antagonist, unlike ICG-001 and C82. This study compared E7386 to established antagonists, finding it lacks specific CBP/β-catenin antagonism.
Area of Science:
- Biochemistry
- Molecular Biology
- Drug Discovery
Background:
- CBP/β-catenin antagonists target diseases of aging by regulating stem cells and metabolism.
- ICG-001 and C82 are well-studied specific CBP/β-catenin antagonists.
- PRI-724, an earlier antagonist, had limited oral bioavailability.
Purpose of the Study:
- To compare the novel, orally available E7386 with specific CBP/β-catenin antagonists ICG-001 and C82.
- To investigate the mechanism of action of E7386.
- To determine if E7386 is a specific CBP/β-catenin antagonist.
Main Methods:
- Utilized validated biochemical and transcriptional assays.
- Performed global transcriptional profiling.
- Compared three small molecules: ICG-001, C82, and E7386.
Main Results:
- E7386 demonstrated significant differences compared to ICG-001 and C82.
- Data strongly suggest E7386 does not specifically antagonize CBP/β-catenin.
Conclusions:
- E7386 is not a specific CBP/β-catenin antagonist.
- Further research is needed to elucidate E7386's mechanism of action.
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