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Can I read New ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein–Protein Interaction on EtoBox?
New ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein–Protein Interaction by Zhen Wang; Min Zhang; Harriet M. Thompson; Haitao Ji is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is New ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein–Protein Interaction about?
A series of 1-(3-(2-amino-2-oxoethoxy)phenyl)piperidine-3-carboxamide derivatives was reported as new smallmolecule β-catenin/B-cell lymphoma 9 (BCL9) protein-protein interaction (PPI) inhibitors. Compounds 17-21 were discovered to inhibit the β-catenin/BCL9 PPI with K i = 0.85-2.7 μM. The effects of 21 on the β-catenin/BCL9 PPI in cellular context were demonstrated by β-catenin/BCL9 pull-down inhibition and dosedependent suppression of Wnt/β-catenin signal transactivation. Notably, compound 21 is more potent than ZW4864, a previously reported analogue, in modulating transcription and expression of β-catenin target genes and suppressing survival of β-catenin-dependent cancer cells. The cellular on-target efficacy of 21 was demonstrated by β-catenin rescue experiments. Compound 21 represents a promising starting point for further optimization of βcatenin/BCL9 PPI inhibitors.
Who reads New ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein–Protein Interaction?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Zhen Wang; Min Zhang; Harriet M. Thompson; Haitao Ji
- Publisher
- American Chemical Society (ACS)
- Published
- 2022
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)