Direct targeting of β-catenin: Inhibition of protein–protein interactions for the inactivation of Wnt signaling
Open accessAbstract
The activation of developmental signaling pathways such as Notch, Hedgehog and Wnt has implications in the onset and progression of numerous types of cancer. Consequently, targeting of such pathways is considered an attractive therapeutic approach. Inhibition of the Wnt signaling cascade proves to be complicated, in part, due to the lack of druggable pathway components. The central hub in Wnt signaling is the protein β-catenin, which is involved in numerous protein-protein interactions. In general, the inhibition of protein-protein interactions is challenging in particular with binding interfaces lacking pronounced hydrophobic pockets. Herein, we give an overview of β-catenin-protein interactions, and we review active agents that were reported to inhibit canonical Wnt signaling via direct targeting of β-catenin.
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Wnt/β-Catenin Signaling Modulates Human Airway Sensitization Induced by β2-Adrenoceptor Stimulation
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Structure‐Based Design of Bicyclic Helical Peptides That Target the Oncogene β‐Catenin
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A Dominant Negative Antisense Approach Targeting β-Catenin
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From Protein Structures to Functional Biomimetics
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- Authors
- Hahne, G., & Grossmann, T. N.
- Affiliations
- Max Planck Society (DE)
- Corresponding author
- Grossmann, Tom N.
- ORCID
- Grossmann, Tom N.
- Venue
- Bioorganic & Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2013-07
- Volume
- 21
- Issue
- 14
- Pages
- 4020-4026
- ISSN
- 0968-0896 (ISSN-L)
- OpenAlex
- W1978927502
- Cited by
- 46
- References
- 62
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 5 · 2022: 3 · 2021: 5 · 2020: 3 · 2019: 3 · 2018: 5 · 2017: 3 · 2016: 3 · 2015: 7 · 2014: 5
- FWCI
- 2.39
- Type
- journal article
- Language
- en
- Open access
- green
- hdl.handle.net
- Locations
- Bioorganic & Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Max Planck Institute for Plasma Physics (submittedVersion)
- MPG.PuRe (Max Planck Society) (submittedVersion, cc-by)
- VU Research Portal (submittedVersion)
- Data Archiving and Networked Services (DANS) (submittedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Wnt/β-catenin signaling in development and cancer
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Signaling Pathways in Disease
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Hedgehog Signaling Pathway Studies
- Keywords
- β-catenin, Wnt signaling, protein-protein interaction inhibitors, Wnt/β-catenin signaling, cancer therapy, druggable targets
- MeSH terms
- Antineoplastic Agents, Humans, Models, Biological, Protein Binding, Proteins, Signal Transduction, Drug Delivery Systems, Wnt Proteins, beta Catenin
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