Cited by 50Wnt/β-catenin signaling in development and cancerSignaling Pathways in DiseaseHedgehog Signaling Pathway Studies

Direct targeting of β-catenin: Inhibition of protein–protein interactions for the inactivation of Wnt signaling

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Hahne, Gernot, Grossmann, Tom N.·2013·Bioorganic & Medicinal Chemistry

Abstract

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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Crossref · 10.1016/j.bmc.2013.02.050

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Authors
Hahne, G., & Grossmann, T. N.
Affiliations
Max Planck Society (DE)
Corresponding author
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
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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