The DOI matches its Crossref record; 97 of the 98 references it cites were found in a registry or an index.
Cell Permeable Stapled Peptide Inhibitor of Wnt Signaling that Targets β-Catenin Protein-Protein Interactions
Open accessAbstract
The Wnt signaling pathway plays a critical role in cell proliferation and differentiation, thus it is often associated with diseases such as cancers. Unfortunately, although attractive, developing anti-cancer strategy targeting Wnt signaling has been challenging given that the most attractive targets are involved in protein-protein interactions (PPIs). Here, we develop a stapled peptide inhibitor that targets the interaction between β-catenin and T cell factor/lymphoid enhancer-binding factor transcription factors, which are crucially involved in Wnt signaling. Our integrative approach combines peptide stapling to optimize proteolytic stability, with lessons learned from cell-penetrating peptide (CPP) design to maximize cellular uptake resulting in NLS-StAx-h, a selective, cell permeable, stapled peptide inhibitor of oncogenic Wnt signaling that efficiently inhibits β-catenin-transcription factor interactions. We expect that this type of integrative strategy that endows stapled peptides with CPP features will be generally useful for developing inhibitors of intracellular PPIs.
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“In addition, several compounds have been selected as inhibitors targeting β-cateninde PPI, including small molecules such as ICG-001 (176),448 NLs-StAx-h (177)449 and CRT inhibitors (iCRT3 (178), iCRT5 (179), iCRT14 (180)),450 Henryin (181),451 PKF115-584 (182) and CGP049090 (183).452”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [449]
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The Perseus computational platform for comprehensive analysis of (prote)omics data
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Wnt/β-catenin signaling and disease
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Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling
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Dougherty, P. G., Sahni, A., & Pei, D. (2019) · Chemical Reviews · doi:10.1021/acs.chemrev.9b00008 · Cited by 598
Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396
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Metadata
- Authors
- Dietrich, L., Rathmer, B., Ewan, K., Bange, T., Heinrichs, S., Dale, T. C., Schade, D., & Grossmann, T. N.
- Affiliations
- Max Planck Society (DE)
- TU Dortmund University (DE)
- Cardiff University (GB)
- Max Planck Institute of Molecular Physiology (DE)
- Essen University Hospital (DE)
- Corresponding author
- Grossmann, Tom N.
- Venue
- Cell Chemical Biology
- Publisher
- Elsevier BV
- Published
- 2017-08
- Volume
- 24
- Issue
- 8
- Pages
- 958-968.e5
- ISSN
- 2451-9448 (ISSN-L)
- 2451-9456
- OpenAlex
- W2741166200
- Cited by
- 126
- References
- 98
- Citations by year
- 2026: 10 · 2025: 4 · 2024: 23 · 2023: 12 · 2022: 13 · 2021: 19 · 2020: 14 · 2019: 14 · 2018: 16 · 2017: 1
- FWCI
- 5.14
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Cell chemical biology (publishedVersion)
- PubMed (publishedVersion)
- ORCA Online Research @Cardiff (Cardiff University) (acceptedVersion)
- ORCA Online Research @Cardiff (Cardiff University) (submittedVersion)
- MPG.PuRe (Max Planck Society) (submittedVersion)
- VU Research Portal (submittedVersion, other-oa)
- Data Archiving and Networked Services (DANS) (submittedVersion)
- Funders
- Max-Planck-Gesellschaft
- Cancer Research UK (C368/A4545, C368/A7990)
- AstraZeneca
- European Research Council (678623)
- Boehringer Ingelheim
- Bayer HealthCare
- Bayer CropScience
- Deutsche Forschungsgemeinschaft (GR3592/2-1)
- Bundesministerium für Bildung und Forschung (131605)
- Biotechnology and Biological Sciences Research Council (BB/D00117X/1)
- Merck KGaA
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
- 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 › RNA Interference and Gene Delivery
- Keywords
- Wnt signaling, β-catenin, protein-protein interaction inhibitors, stapled peptides, cell-penetrating peptides, T-cell factor, nuclear localization signal, membrane permeability, cancer therapy
- MeSH terms
- Amino Acid Sequence, Cell Membrane Permeability, Cell Movement, HeLa Cells, Humans, Gene Expression, Genes, Reporter, Microscopy, Confocal, Cell Line, Tumor, Cell Proliferation, beta Catenin, Basic Helix-Loop-Helix Transcription Factors, Basic Helix-Loop-Helix Proteins, Protein Interaction Domains and Motifs, Cell-Penetrating Peptides, Wnt Signaling Pathway, Axin Protein
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