ArticleThe Journal of biological chemistry2009
Discovery and characterization of a small molecule inhibitor of the PDZ domain of dishevelled.
Article in The Journal of biological chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 105 papers.
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Who cites it
105 citing papers in PubMed.
- Nuclear β-catenin: molecular regulation, challenges and therapeutic opportunities.Cell communication and signaling : CCS · 2025Review
- WNT signaling in cancer: molecular mechanisms and potential therapies.Molecular biomedicine · 2025Review
- Wnt signaling pathways in biology and disease: mechanisms and therapeutic advances.Signal transduction and targeted therapy · 2025Review
- Advances in the development of Wnt/β-catenin signaling inhibitors.RSC medicinal chemistry · 2025Review
- Wnt Signaling Pathway in Tumor Biology.Genes · 2024Review
- Review
- Wnt/β-catenin signaling pathway in carcinogenesis and cancer therapy.Journal of hematology & oncology · 2024Review
- Cyclic stretching combined with cell-cell adhesion is sufficient for inducing cell intercalation.Biophysical journal · 2023Article
- Review
- A New Wave of Targeting 'Undruggable' Wnt Signaling for Cancer Therapy: Challenges and Opportunities.Cells · 2023Review
- Review
- Article
- Intestinal Wnt in the transition from physiology to oncology.World journal of clinical oncology · 2022Review
- Anticancer Activity of (Cancers · 2022Article
- WNT signaling at the intersection between neurogenesis and brain tumorigenesis.Frontiers in molecular neuroscience · 2022Review
- KIF2C: a novel link between Wnt/β-catenin and mTORC1 signaling in the pathogenesis of hepatocellular carcinoma.Protein & cell · 2021Article
- The Wnt signaling pathway in tumorigenesis, pharmacological targets, and drug development for cancer therapy.Biomarker research · 2021Review
- Wnt/β-catenin signaling in cancers and targeted therapies.Signal transduction and targeted therapy · 2021Review
- Molecular docking-aided identification of small molecule inhibitors targeting β-catenin-TCF4 interaction.iScience · 2021Article
- Small-molecule probe reveals a kinase cascade that links stress signaling to TCF/LEF and Wnt responsiveness.Cell chemical biology · 2021Article
45 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
Dishevelled (Dvl) is an essential protein in the Wnt signaling pathways; it uses its PDZ domain to transduce the Wnt signals from the membrane receptor Frizzled to downstream components. Here, we report identifying a drug-like small molecule compound through structure-based ligand screening and NMR spectroscopy and show the compound to interact at low micromolar affinity with the PDZ domain of Dvl. In a Xenopus testing system, the compound could permeate the cell membrane and block the Wnt signaling pathways. In addition, the compound inhibited Wnt signaling and reduced the levels of apoptosis in the hyaloid vessels of eye. Moreover, this compound also suppressed the growth of prostate cancer PC-3 cells. These biological effects suggest that by blocking the PDZ domain of Dvl, the compound identified in our studies effectively inhibits the Wnt signaling and thus provides a useful tool for studies dissecting the Wnt signaling pathways.
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Registered trials
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