ArticleProceedings of the National Academy of Sciences of the United States of America2011
An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 214 papers.
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Who cites it
214 citing papers in PubMed.
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- SGEF coordinates epithelial morphogenesis by regulating junction stability, collective migration, and extracellular matrix remodeling.bioRxiv : the preprint server for biology · 2026Article
- A Double-Negative Prostate Cancer Subtype Is Vulnerable to SWI/SNF-Targeting Degrader Molecules.Cancer research · 2026Article
- Evolutionary rewiring of the endomesoderm gene regulatory networks specify skeleton secreting cells in stony corals.bioRxiv : the preprint server for biology · 2026Article
- Rho/ROCK signaling and α-catenin mediate β-catenin-driven hyperplasia in the adrenal cortex via adherens junctions.The Journal of clinical investigation · 2026Article
- Wnt/β-Catenin Activation by iCRT3 Enhanced the Pluripotency of Bovine Expanded Pluripotent Stem Cells.Animals : an open access journal from MDPI · 2026Article
- Hepatocellular carcinoma-linkediScience · 2026Article
- Parallel and non-parallel features of adaptive radiation in Yucatán pupfishes.bioRxiv : the preprint server for biology · 2025Article
- Phenotypic Screening Coupled with AI-Driven Target Deconvolution Identifies α-Terthienyl as a Dual DPP-IV/HSD17β13 Modulator with Efficacy in a Mouse Model of MASLD.bioRxiv : the preprint server for biology · 2025Article
- A double-negative prostate cancer subtype is vulnerable to SWI/SNF-targeting degrader molecules.bioRxiv : the preprint server for biology · 2025Article
- Wnt/β-catenin mediated signaling pathways in cancer: recent advances, and applications in cancer therapy.Molecular cancer · 2025Review
- Wnt signaling pathways in biology and disease: mechanisms and therapeutic advances.Signal transduction and targeted therapy · 2025Review
- PGK1 enhances productive bovine herpesvirus 1 infection by stimulating β-catenin-dependent transcription.Veterinary research · 2025Article
- Ccn2a acts downstream of cx43 to influence joint formation during zebrafish fin regeneration.Biology open · 2025Article
- Notch signaling mediates between two pattern-forming processes during head regeneration inLife science alliance · 2025Article
- Mindin regulates fibroblast subpopulations through distinct Src family kinases during fibrogenesis.JCI insight · 2024Article
- Wnt Signaling Pathway in Tumor Biology.Genes · 2024Review
- Thiouracil and triazole conjugate induces autophagy through the downregulation of Wnt/β-catenin signaling pathway in human breast cancer cells.IUBMB life · 2024Article
- The Scribble-SGEF-Dlg1 complex regulates E-cadherin and ZO-1 stability, turnover and transcription in epithelial cells.Journal of cell science · 2024Article
- Ultra-large scale virtual screening identifies a small molecule inhibitor of the Wnt transporter Wntless.iScience · 2024Article
154 more citing papers are in PubMed but not listed here.
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10 authors.
Funding
Abstract
Misregulated β-catenin responsive transcription (CRT) has been implicated in the genesis of various malignancies, including colorectal carcinomas, and it is a key therapeutic target in combating various cancers. Despite significant effort, successful clinical implementation of CRT inhibitory therapeutics remains a challenging goal. This is, in part, because of the challenge of identifying inhibitory compounds that specifically modulate the nuclear transcriptional activity of β-catenin while not affecting its cytoskeletal function in stabilizing adherens junctions at the cell membrane. Here, we report an RNAi-based modifier screening strategy for the identification of CRT inhibitors. Our data provide support for the specificity of these inhibitory compounds in antagonizing the transcriptional function of nuclear β-catenin. We show that these inhibitors efficiently block Wnt/β-catenin-induced target genes and phenotypes in various mammalian and cancer cell lines. Importantly, these Wnt inhibitors are specifically cytotoxic to human colon tumor biopsy cultures as well as colon cancer cell lines that exhibit deregulated Wnt signaling.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.