ArticleNature chemical biology2016
Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation.
Article in Nature chemical biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 70 papers.
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Who cites it
70 citing papers in PubMed, 101 citations in OpenAlex.
- Phosphorylation Protects Oncogenic RAS from LZTR1-Mediated Degradation.bioRxiv : the preprint server for biology · 2026Article
- Identification of Hub Neutrophil Coexpressed Genes in Acute PancreatitisEndocrine, metabolic & immune disorders drug targets · 2026Article
- β-catenin initiates peritoneal fibrosis by triggering mitochondrial fission-mediated mesothelial cell senescence fate transition.Military Medical Research · 2025Article
- Review
- Wnt signaling pathways in biology and disease: mechanisms and therapeutic advances.Signal transduction and targeted therapy · 2025Review
- Anti-lymphoma peptide is inspired by mapping a sequence of four amino acids of KRAI motif as nuclear localization signal of Crlz-1.Molecular therapy. Oncology · 2025Article
- Advances in the development of Wnt/β-catenin signaling inhibitors.RSC medicinal chemistry · 2025Review
- Signaling pathway dysregulation in breast cancer.Oncotarget · 2025Review
- Modulation of Wnt/Beta-Catenin Pathway by Major Dietary Phytochemicals Against Breast Cancer Development.Biology · 2025Review
- N-Cadherin promotes cardiac regeneration by potentiating pro-mitotic β-Catenin signaling in cardiomyocytes.Nature communications · 2025Article
- Transcriptional Regulation of Lipid Metabolism by Wnt Signaling and Hox Protein Cues.Advances in experimental medicine and biology · 2025Review
- An overview of recent advancements in small molecules suppression of oncogenic signaling of K-RAS: an updated review.Molecular diversity · 2024Review
- AXIN1 boosts antiviral response through IRF3 stabilization and induced phase separation.Signal transduction and targeted therapy · 2024Article
- KCTD17-mediated Ras stabilization promotes hepatocellular carcinoma progression.Clinical and molecular hepatology · 2024Article
- Blocking the WNT/β-catenin pathway in cancer treatment:pharmacological targets and drug therapeutic potential.Heliyon · 2024Review
- Canonical WNT/β-catenin signaling upregulates aerobic glycolysis in diverse cancer types.Molecular biology reports · 2024Review
- Optimizing Alkyl Side Chains in Difluorobenzene-Rhodanine Small-Molecule Acceptors for Organic Solar Cells.Materials (Basel, Switzerland) · 2024Article
- Inhibition of ADAM9 promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.Nature cancer · 2024Article
- The Wnt/β-catenin pathway is important for replication of SARS-CoV-2 and other pathogenic RNA viruses.Npj viruses · 2024Article
- Regulators of G-Protein Signaling (RGS) in Sporadic and Colitis-Associated Colorectal Cancer.International journal of molecular sciences · 2024Review
10 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
18 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Both the Wnt/β-catenin and Ras pathways are aberrantly activated in most human colorectal cancers (CRCs) and interact cooperatively in tumor promotion. Inhibition of these signaling may therefore be an ideal strategy for treating CRC. We identified KY1220, a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway, and synthesized its derivative KYA1797K. KYA1797K bound directly to the regulators of G-protein signaling domain of axin, initiating β-catenin and Ras degradation through enhancement of the β-catenin destruction complex activating GSK3β. KYA1797K effectively suppressed the growth of CRCs harboring APC and KRAS mutations, as shown by various in vitro studies and by in vivo studies using xenograft and transgenic mouse models of tumors induced by APC and KRAS mutations. Destabilization of both β-catenin and Ras via targeting axin is a potential therapeutic strategy for treatment of CRC and other type cancers activated Wnt/β-catenin and Ras pathways.
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Registered trials
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.