ArticleScientific reports2019
A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Beta-glucans in oncology: revolutionizing treatment with immune power & tumor targeting.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Resistance to third-generation EGFR TKIs - what can be expected from the fourth-generation?Cancer drug resistance (Alhambra, Calif.) · 2026Review
- STAT3 mediates CAF-induced osimertinib resistance via regulating protein secretion in non-small cell lung cancer.Frontiers in pharmacology · 2025Article
- ELK1/MTOR/S6K1 Pathway Contributes to Acquired Resistance to Gefitinib in Non-Small Cell Lung Cancer.International journal of molecular sciences · 2024Article
- Mediating kinase activity in Ras-mutant cancer: potential for an individualised approach?Frontiers in pharmacology · 2024Review
- Pygo1 Regulates the Behavior of Human Non-Small-Cell Lung Cancer via the Wnt/Disease markers · 2022Article
- Post-translational modification of RAS proteins.Current opinion in structural biology · 2021Review
- Drug resistance of targeted therapy for advanced non-small cell lung cancer harbored EGFR mutation: from mechanism analysis to clinical strategy.Journal of cancer research and clinical oncology · 2021Review
- Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?International journal of molecular sciences · 2021Review
- Interaction of FLNA and ANXA2 promotes gefitinib resistance by activating the Wnt pathway in non-small-cell lung cancer.Molecular and cellular biochemistry · 2021Article
- Leukotriene B4 receptor-2 contributes to KRAS-driven lung tumor formation by promoting interleukin-6-mediated inflammation.Experimental & molecular medicine · 2021Article
- Review
- Small molecule-induced simultaneous destabilization of β-catenin and RAS is an effective molecular strategy to suppress stemness of colorectal cancer cells.Cell communication and signaling : CCS · 2020Article
- Regulation of large and small G proteins by ubiquitination.The Journal of biological chemistry · 2019Review
- A positive feedback loop of β-catenin/CCR2 axis promotes regorafenib resistance in colorectal cancer.Cell death & disease · 2019Article
- Restoration of mutant K-Ras repressed miR-199b inhibits K-Ras mutant non-small cell lung cancer progression.Journal of experimental & clinical cancer research : CR · 2019Article
- A Potential Off-Target Effect of the Wnt/β-Catenin Inhibitor KYA1797K: PD-L1 Binding and Checkpoint Inhibition.Biomedicine hubArticle
Corrections and comments
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The epidermal growth factor receptor (EGFR) inhibitors such as erlotinib and gefitinib are widely used for treatment of non-small cell lung cancer (NSCLC), but they have shown limited efficacy in an unselected population of patients. The KRAS mutations, which are identified in approximately 20% of NSCLC patients, have shown to be associated with the resistance to the EGFR tyrosine kinase inhibitors (TKIs). Currently, there is no clinically available targeted therapy which can effectively inhibit NSCLC tumors harboring KRAS mutations. This study aims to show the effectiveness of KYA1797K, a small molecule which revealed anti-cancer effect in colorectal cancer by destabilizing Ras via inhibiting the Wnt/β-catenin pathway, for the treatment of KRAS-mutated NSCLC. While erlotinib fail to have anti-transforming effect in NSCLC cell lines harboring KRAS mutations, KYA1797K effectively inhibited the Ras-ERK pathway in KRAS-mutant NSCLC cell lines. As a result, KYA1797K treatment suppressed the growth and transformation of KRAS mutant NSCLC cells and also induced apoptosis. Furthermore, KYA1797K effectively inhibited Kras-driven tumorigenesis in the Kras
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