ArticleThe Journal of biological chemistry2014
Isoliquiritigenin induces apoptosis and inhibits xenograft tumor growth of human lung cancer cells by targeting both wild type and L858R/T790M mutant EGFR.
Article in The Journal of biological chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
49 citing papers in PubMed, 129 citations in OpenAlex.
- Chalcones as multitarget modulators in non-small cell lung cancer: mechanistic insights and therapeutic perspectives.Archives of toxicology · 2026Review
- Synthesis and Biological Assessment of 3',4',5'-Trimethoxychalcone Derivatives against A549 and Molecular Insight Through Molecular Docking and Dynamics Studies.Current medicinal chemistry · 2026Article
- In vitro and in silico evaluation of flavonoids from Erythrina crista-galli with cytotoxic potential against MCF-7 breast cancer cell.Scientific reports · 2025Article
- From Traditional Efficacy to Drug Design: A Review of Astragali Radix.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Licorice Extract Isoliquiritigenin Increased Cytosol Calcium and Induced Apoptosis in Colon Cancer Cells via Transient Receptor Potential Vanilloid-1.Cancer medicine · 2025Article
- Targeting digestive system cancers with isoliquiritigenin: a comprehensive review of antitumor mechanisms.Frontiers in pharmacology · 2025Review
- Isoliquiritigenin induced hepatotoxicity and endoplasmic reticulum stress in zebrafish embryos.Scientific reports · 2024Article
- The Role of Licorice Chalcones as Molecular Genes and Signaling Pathways Modulator-A Review of Experimental Implications for Nicotine-Induced Non-Small Cell Lung Cancer Treatment.Current issues in molecular biology · 2024Review
- Hydroxy Chalcones and Analogs with Chemopreventive Properties.International journal of molecular sciences · 2023Review
- Anticancer Potential of Natural Chalcones: In Vitro and In Vivo Evidence.International journal of molecular sciences · 2023Review
- Sinapic acid alleviates inflammatory bowel disease (IBD) through localization of tight junction proteins by direct binding to TAK1 and improves intestinal microbiota.Frontiers in pharmacology · 2023Article
- Exploring the Phytochemicals and Anti-Cancer Potential of the Members of Fabaceae Family: A Comprehensive Review.Molecules (Basel, Switzerland) · 2022Review
- Effects of 2,2',4'-trihydroxychalcone on the proliferation, metastasis and apoptosis of A549 human lung cancer cells.Oncology letters · 2022Article
- GLP2-GLP2R signal affects the viability and EGFR-TKIs sensitivity of PC9 and HCC827 cells.BMC pulmonary medicine · 2022Article
- Review
- Synergistic anticancer effect of docosahexaenoic acid and isoliquiritigenin on human colorectal cancer cells through ROS-mediated regulation of the JNK and cytochrome c release.Molecular biology reports · 2021Article
- Perspectives on the Role of Isoliquiritigenin in Cancer.Cancers · 2021Review
- Molecular targets and anticancer activity of quinoline-chalcone hybrids: literature review.RSC advances · 2020Review
- Enhancement of the apoptotic effects of Arctii Fructus extracts on cancer cells by the enzymatic bioconversion of lignans.Food science & nutrition · 2020Article
- Isoliquiritigenin inhibits the proliferation, migration and metastasis of Hep3B cells via suppressing cyclin D1 and PI3K/AKT pathway.Bioscience reports · 2020Article
Corrections and comments
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Authors and funding
17 authors at 6 institutions in 2 countries.
Funding
Abstract
Non-small-cell lung cancer (NSCLC) is associated with diverse genetic alterations including mutation of epidermal growth factor receptor (EGFR). Isoliquiritigenin (ILQ), a chalcone derivative, possesses anticancer activities. In the present study, we investigated the effects of ILQ on the growth of tyrosine kinase inhibitor (TKI)-sensitive and -resistant NSCLC cells and elucidated its underlying mechanisms. Treatment with ILQ inhibited growth and induced apoptosis in both TKI-sensitive and -resistant NSCLC cells. ILQ-induced apoptosis was associated with the cleavage of caspase-3 and poly-(ADP-ribose)-polymerase, increased expression of Bim, and reduced expression of Bcl-2. In vitro kinase assay results revealed that ILQ inhibited the catalytic activity of both wild type and double mutant (L858R/T790M) EGFR. Treatment with ILQ inhibited the anchorage-independent growth of NIH3T3 cells stably transfected with either wild type or double-mutant EGFR with or without EGF stimulation. ILQ also reduced the phosphorylation of Akt and ERK1/2 in both TKI-sensitive and -resistant NSCLC cells, and attenuated the kinase activity of Akt1 and ERK2 in vitro. ILQ directly interacted with both wild type and double-mutant EGFR in an ATP-competitive manner. A docking model study showed that ILQ formed two hydrogen bonds (Glu-762 and Met-793) with wild type EGFR and three hydrogen bonds (Lys-745, Met-793, and Asp-855) with mutant EGFR. ILQ attenuated the xenograft tumor growth of H1975 cells, which was associated with decreased expression of Ki-67 and diminished phosphorylation of Akt and ERK1/2. Taken together, ILQ suppresses NSCLC cell growth by directly targeting wild type or mutant EGFR.
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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.