ArticleOncotarget2015
Apigenin blocks IKKα activation and suppresses prostate cancer progression.
Article in Oncotarget, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
48 citing papers in PubMed, 99 citations in OpenAlex.
- The roles of IKKα in normal physiology and cancer.Cell communication and signaling : CCS · 2026Review
- Apigenin accelerates fracture healing by enhancing endochondral differentiation and inflammation resolution via targeting NF-κB signaling.Frontiers in immunology · 2026Article
- Screening the Active Phytochemicals FromCancer innovation · 2025Review
- Double trouble: cytosolic and nuclear IKKα in cancer.Open biology · 2025Review
- Role of long non-coding RNAs and natural products in prostate cancer: insights into key signaling pathways.Functional & integrative genomics · 2025Review
- Potential anticancer effects and toxicity of flavones luteolin and apigeninJournal of environmental science and health. Part C, Toxicology and carcinogenesis · 2025Review
- Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3-Molecules (Basel, Switzerland) · 2024Article
- NFκB signalling in colorectal cancer: Examining the central dogma of IKKα and IKKβ signalling.Heliyon · 2024Review
- Apigenin: Molecular Mechanisms and Therapeutic Potential against Cancer Spreading.International journal of molecular sciences · 2024Review
- An updated review summarizing the anticancer potential of flavonoids via targeting NF-kB pathway.Frontiers in pharmacology · 2024Review
- In silico study of polyphenols as potential inhibitors of MALT1 protein in non-Hodgkin lymphoma.Medical oncology (Northwood, London, England) · 2023Article
- Transcriptome reprogramming through alternative splicing triggered by apigenin drives cell death in triple-negative breast cancer.Cell death & disease · 2023Article
- Flavones: The Apoptosis in Prostate Cancer of Three Flavones Selected as Therapeutic Candidate Models.International journal of molecular sciences · 2023Review
- Effects of Flavonoids on Cancer, Cardiovascular and Neurodegenerative Diseases: Role of NF-κB Signaling Pathway.International journal of molecular sciences · 2023Review
- Insight into the Biological Roles and Mechanisms of Phytochemicals in Different Types of Cancer: Targeting Cancer Therapeutics.Nutrients · 2023Review
- Flavones: Six Selected Flavones and Their Related Signaling Pathways That Induce Apoptosis in Cancer.International journal of molecular sciences · 2022Review
- The Potential Role of Apigenin in Cancer Prevention and Treatment.Molecules (Basel, Switzerland) · 2022Review
- Pharmacological Properties of 4', 5, 7-Trihydroxyflavone (Apigenin) and Its Impact on Cell Signaling Pathways.Molecules (Basel, Switzerland) · 2022Review
- Role of Induced Programmed Cell Death in the Chemopreventive Potential of Apigenin.International journal of molecular sciences · 2022Review
- IKKα Induces Epithelial-Mesenchymal Changes in Mouse Skin Carcinoma Cells That Can Be Partially Reversed by Apigenin.International journal of molecular sciences · 2022Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
IKKα has been implicated as a key regulator of oncogenesis and driver of the metastatic process; therefore is regarded as a promising therapeutic target in anticancer drug development. In spite of the progress made in the development of IKK inhibitors, no potent IKKα inhibitor(s) have been identified. Our multistep approach of molecular modeling and direct binding has led to the identification of plant flavone apigenin as a specific IKKα inhibitor. Here we report apigenin, in micro molar range, inhibits IKKα kinase activity, demonstrates anti-proliferative and anti-invasive activities in functional cell based assays and exhibits anticancer efficacy in experimental tumor model. We found that apigenin directly binds with IKKα, attenuates IKKα kinase activity and suppresses NF-ĸB/p65 activation in human prostate cancer PC-3 and 22Rv1 cells much more effectively than IKK inhibitor, PS1145. We also showed that apigenin caused cell cycle arrest similar to knockdown of IKKα in prostate cancer cells. Studies in xenograft mouse model indicate that apigenin feeding suppresses tumor growth, lowers proliferation and enhances apoptosis. These effects correlated with inhibition of p-IKKα, NF-ĸB/p65, proliferating cell nuclear antigen and increase in cleaved caspase 3 expression in a dose-dependent manner. Overall, our results suggest that inhibition of cell proliferation, invasiveness and decrease in tumor growth by apigenin are mediated by its ability to suppress IKKα and downstream targets affecting NF-ĸB signaling 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.