ArticleCancer prevention research (Philadelphia, Pa.)2014
Kaempferol targets RSK2 and MSK1 to suppress UV radiation-induced skin cancer.
Article in Cancer prevention research (Philadelphia, Pa.), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 64 citations in OpenAlex.
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- A deep dive into the orchard of health: Exploring the anti-cancer and anti-aging potential of apple polyphenols.Journal of food and drug analysis · 2025Review
- Targeting RSK2 in Cancer Therapy: A Review of Natural Products.Anti-cancer agents in medicinal chemistry · 2025Review
- RSK1 and RSK2 as therapeutic targets: an up-to-date snapshot of emerging data.Expert opinion on therapeutic targets · 2024Review
- A recent update on the connection between dietary phytochemicals and skin cancer: emerging understanding of the molecular mechanism.Annals of medicine and surgery (2012) · 2024Review
- Natural Compounds in Non-Melanoma Skin Cancer: Prevention and Treatment.Molecules (Basel, Switzerland) · 2024Review
- Skin cancer: understanding the journey of transformation from conventional to advanced treatment approaches.Molecular cancer · 2023Review
- Spice-Derived Phenolic Compounds: Potential for Skin Cancer Prevention and Therapy.Molecules (Basel, Switzerland) · 2023Review
- Targeting receptor tyrosine kinase signaling: Avenues in the management of cutaneous squamous cell carcinoma.iScience · 2023Review
- Effects and Mechanisms of Kaempferol in the Management of Cancers through Modulation of Inflammation and Signal Transduction Pathways.International journal of molecular sciences · 2023Review
- Exploring the Remarkable Chemotherapeutic Potential of Polyphenolic Antioxidants in Battling Various Forms of Cancer.Molecules (Basel, Switzerland) · 2023Review
- Therapeutic targeting of p90 ribosomal S6 kinase.Frontiers in cell and developmental biology · 2023Review
- A systematic review of anti-cancer roles and mechanisms of kaempferol as a natural compound.Cancer cell international · 2022Review
- Evidence for Involvement of Nonclassical Pathways in the Protection From UV-Induced DNA Damage by Vitamin D-Related Compounds.JBMR plus · 2021Article
- Lipid Nanoparticles Containing Mixtures of Antioxidants to Improve Skin Care and Cancer Prevention.Pharmaceutics · 2021Article
- Association BetweenFrontiers in genetics · 2021Review
- Safflower Seed Oil and Its Active Compound Acacetin Inhibit UVB-Induced Skin Photoaging.Journal of microbiology and biotechnology · 2020Article
- Discovery of a novel dual-target inhibitor against RSK1 and MSK2 to suppress growth of human colon cancer.Oncogene · 2020Article
- Review
- Kaempferol targeting on the fibroblast growth factor receptor 3-ribosomal S6 kinase 2 signaling axis prevents the development of rheumatoid arthritis.Cell death & disease · 2018Article
Corrections and comments
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Authors and funding
16 authors at 2 institutions in 1 country.
Funding
Abstract
Solar UV (SUV) irradiation is a major factor in skin carcinogenesis, the most common form of cancer in the United States. The MAPK cascades are activated by SUV irradiation. The 90 kDa ribosomal S6 kinase (RSK) and mitogen and stress-activated protein kinase (MSK) proteins constitute a family of protein kinases that mediate signal transduction downstream of the MAPK cascades. In this study, phosphorylation of RSK and MSK1 was upregulated in human squamous cell carcinoma (SCC) and SUV-treated mouse skin. Kaempferol, a natural flavonol, found in tea, broccoli, grapes, apples, and other plant sources, is known to have anticancer activity, but its mechanisms and direct target(s) in cancer chemoprevention are unclear. Kinase array results revealed that kaempferol inhibited RSK2 and MSK1. Pull-down assay results, ATP competition, and in vitro kinase assay data revealed that kaempferol interacts with RSK2 and MSK1 at the ATP-binding pocket and inhibits their respective kinase activities. Mechanistic investigations showed that kaempferol suppresses RSK2 and MSK1 kinase activities to attenuate SUV-induced phosphorylation of cAMP-responsive element binding protein (CREB) and histone H3 in mouse skin cells. Kaempferol was a potent inhibitor of SUV-induced mouse skin carcinogenesis. Further analysis showed that skin from the kaempferol-treated group exhibited a substantial reduction in SUV-induced phosphorylation of CREB, c-Fos, and histone H3. Overall, our results identify kaempferol as a safe and novel chemopreventive agent against SUV-induced skin carcinogenesis that acts by targeting RSK2 and MSK1.
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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.