2015
DOI: 10.18632/oncotarget.5157
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Apigenin blocks IKKα activation and suppresses prostate cancer progression

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 k… Show more

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Cited by 84 publications
(60 citation statements)
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“…The oral administration of apigenin (20 and 50 μg/mice) decreased the volume and wet weight of tumors in nude mice bearing human prostate cancer, without any undesirable side effects 2730. Apigenin intake also decreased serum-IGF-I level and induced apoptosis and cell cycle arrest in tumor xenograft.…”
Section: Role Of Apigenin In Cancer Preventionmentioning
confidence: 99%
See 1 more Smart Citation
“…The oral administration of apigenin (20 and 50 μg/mice) decreased the volume and wet weight of tumors in nude mice bearing human prostate cancer, without any undesirable side effects 2730. Apigenin intake also decreased serum-IGF-I level and induced apoptosis and cell cycle arrest in tumor xenograft.…”
Section: Role Of Apigenin In Cancer Preventionmentioning
confidence: 99%
“…Apigenin intake also decreased serum-IGF-I level and induced apoptosis and cell cycle arrest in tumor xenograft. 27,29,31,32 Apigenin was shown to interrupt the NF-κB signaling pathways; this was responsible for the suppression of prostate cancer progression 30. Moreover, apigenin significantly decreased the level of Her2/neu, a protein involved in growth factor signaling, which indicated a reduction in breast cancer cell proliferation in apigenin-treated mice 33.…”
Section: Role Of Apigenin In Cancer Preventionmentioning
confidence: 99%
“…Additional evidence supported that apigenin-mediated reduction in cell proliferation, invasiveness, and decrease in tumor growth results from the downregulation of IKKα and downstream targets affecting NF-κB signaling pathways [126]. Shukla et al [127] elucidated that apigenin directly binds to IKKα, inhibiting its kinase activity. Apigenin treatment restored IκBα expression, preventing its phosphorylation by upstream kinase IKK which undergoes proteasomal degradation [127].…”
Section: 0 Effect Of Apigenin In Various Human Cancersmentioning
confidence: 99%
“…Shukla et al [127] elucidated that apigenin directly binds to IKKα, inhibiting its kinase activity. Apigenin treatment restored IκBα expression, preventing its phosphorylation by upstream kinase IKK which undergoes proteasomal degradation [127]. Further assessment by Shukla et al [128] examined the apigenin-induced 22Rv1 tumor growth inhibition subcutaneously implanted in athymic male nude mice.…”
Section: 0 Effect Of Apigenin In Various Human Cancersmentioning
confidence: 99%
“…Many diseases are related to IKK [1]. IKKα has been implicated as a key regulator of oncogenesis by affecting NF-ĸB signaling pathways [2]. Activation of IKK-β contributes to cancer pathogenesis and inflammatory disease [3].…”
Section: Introductionmentioning
confidence: 99%