바이오칩을 이용한 Protein Kinase C의 활성에 대한헤스페리딘의 저해 효과
The Inhibitory Potency of Hesperidin on Protein Kinase C Activity Using a Biochip
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Protein kinases are the most important drug targets for the treatment of numerousdiseases. The involvement of protein kinase C (PKC) in many biological processes such as development,memory, cell differentiation, and proliferation has been demonstrated. PKC is recognizedas an important player in carcinogenesis. Thus, a variety of PKC inhibitors have been investigated. Among them, flavonoids have been demonstrated to affect the activity of many mammalianin vitro enzyme systems. The recent investigation was performed to evaluate the inhibitory effectsof hesperidin, which is a flavonoid, on the proliferation and carcinogenesis of many cancers. Inthis study, an efficient kinase assay based on a biochip using radio-phosphorylation was establishedand performed for an examination of the inhibitory effects of hesperidin on PKC activity atdifferent concentrations of 50, 200, 500 nM. It was found that hesperidin shows inhibitory potencyon PKC, and that the biochip can be used to rapidly screen kinase inhibitors resulting in the therapeuticagents.
Abstract
Protein kinases are the most important drug targets for the treatment of numerousdiseases. The involvement of protein kinase C (PKC) in many biological processes such as development,memory, cell differentiation, and proliferation has been demonstrated. PKC is recognizedas an important player in carcinogenesis. Thus, a variety of PKC inhibitors have been investigated. Among them, flavonoids have been demonstrated to affect the activity of many mammalianin vitro enzyme systems. The recent investigation was performed to evaluate the inhibitory effectsof hesperidin, which is a flavonoid, on the proliferation and carcinogenesis of many cancers. Inthis study, an efficient kinase assay based on a biochip using radio-phosphorylation was establishedand performed for an examination of the inhibitory effects of hesperidin on PKC activity atdifferent concentrations of 50, 200, 500 nM. It was found that hesperidin shows inhibitory potencyon PKC, and that the biochip can be used to rapidly screen kinase inhibitors resulting in the therapeuticagents.
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