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Inhibition of oncogene product enzyme activity as an approach to cancer chemoprevention. Tyrosine-specific protein kinase inhibition by daphnoretin from Thymelaea hirsuta root

โœ Scribed by Mohamed Abou-Karam; Nagwa S. El-Shaer; W. Thomas Shier


Publisher
John Wiley and Sons
Year
1998
Tongue
English
Weight
91 KB
Volume
12
Category
Article
ISSN
0951-418X

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โœฆ Synopsis


Inhibitors of oncogene product enzyme activity were sought as a prescreen for potential cancer chemopreventive agents. Daphnoretin, a dicoumaryl ether from Thymelaea hirsuta root, inhibited the erb-b oncogene product, the tyrosine-specific protein kinase of human epidermal growth factor receptor (IC 50 = 97.5 mM). Daphnoretin was moderately cytotoxic (IC 50 = 21-114 mM) only in rapidly proliferating cultured mammalian cells.


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Inhibitors of oncogene product enzyme activity were sought as a prescreen for potential cancer chemopreventive agents. Purpurogallin, a polyphenol from Quercus sp. nutgall, was found to inhibit the tyrosine-specific protein kinase of the human erb-b oncogene product (epidermal growth factor receptor