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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
Author(s) -
AbouKaram Mohamed,
ElShaer Nagwa S.,
Shier W. Thomas
Publication year - 1998
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/(sici)1099-1573(199806)12:4<282::aid-ptr225>3.0.co;2-x
Subject(s) - oncogene , enzyme , tyrosine kinase , ic50 , chemistry , cancer , biochemistry , receptor tyrosine kinase , kinase , biology , in vitro , receptor , cell cycle , cell , genetics
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 μ M ). Daphnoretin was moderately cytotoxic (IC 50 = 21–114 μ M ) only in rapidly proliferating cultured mammalian cells. © 1998 John Wiley & Sons, Ltd.