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

Mohamed Abou-Karam; Nagwa S. El-Shaer; W. Thomas Shier

doi:10.1002/(SICI)1099-1573(199806)12:4<282::AID-PTR225>3.0.CO;2-X

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

Mohamed Abou-Karam, Nagwa S. El-Shaer, W. Thomas Shier

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

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Abstract

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 (IC₅₀ = 97.5 μM). Daphnoretin was moderately cytotoxic (IC₅₀ = 21-114 μM) only in rapidly proliferating cultured mammalian cells.

Original language	English (US)
Pages (from-to)	282-284
Number of pages	3
Journal	Phytotherapy Research
Volume	12
Issue number	4
DOIs	https://doi.org/10.1002/(SICI)1099-1573(199806)12:4<282::AID-PTR225>3.0.CO;2-X
State	Published - Jun 1998

Keywords

Cultured mammalian cells
Cytotoxicity
Daphnoretin
Thymelaea hirsuta (L.) Endl.
Thymelaeaceae
Tyrosine kinase inhibition

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AU - El-Shaer, Nagwa S.

AU - Shier, W. Thomas

PY - 1998/6

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AB - 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 (IC50 = 97.5 μM). Daphnoretin was moderately cytotoxic (IC50 = 21-114 μM) only in rapidly proliferating cultured mammalian cells.

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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

Abstract

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UN SDGs

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