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

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...

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Published in:Phytotherapy research 1998-06, Vol.12 (4), p.282-284
Main Authors: Abou-Karam, Mohamed, El-Shaer, Nagwa S., Shier, W. Thomas
Format: Article
Language:English
Subjects:
Biological and medical sciences
cultured mammalian cells
cytotoxicity
daphnoretin
General pharmacology
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Thymelaea hirsuta (L.) Endl
Thymelaeaceae
tyrosine kinase inhibition
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container_end_page 284
container_issue 4
container_start_page 282
container_title Phytotherapy research
container_volume 12
creator Abou-Karam, Mohamed
El-Shaer, Nagwa S.
Shier, W. Thomas
description 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. © 1998 John Wiley & Sons, Ltd.
doi_str_mv 10.1002/(SICI)1099-1573(199806)12:4<282::AID-PTR225>3.0.CO;2-X
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subjects Biological and medical sciences
cultured mammalian cells
cytotoxicity
daphnoretin
General pharmacology
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Thymelaea hirsuta (L.) Endl
Thymelaeaceae
tyrosine kinase inhibition
title Inhibition of oncogene product enzyme activity as an approach to cancer chemoprevention. Tyrosine-specific protein kinase inhibition by daphnoretin from Thymelaea hirsuta root
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