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  • Title: Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors.
    Author: Umezawa K, Hori T, Tajima H, Imoto M, Isshiki K, Takeuchi T.
    Journal: FEBS Lett; 1990 Jan 29; 260(2):198-200. PubMed ID: 2298299.
    Abstract:
    We prepared methyl 2,5-dihydroxycinnamate as a stable analogue of erbstatin, a tyrosine kinase inhibitor. This analogue was about 4 times more stable than erbstatin in calf serum. It inhibited epidermal growth factor receptor-associated tyrosine kinase in vitro with an IC50 of 0.15 micrograms/ml. It also inhibited in situ autophosphorylation of epidermal growth factor receptor in A431 cells. Methyl 2,5-dihydroxycinnamate was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount of DNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.
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