Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors

Kazuo Umezawa, Takashi Hori, Hirohisa Tajima, Masaya Imoto, Kunio Isshiki, Tomio Takeuchi

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)


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 μg 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 ofDNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.

Original languageEnglish
Pages (from-to)198-200
Number of pages3
JournalFEBS Letters
Issue number2
Publication statusPublished - 1990 Jan 29
Externally publishedYes


  • (Normal rat kidney cell)
  • Cell cycle
  • DNA synthesis
  • Epidermal growth factor
  • Erbstatin

ASJC Scopus subject areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology


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