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Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide

Authors
Journal
FEBS Letters
0014-5793
Publisher
Wiley Blackwell (John Wiley & Sons)
Publication Date
Volume
334
Issue
2
Identifiers
DOI: 10.1016/0014-5793(93)81704-4
Keywords
  • Epidermal Growth Factor Receptor
  • Tyrosine-Specific Kinase
  • Leflunomide
  • Human Foreskin Fibroblast Cell

Abstract

Abstract The active metabolite of leflunomide, A77 1726 inhibits the proliferation of a variety of mammalian cell lines in culture. Epidermal growth factor (EGF)-dependent proliferation is inhibited by A77 1726 at an effective dose of 30–40 μM. A77 1726 appears to directly inhibit the EGF receptor tyrosine-specific kinase activity both in intact cells and purified EGF receptors at the same effective dose. These data suggest that leflunomide inhibits cellular proliferation by the inhibition of tyrosine-specific kinase activities.

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