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

FEBS Lett. 1993 Nov 15;334(2):161-4. doi: 10.1016/0014-5793(93)81704-4.

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 microM. 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.

MeSH terms

  • Aniline Compounds / pharmacology*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Carcinoma, Squamous Cell
  • Cell Line
  • Cells, Cultured
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / metabolism*
  • Fibroblasts
  • Humans
  • Hydroxybutyrates / pharmacology*
  • Isoxazoles / pharmacology*
  • KB Cells
  • Leflunomide
  • Male
  • Phosphorylation
  • Skin / metabolism
  • Tumor Cells, Cultured

Substances

  • Aniline Compounds
  • Anti-Inflammatory Agents, Non-Steroidal
  • Hydroxybutyrates
  • Isoxazoles
  • teriflunomide
  • ErbB Receptors
  • Leflunomide