6533b839fe1ef96bd12a5a82
RESEARCH PRODUCT
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide.
Alison FinneganThomas MattarKulvinder KochharRobert BartlettEric G. Bremersubject
MaleToluidinesmedicine.medical_treatmentBiophysicsHydroxybutyratesBiochemistryKB CellsCell LineHuman foreskin fibroblast cellStructural BiologyEpidermal growth factorNitrilesGeneticsmedicineTumor Cells CulturedAnimalsHumansEpidermal growth factor receptorKinase activityPhosphorylationReceptorMolecular BiologyCells CulturedSkinAniline CompoundsbiologyCell growthKinaseEpidermal growth factor receptorGrowth factorAnti-Inflammatory Agents Non-SteroidalCell BiologyIsoxazolesFibroblastsTyrosine-specific kinaseCell biologyErbB ReceptorsBiochemistryCrotonatesbiology.proteinCarcinoma Squamous CellPlatelet-derived growth factor receptorLeflunomidedescription
AbstractThe 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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1993-11-15 | FEBS letters |