INHIBITION OF THE EPIDERMAL GROWTH-FACTOR RECEPTOR TYROSINE KINASE-ACTIVITY BY LEFLUNOMIDE

被引:154
作者
MATTAR, T
KOCHHAR, K
BARTLETT, R
BREMER, EG
FINNEGAN, A
机构
[1] UNIV MAINZ,DEPT IMMUNOL,W-6500 MAINZ,GERMANY
[2] HOECHST AG,W-6200 WIESBADEN,GERMANY
[3] RUSH PRESBYTERIAN ST LUKES MED CTR,DEPT IMMUNOL MICROBIOL,CHICAGO,IL 60612
[4] RUSH PRESBYTERIAN ST LUKES MED CTR,DEPT MED,CHICAGO,IL 60612
关键词
EPIDERMAL GROWTH FACTOR RECEPTOR; TYROSINE-SPECIFIC KINASE; LEFLUNOMIDE; HUMAN FORESKIN FIBROBLAST CELL;
D O I
10.1016/0014-5793(93)81704-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 muM. 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.
引用
收藏
页码:161 / 164
页数:4
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