INHIBITION OF THE EPIDERMAL GROWTH-FACTOR RECEPTOR TYROSINE KINASE-ACTIVITY BY LEFLUNOMIDE
INHIBITION OF THE EPIDERMAL GROWTH-FACTOR RECEPTOR TYROSINE KINASE-ACTIVITY BY LEFLUNOMIDE
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DOI：
10.1016/0014-5793(93)81704-4
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发表时间：
1993-11-15
期刊：
影响因子：
3.5
通讯作者：
FINNEGAN, A
中科院分区：
文献类型：
--
作者：
MATTAR, T;KOCHHAR, K;FINNEGAN, A
来氟米特的活性代谢物 A77 1726 可抑制多种哺乳动物细胞系的增殖。 A77 1726 在 30-40 muM 的有效剂量下可抑制表皮生长因子 (EGF) 依赖性增殖。在相同的有效剂量下，A77 1726 似乎可以直接抑制完整细胞和纯化 EGF 受体中的 EGF 受体酪氨酸特异性激酶活性。这些数据表明来氟米特通过抑制酪氨酸特异性激酶活性来抑制细胞增殖。
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.