自磷酸化
原肌球蛋白受体激酶C
酪氨酸激酶
表皮生长因子
血小板源性生长因子受体
受体酪氨酸激酶
丝裂原活化蛋白激酶激酶
ROR1型
细胞生物学
胰岛素样生长因子1受体
化学
生物
生物化学
分子生物学
受体
蛋白激酶A
激酶
生长因子
作者
Pnina Yaish,Aviv Gazit,Chaim Gilon,Alexander Levitzki
出处
期刊:Science
[American Association for the Advancement of Science (AAAS)]
日期:1988-11-11
卷期号:242 (4880): 933-935
被引量:593
标识
DOI:10.1126/science.3263702
摘要
A systematic series of low molecular weight protein tyrosine kinase inhibitors were synthesized; they had progressively increasing affinity over a 2500-fold range toward the substrate site of epidermal growth factor (EGF) receptor kinase domain. These compounds inhibited EGF receptor kinase activity up to three orders of magnitude more than they inhibited insulin receptor kinase, and they also effectively inhibited the EGF-dependent autophosphorylation of the receptor. The most potent compounds effectively inhibited the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on the EGF-independent proliferation of these cells. The potential use of tyrosine protein kinase inhibitors as antiproliferative agents is demonstrated.
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