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最近几年癌基因的研究取得了很大进展。如果能分离出癌基因作用的抑制物质,则能开发出高特异性抗癌剂。表皮生长因子(EGF)的受体蛋白具有酪氨酸激酶活性,也是癌基因erbB1的产物。从放线菌(链霉菌属)的次级代谢产物分离出来的对酪氨酸激酶有抑制作用的物质叫做erbstatin[2,5-二羟基-苯乙烯-N-甲酰胺]。erbstatin对EGF受体的酪氨酸激酶的IC_(50)是0.2～0.5μg/ml。在A431细胞内加入15μg/ml erbstatin,能抑制EGF激活的EGF受体的激酶活性。erbstatin能使癌变细胞形态恢复正
In recent years, great progress has been made in the research of oncogenes. If we can isolate the inhibitory effect of oncogene function, we can develop a high-specific anti-cancer agent. The receptor protein of epidermal growth factor (EGF) has tyrosine kinase activity and is also a product of the oncogene erbB1. The substance that inhibits tyrosine kinase isolated from the secondary metabolites of actinomycetes (Streptomyces) is called erbstatin [2,5-dihydroxy-styrene-N-carboxamide]. The IC 50 of tyrosine kinase of erbstatin to EGF receptor is 0.2-0.5 μg / ml. Addition of 15 μg / ml erbstatin to A431 cells inhibited the kinase activity of EGF-activated EGF receptors. Erbstatin can make cancerous cells morphologically positive