自磷酸化
酪氨酸激酶
血小板源性生长因子受体
原肌球蛋白受体激酶C
受体酪氨酸激酶
ROR1型
表皮生长因子
酪氨酸磷酸化
酪氨酸
酪氨酸激酶抑制剂
生物
分子生物学
原癌基因酪氨酸蛋白激酶Src
化学
细胞生物学
磷酸化
生物化学
受体
信号转导
生长因子
蛋白激酶A
癌症
遗传学
作者
David W. Fry,Alan J. Kraker,Amy McMichael,Linda A. Ambroso,James M. Nelson,Wilbur R. Leopold,Richard W. Connors,Alexander J. Bridges
出处
期刊:Science
[American Association for the Advancement of Science (AAAS)]
日期:1994-08-19
卷期号:265 (5175): 1093-1095
被引量:765
标识
DOI:10.1126/science.8066447
摘要
A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF receptor tyrosine kinase and inhibited other purified tyrosine kinases only at micromolar or higher concentrations. PD 153035 rapidly suppressed autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocked EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD 153035 demonstrates an increase in potency over that of other tyrosine kinase inhibitors of four to five orders of magnitude for inhibition of isolated EGF receptor tyrosine kinase and three to four orders of magnitude for inhibition of cellular phosphorylation.
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