Levitzki Alexander
Unit of Cellular Signaling, Department of Biological Chemistry, The Alexander Silberman Institute of Life Sciences, The Hebrew University of Jerusalem, Jerusalem 91904, Israel.
Acc Chem Res. 2003 Jun;36(6):462-9. doi: 10.1021/ar0201207.
Most of the signal transduction pathways are mediated by protein kinases regulating every aspect of cell function. Mutations which deregulate their expression or their function or both result in cancers. Therefore, protein kinase inhibitors has become the focus of development of new therapies for cancer. Almost all 120 protein tyrosine kinases are involved in signaling, whereas only a handful of Ser/Thr kinases are involved. Thus, most of the effort is directed toward the development of tyrosine phosphorylation inhibitors. The success of Gleevec in the treatment of chronic myeloid leukemia and of Iressa for lung cancer validates the approach.
大多数信号转导途径由调节细胞功能各个方面的蛋白激酶介导。使它们的表达或功能或两者失调的突变会导致癌症。因此，蛋白激酶抑制剂已成为癌症新疗法开发的焦点。几乎所有120种蛋白酪氨酸激酶都参与信号传导，而只有少数丝氨酸/苏氨酸激酶参与其中。因此，大部分研究工作都致力于酪氨酸磷酸化抑制剂的开发。格列卫在治疗慢性髓性白血病以及易瑞沙在治疗肺癌方面的成功验证了这种方法。
