小分子蛋白酪氨酸激酶抑制剂及其作用机制

Small-molecule inhibitors of protein tyrosine kinases and their mechanisms of action

随着大量的酪氨酸激酶小分子抑制剂的出现以及部分此类药物在临床上抗肿瘤方面的成功应用,对于蛋白酪氨酸激酶抑制剂的研究受到了广泛的关注。本文介绍了已上市的10种蛋白酪氨酸激酶小分子抑制剂,并按作用机制的不同将其分为TypeⅠ和TypeⅡ两类。介绍了两种尚无上市药物的新型的酪氨酸激酶抑制剂,并对开发新酪氨酸激酶抑制剂的方法进行了简介。

As a large number of protein tyrosine kinase inhibitors have been found and some of them were applied to treat cancer patients successfully, the studies of protein tyrosine kinase inhibitors have attracted more and more attention. This paper introduces ten marketed protein tyrosine kinase inhibitors as two groups： Type I and Type Ⅱ , and then introduces two new inhibitors which have not been approved yet. The methods of finding new in- hibitors are also briefly summarized.