已上市酪氨酸激酶抑制剂抗肿瘤作用机制及构效关系研究

摘要

在人类基因组中发现了大约2000个激酶,其中超过90个为蛋白酪氨酸激酶,在靶向性抗肿瘤药物中,靶向酪氨酸激酶类的药物已成为研发热点,并且已获得巨大成功.本文综述了一类已上市的酪氨酸激酶抑制剂的研究进展,介绍了抑制剂结合受体蛋白的方式及其作用机制,重点讨论了这类药物的构效关系,发现分子对接的结构与真实构效关系基本一致.%There are about 2000 kinases in the human genome, of which more than 90 are protein tyrosine kinase. The drugs targeting at protein tyrosine kinase are a class of quite important anticancer drugs. This paper reviews the research advances on the small molecular tyrosine kinase inhibitors, the way of receptor protein binding with inhibitors and their mechanism. Emphasizing on summarizing the structure-activity relationship, it was found that the structure of molecular docking is consistent with that of real structure-activity relationship.