蛋白酪氨酸激酶信号转导途径与抗肿瘤药物  

Signal transduction by protein tyrosine kinases and antitumor agents

作　　者：茆勇军[1] 李海泓 李剑峰[1] 沈敬山[1] 

机构地区：[1]中国科学院上海药物研究所,上海201203 [2]上海特化医药科技有限公司,上海201209

出　　处：《药学学报》2008年第4期323-334,共12页Acta Pharmaceutica Sinica

摘　　要：细胞信号转导(signal transduction)在细胞的代谢、分裂、分化、生物功能及死亡过程中起着重要作用,肿瘤的发生和发展与细胞信号转导过度激活有关。本文简要阐述了蛋白酪氨酸激酶(prote in tyrosine k inases,PTKs)介导的信号转导途径,分别介绍了受体酪氨酸激酶介导的Ras/Raf/MAPK和PI-3K/Akt途径,非受体酪氨酸激酶介导的Src、Bcr-Ab l和JAK/STAT途径。以此5条信号转导通路中参与的重要蛋白分子为靶点,统计和介绍了相关的已经上市或处于临床研究的抗肿瘤药物。Intracellular signal transduction plays an important role in the process of cellular metabolism, segmentation, differentiation, biological behaviour and cell death. Overactive signal transduction relates to tumor development and progression. Signaling pathways operated by protein tyrosine kinases （PTKs） will be illuminated here briefly. The Ras/Raf/MAPK and PI-3K/Akt pathways through receptor protein tyrosine kinases （RTKs）, the Src, Bcr-Abl and JAK/STAT pathways by non-receptor protein tyrosine kinases （nrPTKs） are shown separately. Antitumor agents targeting the key proteins involved in the above five signalling routes are also summarized in this review.

关 键 词：信号转导 受体酪氨酸激酶 非受体酪氨酸激酶 酪氨酸激酶抑制剂 抗肿瘤药物 

分 类 号：R979.1[医药卫生—药品]