激酶
酪氨酸激酶
癌症研究
受体酪氨酸激酶
生物
化学
细胞生物学
生物化学
信号转导
作者
M.E.M. Noble,Jane Endicott,L.N. Johnson
出处
期刊:Science
[American Association for the Advancement of Science (AAAS)]
日期:2004-03-19
卷期号:303 (5665): 1800-1805
被引量:1118
标识
DOI:10.1126/science.1095920
摘要
Protein kinases are targets for treatment of a number of diseases. This review focuses on kinase inhibitors that are in the clinic or in clinical trials and for which structural information is available. Structures have informed drug design and have illuminated the mechanism of inhibition. We review progress with the receptor tyrosine kinases (growth factor receptors EGFR, VEGFR, and FGFR) and nonreceptor tyrosine kinases (Bcr-Abl), where advances have been made with cancer therapeutic agents such as Herceptin and Gleevec. Among the serine-threonine kinases, p38, Rho-kinase, cyclin-dependent kinases, and Chk1 have been targeted with productive results for inflammation and cancer. Structures have provided insights into targeting the inactive or active form of the kinase, for targeting the global constellation of residues at the ATP site or less conserved additional pockets or single residues, and into targeting noncatalytic domains.
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