癌症中蛋白激酶的小分子抑制剂——如何克服耐药性

Small molecule inhibitors of protein kinases in cancer- how to overcome resistance.

作者信息

Griffith R, Brown M N, McCluskey A, Ashman L K

机构信息

School of Environmental and Life Sciences, Faculty of Science and IT, University of Newcastle, Callaghan NSW 2308, Australia.

出版信息

Mini Rev Med Chem. 2006 Oct;6(10):1101-10. doi: 10.2174/138955706778560184.

DOI:10.2174/138955706778560184

PMID:17073710

Abstract

Small molecule protein kinase inhibitors show great promise as anti-cancer agents, however, de novo and acquired resistance present problems. These are reviewed and illustrated using the receptor tyrosine kinase, KIT, as an example. Emerging solutions are presented, such as targeting active kinase conformations.

摘要

小分子蛋白激酶抑制剂作为抗癌药物显示出巨大的前景，然而，原发性和获得性耐药带来了问题。本文以受体酪氨酸激酶KIT为例进行综述和说明。文中还介绍了一些新出现的解决方案，例如靶向活性激酶构象。