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即将问世的受体酪氨酸激酶抑制剂。

Forthcoming receptor tyrosine kinase inhibitors.

作者信息

Choong Nicholas W, Cohen Ezra E W

出版信息

Expert Opin Ther Targets. 2006 Dec;10(6):793-7. doi: 10.1517/14728222.10.6.793.

Abstract

Receptor tyrosine kinases play a significant role in carcinogenesis and have been successfully targeted with monoclonal antibodies and small-molecule inhibitors. There have been recent developments in the understanding of receptor tyrosine kinase signal transduction which have enabled better drug development. The use of receptor tyrosine kinase inhibitors in clinical practice has expanded the knowledge on cancer biology, in particular the understanding of resistant mutations and strategies to overcome such resistance. This has driven drug development from single kinase inhibitors to multi-kinase inhibitors and high-affinity kinase inhibitors. Finally, as the use of receptor tyrosine kinase inhibitors grows in clinical practice, more is learned about appropriate patient selection for such therapies. This is an exciting time in cancer therapeutics, highlighted by the advent of effective targeted therapy with receptor tyrosine kinase inhibitors.

摘要

受体酪氨酸激酶在癌症发生过程中发挥着重要作用,并且已成功地用单克隆抗体和小分子抑制剂作为靶点。最近在受体酪氨酸激酶信号转导的理解方面取得了进展,这使得更好的药物开发成为可能。受体酪氨酸激酶抑制剂在临床实践中的应用扩展了对癌症生物学的认识,特别是对耐药突变以及克服此类耐药性策略的理解。这推动了药物开发从单一激酶抑制剂向多激酶抑制剂和高亲和力激酶抑制剂的转变。最后,随着受体酪氨酸激酶抑制剂在临床实践中的应用不断增加,人们对这类疗法的合适患者选择有了更多了解。这是癌症治疗中一个令人兴奋的时期,有效的受体酪氨酸激酶抑制剂靶向治疗的出现突显了这一点。

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