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[蛋白酪氨酸激酶抑制剂在癌症治疗中的应用]

[Protein tyrosine kinase inhibitors in cancer therapy].

作者信息

Boutayeb S, Zakkouri F Z, Aitelhaj M, Mesmoudi M, Boutayeb A, Boutayeb W, Mrabti H, Errihani H

机构信息

Service d'oncologie médicale, institut national d'oncologie, CHU Ibn Sina, Rabat, Maroc.

出版信息

Pathol Biol (Paris). 2012 Aug;60(4):229-33. doi: 10.1016/j.patbio.2012.05.007. Epub 2012 Jun 26.

Abstract

The tyrosine kinase inhibitors (TKI) are small molecules of low molecular weight that inhibit tyrosine kinases, enzymes responsible for the activation of signal transduction cascades. Currently, a number of TKI received approval in various cancers, while others are in clinical development process: TKI are specifically clinically active when they target a tyrosine kinase (TK) with constitutional activity subsequent to a mutation, being then a master-gene driving transformation and tumour progression. Already, this drug-family provides a major therapeutic weapon against cancer.

摘要

酪氨酸激酶抑制剂(TKI)是低分子量的小分子,可抑制酪氨酸激酶,即负责激活信号转导级联反应的酶。目前,多种TKI已在各类癌症中获批,其他一些则正处于临床开发阶段:当TKI靶向因突变而具有组成性活性的酪氨酸激酶(TK)时,具有特异性临床活性,该酪氨酸激酶随后成为驱动肿瘤转化和进展的主基因。该药物家族已然成为对抗癌症的一种主要治疗手段。

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