Boutayeb S, Zakkouri F Z, Aitelhaj M, Mesmoudi M, Boutayeb A, Boutayeb W, Mrabti H, Errihani H
Service d'oncologie médicale, institut national d'oncologie, CHU Ibn Sina, Rabat, Maroc.
Pathol Biol (Paris). 2012 Aug;60(4):229-33. doi: 10.1016/j.patbio.2012.05.007. Epub 2012 Jun 26.
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.
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。