Farnesyltransferase inhibitors in breast cancer therapy
Farnesyltransferase inhibitors in breast cancer therapy
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DOI：
10.1081/cnv-120014884
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发表时间：
2002-01-01
影响因子：
2.4
通讯作者：
Adjei, AA
中科院分区：
文献类型：
--
作者：
Dy, GK;Adjei, AA
法尼基转移酶抑制剂（FTIs）属于一组最初设计用于通过抑制Ras蛋白翻译后加工中的关键步骤来防止Ras蛋白膜附着的药物。因此，假设FTIs会减少在人类肿瘤中激活的致癌ras介导的增殖和抗凋亡信号。尽管Ras蛋白仅在< 5%的乳腺癌中发生突变，但存在多种导致野生型ras信号转导激活的异常途径。此外，无论其ras突变状态如何，FTI始终在肿瘤中显示出疗效。因此，正在阐明其他蛋白质靶点在介导FTIs抗肿瘤作用中的作用。本文回顾了目前的数据，在乳腺癌中使用的FTIs。
Farnesyltransferase inhibitors (FTIs) belong to a group of agents originally designed to prevent membrane attachment of Ras protein by inhibiting a key step in its post-translational processing. It was thus hypothesized that FTIs would curtail the oncogenic ras-mediated proliferative and antiapoptotic signals that are activated in human tumors. Although the Ras protein is mutated in only < 5% of breast cancers, there are multiple aberrant pathways that lead to activation of wildtype ras signaling. Moreover, FTIs have consistently demonstrated efficacy in tumors regardless of their ras mutational status. Thus, the role of other protein targets in mediating the antitumor effect of FTIs is being elucidated. This article reviews current data on the use of FTIs in breast cancer.