Department of Internal Medicine, University of Iowa, C32 GH, Iowa City, IA 52242, USA.
Curr Opin Pharmacol. 2012 Dec;12(6):704-9. doi: 10.1016/j.coph.2012.06.013. Epub 2012 Jul 18.
It has been over 20 years since it was first recognized that the function of both normal and oncogenic Ras is dependent on the post-translational modification termed farnesylation. Since that time, intense effort has been expended on the development of farnesyltransferase inhibitors as novel anticancer agents. Over 70 clinical trials have now been conducted, with limited efficacy demonstrated. Here we provide an update of the most recently published clinical trials, discuss the use of the RASGRP1/APTX two-gene expression screen to select patients with acute myeloid leukemia for therapy, and report on the latest discoveries related to the targets of prenyltransferase inhibitors.
自首次认识到正常和致癌 Ras 的功能依赖于被称为法呢基化的翻译后修饰以来，已经过去了 20 多年。自那时以来，人们一直在努力开发法尼基转移酶抑制剂作为新型抗癌药物。目前已经进行了超过 70 项临床试验，但疗效有限。在这里，我们提供了最新发表的临床试验的最新更新，讨论了使用 RASGRP1/APTX 双基因表达筛选来选择急性髓系白血病患者进行治疗的方法，并报告了与 prenyltransferase 抑制剂的靶点相关的最新发现。
