Sir James Black Centre, Dundee, Scotland, UK.
Cell. 2010 Nov 24;143(5):686-93. doi: 10.1016/j.cell.2010.11.016.
Protein phosphorylation and protein ubiquitination regulate most aspects of cell life, and defects in these control mechanisms cause cancer and many other diseases. In the past decade, protein kinases have become one of the most important classes of drug targets for the pharmaceutical industry. In contrast, drug discovery programs that target components of the ubiquitin system have lagged behind. In this Perspective, we discuss the reasons for the delay in this pipeline, the drugs targeting the ubiquitin system that have been developed, and new approaches that may popularize this area of drug discovery in the future.
蛋白质磷酸化和蛋白质泛素化调节细胞生命的各个方面,这些控制机制的缺陷会导致癌症和许多其他疾病。在过去的十年中,蛋白激酶已成为制药行业最重要的药物靶点之一。相比之下,针对泛素系统成分的药物发现计划却落后了。在本文中,我们讨论了这条管线延迟的原因、已经开发的针对泛素系统的药物,以及未来可能使这一药物发现领域普及的新方法。