去泛素化酶在肿瘤中的作用及其抑制剂相关研究进展

The roles of deubiquitinating enzymes in cancer therapy

泛素化和去泛素化是机体中调控蛋白质降解的重要分子机制。去泛素化酶(deubiquitinating enzymes,DUB)通过多种分子通路参与调控肿瘤细胞的存活、增殖和侵袭等过程,在多种细胞生命活动中均扮演着重要角色。目前研究表明,尽管少数DUB具有一定的抑癌作用,但绝大多数DUB发挥着显著的促肿瘤作用,因此被认为是前景良好的抗肿瘤靶点;研究人员已针对这些致癌DUB开发了一系列小分子抑制剂。本文将对肿瘤相关DUB及抑制剂研究的最新进展进行综述。

Ubiquitination and deubiquitination play important roles in the regulation of protein stability and function. Deubiquitinating enzymes （DUBs） are involved in the regulation of survival, migration and proliferation of cancer cells, by participating in a variety of signaling pathways. Most of the DUBs promote the malignant transformation and progression, while the others may function as tumor-suppressors. Given the central roles of DUBs in tumorigenesis and malignant progression, some of these enzymes have been regarded as promising anti-cancer targets. This paper reviews the recent advances in tumor-related DUBs and inhibitors.