摘要
Wnt信号途径涉及一系列发育的过程,其异常激活可以导致多种癌症。《Nature》报道了一系列作用于Wnt信号途径的新型小分子抑制剂。这些小分子抑制剂的作用目标是端锚聚合酶Tankyrases,它负责控制降解Wnt信号途径中的β-catenin。在此过程中,E3泛素连接酶与Tankyrases的调控也有关联,泛素化蛋白酶系统起着重要的监管职能。通过这些新型的小分子抑制剂来调控Wnt信号途径及其核心部件可能为Wnt相关的癌症治疗提供一种新的手段。该文重点阐述了通过小分子化合物抑制Tankyrases作用于经典Wnt途径及其与癌症治疗的研究进展。
Wnt signaling is involved throughout development and maybe inappropriately actlvateo in a va-riety of human cancers. New study in Nature has identified small molecule inhibitor for Wnt pathway. Those inhibi-tors target an unsuspected cellular enzyme, Tankyrases, which controls the destruction of a β-catenin destructor. E3 ubiquitin ligases have been implicated in its regulation. The ubiquitinproteasome system plays important regulatory functions in Writ pathway by regulating the activity of several of its core components. The development of small molecule inhibitors may offer a novel therapeutic opportunity. In this review, we focus on the roles of how small chemical affect Tankyrases to inhibit canonical Wnt signaling.
出处
《中国细胞生物学学报》
CAS
CSCD
北大核心
2012年第11期1134-1140,共7页
Chinese Journal of Cell Biology
基金
国家留学基金委公派CSC(No.2008632066)资助项目~~
