Procaspase-3小分子激活剂的研究进展

Caspase-3作为细胞凋亡通路的下游关键执行蛋白，在细胞凋亡信号传导中扮演着重要的角色。开发直接通过激活高表达状态的procaspase-3成为caspase-3，进而重启肿瘤细胞凋亡的小分子药物，已成为克服中/上游凋亡蛋白突变的有效策略。目前，以procaspase-3为靶点已经报道了一些特异性小分子激活剂，至今还没有上市药物，开发直接激活procaspase-3的新型药物仍然是一项重要和艰难的挑战。本文介绍了procaspase-3与肿瘤之间的关系及小分子procaspase-3激活剂的研究进展。

Research Progress of Procaspase-3 Small Molecule Activators

Caspase-3 plays a very important role in the apoptotic cascade as the downstream key executioner caspase. Identification of small molecules that restart the apoptosis of tumor cells by directly activating over-expression procaspase-3 to active caspase-3 has become an effective strategy for overcoming the mutation of the middle/upstream apoptotic protein. Currently, some procaspase-3 small molecule activators have been reported, but no marketed drugs are available so far. The development of procaspase-3 activator remains an important and difficult challenge. In this article, the relationship between procaspase-3 and tumor and the research progress of procaspase-3 small molecule activators were introduced.