| 引用本文: | 倪欣,黄坤,马俊杰.Procaspase-3小分子激活剂的研究进展[J].中国现代应用药学,2019,36(3):368-371. |
| NI Xin,HUANG Kun,MA Junjie.Research Progress of Procaspase-3 Small Molecule Activators[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(3):368-371. |
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| 摘要: |
| 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。 |
| 关键词: procaspase-3 抗肿瘤 小分子激活剂 细胞凋亡 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.03.023 |
| 分类号:R966 |
| 基金项目:国家自然科学基金项目（81602970）；福建省自然科学基金项目（2017J01143）；华侨大学科研启动项目（15BS415） |
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| Research Progress of Procaspase-3 Small Molecule Activators |
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NI Xin, HUANG Kun, MA Junjie
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Medical College of Huaqiao University, Engineering Research Center of Molecular Medicine of Ministry of Education, Quanzhou 362021, China
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| Abstract: |
| 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. |
| Key words: procaspase-3 antitumor small molecule activator apoptosis |
