诱导蛋白降解的小分子PROTACs的研究进展
发布时间:2018-02-21 19:42
本文关键词: 蛋白降解 PROTACs 药物设计 靶点 进展 出处:《中国新药杂志》2017年22期 论文类型:期刊论文
【摘要】:利用小分子蛋白降解靶向嵌合体(PROTACs)诱导蛋白降解的新型肿瘤治疗策略能够通过细胞内泛素-蛋白酶体降解系统而调控靶蛋白水平,从而克服传统小分子抑制剂的缺陷。因此针对小分子PROTACs的设计、合成及表征成为当前药物化学研究的前沿之一。本文简介小分子PROTACs的功能及作用机制,着重综述小分子PROTACs的最新研究成果,展望其应用前景和亟需解决的问题。
[Abstract]:A novel tumor therapy strategy for protein degradation induced by small molecular protein degradation target chimera (PROTACs) can regulate target protein level through intracellular ubiquitin proteasome degradation system. Therefore, the design, synthesis and characterization of small molecular PROTACs have become one of the frontiers in the field of drug chemistry. In this paper, the function and mechanism of small molecule PROTACs are briefly introduced. The latest research results of small molecule PROTACs are reviewed, and its application prospect and problems that need to be solved are prospected.
【作者单位】: 中国药科大学药学院;
【基金】:国家自然科学基金(21372260)
【分类号】:R979.1
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本文编号:1522713
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