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基于喹唑啉的小分子通过miRNA的整体上调发挥抗癌治疗潜力。

Anti-cancer therapeutic potential of quinazoline based small molecules via global upregulation of miRNAs.

作者信息

Nahar Smita, Bose Debojit, Kumar Panja Sumit, Saha Satyen, Maiti Souvik

机构信息

Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, 2 Rafi Marg, New Delhi-110001, India.

出版信息

Chem Commun (Camb). 2014 May 7;50(35):4639-42. doi: 10.1039/c3cc49337g.

Abstract

Three quinazoline based small molecules showed global upregulation of miRNA expression with a selective enrichment of tumor suppressor miRNAs. The target genes of the upregulated miRNAs were predicted to be enriched for apoptotic pathways. Apoptotic induction following treatment with quinazoline compounds was confirmed by in cellulo studies. Thus, these small molecules having the core structural moiety (2,4-diphenyl-quinazoline) can be used as scaffolds to design activators of miRNA expression paving the way for novel anti-cancer drugs.

摘要

三种基于喹唑啉的小分子显示出miRNA表达的整体上调,并选择性富集了肿瘤抑制性miRNA。上调的miRNA的靶基因预计在凋亡途径中富集。喹唑啉化合物处理后的凋亡诱导通过细胞内研究得到证实。因此,这些具有核心结构部分(2,4-二苯基喹唑啉)的小分子可作为支架来设计miRNA表达激活剂,为新型抗癌药物铺平道路。

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