Identification of phenazine analogue as a novel scaffold for thioredoxin reductase I inhibitors against Hep G2 cancer cell lines

Identification of phenazine analogue as a novel scaffold for thioredoxin reductase I inhibitors against Hep G2 cancer cell lines
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吩嗪类似物作为抗 Hep G2 癌细胞系硫氧还蛋白还原酶 I 抑制剂的新型支架的鉴定

DOI:
10.1080/14756366.2019.1624541
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发表时间:
2019-01
影响因子:
5.6
通讯作者:
Lu Yuanyuan
Lu Yuanyuan
中科院分区:
医学2区
文献类型:
--
作者:
Liao Jianming;Wang Linlin;Wu Zhongxi;Wang Zhixiang;Chen Jun;Zhong Yucheng;Jiang Feng;Lu Yuanyuan

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摘要吩嗪类化合物作为抗癌分子已被广泛报道,但其分子靶点研究却严重滞后。因此,我们的研究集中在吩嗪类似物(CPUL 1)的抗癌靶点,因为它在初始阶段具有强大的抗肿瘤活性。沿着Hep G2细胞氧化还原状态的变化,推测硫氧还蛋白还原酶I(TrxR1)是CPUL 1的抗癌靶点。通过酶学、免疫学和分子生物学实验,我们证明了TrxR1可能是CPUL1的抗癌靶点。关于吩嗪靶向TrxR1的研究未见报道。因此,它可以为进一步开发TrxR1抑制剂提供有价值的信息。
Abstract Even though phenazines have been extensively reported as anticancer molecules, the molecular target of these compounds is severely lagging behind. Our study consequently focuses on the anticancer target of a phenazine analogue (CPUL1) for its potently antitumor activities in initial stage. Along with redox status courses of Hep G2 cells, thioredoxin reductase I (TrxR1) was speculated as anticancer target of CPUL1. By virtue of zymologic, immunological and molecular biological experiments, we demonstrated that TrxR1 could be the anticancer target of CPUL1. The knowledge on phenazine targeting to TrxR1 have not been reported previously. Thus, it can provide valuable information for further development of the TrxR1 inhibitors.
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