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

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journal contribution
posted on 2019-06-10, 06:48 authored by Jianming Liao, Linlin Wang, Zhongxi Wu, Zhixiang Wang, Jun Chen, Yucheng Zhong, Feng Jiang, Yuanyuan Lu

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.

Funding

The study received financial support from National Key R&D Program of China (2018YFC0311003), the Project Program of National Nature Science Foundation of China (Grant No. 81872757), the Project Program of Nature Science Foundation of Jiangsu Province of China for Young Scientists (Grant No. BK20130648), the Priority Academic Program Development of Jiangsu Higher Education Institution and Qing Lan Project.

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