Journal of Enzyme Inhibition and Medicinal Chemistry (Jan 2019)

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

  • Jianming Liao,
  • Linlin Wang,
  • Zhongxi Wu,
  • Zhixiang Wang,
  • Jun Chen,
  • Yucheng Zhong,
  • Feng Jiang,
  • Yuanyuan Lu

DOI
https://doi.org/10.1080/14756366.2019.1624541
Journal volume & issue
Vol. 34, no. 1
pp. 1158 – 1163

Abstract

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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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