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J Enzyme Inhib Med Chem. 2019 Dec;34(1):1158-1163. doi: 10.1080/14756366.2019.1624541.

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

Author information

1
a School of Life Science and Technology , China Pharmaceutical University , Nanjing , China.
2
b School of Engineering , China Pharmaceutical University , Nanjing , China.

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.

KEYWORDS:

Anticancer target; Hep G2; inhibitors; phenazines; thioredoxin reductase I

PMID:
31179772
PMCID:
PMC6567043
DOI:
10.1080/14756366.2019.1624541
[Indexed for MEDLINE]
Free PMC Article

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