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Review
. 2017 Sep;38(9):794-808.
doi: 10.1016/j.tips.2017.06.001. Epub 2017 Jun 22.

Targeting the Thioredoxin System for Cancer Therapy

Junmin Zhang  1 , Xinming Li  2 , Xiao Han  2 , Ruijuan Liu  1 , Jianguo Fang  3
Affiliations
Review

Targeting the Thioredoxin System for Cancer Therapy

Junmin Zhang et al. Trends Pharmacol Sci. 2017 Sep.

Abstract

Thioredoxin (Trx) and thioredoxin reductase (TrxR) are essential components of the Trx system which plays pivotal roles in regulating multiple cellular redox signaling pathways. In recent years TrxR/Trx have been increasingly recognized as an important modulator of tumor development, and hence targeting TrxR/Trx is a promising strategy for cancer treatment. In this review we first discuss the structural details of TrxR, the functions of the Trx system, and the rational of targeting TrxR/Trx for cancer treatment. We also highlight small-molecule TrxR/Trx inhibitors that have potential anticancer activity and review their mechanisms of action. Finally, we examine the challenges of developing TrxR/Trx inhibitors as anticancer agents and perspectives for selectively targeting TrxR/Trx.

Keywords: cancer therapy; reactive oxygen species; redox regulation; selenocysteine; thioredoxin.

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