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.

硫氧还蛋白（Trx）和硫氧还蛋白还原酶（TrxR）是Trx系统的重要组成部分，在调节多个细胞氧化还原信号通路中起着关键作用。近年来，TrxR / Trx被越来越多地认为是肿瘤发展的重要调节剂，因此靶向TrxR / Trx是一种有前途的癌症治疗策略。在这篇综述中，我们首先讨论TrxR的结构细节，Trx系统的功能以及针对TrxR / Trx进行癌症治疗的合理性。我们还将重点介绍具有潜在抗癌活性的小分子TrxR / Trx抑制剂，并综述其作用机理。最后，我们研究了开发TrxR / Trx抑制剂作为抗癌药所面临的挑战以及选择性靶向TrxR / Trx的前景。