Abstract: Thioredoxin reductase (TrxR) is a major functional protein in the thioredoxin system (Trx) and plays a key role in regulating various cellular redox signaling pathways. In recent years, TrxR/Trx has been increasingly recognized as an important regulator of tumor development, therefore, targeting TrxR/Trx is a promising tumor treatment strategy. In this paper, the structural characteristics, tumor-related physiological functions and inhibitors of TrxR were reviewed to provide references for the research of TrxR.