Small molecules targeting the selenoprotein thioredoxin reductase.

The selenoprotein thioredoxin reductase (TrxR) enzymes are the only identified proteins in maintaining the thioredoxin (Trx) proteins in a reduced state under physiological conditions, and play a pivotal role in regulating various cellular redox signaling pathways involved in cell differentiation, growth and death. The elevated expression of TrxR enzymes has been observed in different types of cancer cells, and this overexpression is of pathological significance in keeping the phenotypes of tumor, such as uncontrolled proliferation and resistance to apoptosis. In this Focus Review, we discussed the recent advances in TrxR studies, including the classic assays of TrxR, the emerging chemical tools of TrxR and small molecules targeting TrxR as potential anticancer agents.