Small Molecules to Target the Selenoprotein Thioredoxin Reductase
Small Molecules to Target the Selenoprotein Thioredoxin Reductase
复制标题
靶向硒蛋白硫氧还蛋白还原酶的小分子
DOI：
10.1002/asia.201801136
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发表时间：
2018
期刊：
影响因子：
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通讯作者：
Jianguo Fang
中科院分区：
文献类型：
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作者：
Baoxin Zhang;Yuxin Liu;Xinming Li;Jiangqiang Xu;Jianguo Fang
硒蛋白硫氧还蛋白还原酶（TrxR）是唯一已鉴定的在生理条件下维持硫氧还蛋白（Trx）蛋白处于还原状态的蛋白质，因此在调节参与细胞分化的各种细胞氧化还原信号通路中发挥关键作用、生长和死亡。在不同类型的癌细胞中已经观察到TrxR酶的表达升高，并且这种过表达在维持肿瘤表型中具有病理学意义，例如不受控制的增殖和对凋亡的抗性。在此，我们讨论了TrxR研究的最新进展，包括TrxR的经典测定，TrxR的新兴化学工具，以及靶向TrxR作为潜在抗癌剂的小分子。
The selenoprotein thioredoxin reductase (TrxR) enzymes are the only identified proteins that maintain thioredoxin (Trx) proteins in a reduced state under physiological conditions, and consequently play a pivotal role in the regulation of 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 maintaining tumor phenotypes, such as uncontrolled proliferation and resistance to apoptosis. Herein, we discuss recent advances in the study of TrxR, including classic assays of TrxR, the emerging chemical tools of TrxR, and small molecules that target TrxR as potential anticancer agents.