蛋白质二硫键异构酶的结构及抑制剂研究进展

蛋白质二硫键异构酶(PDI)可催化二硫键的形成、断裂和重排,并促进蛋白质折叠,对稳定蛋白质的三维结构至关重要. PDI的表达或酶活性的失调与一系列疾病如癌症、神经退行性疾病、血栓形成等密切相关.本文综述了PDI结构、与疾病的关系及其抑制剂的研究进展,并指出目前PDI抑制剂存在的问题及未来发展方向,以期为PDI抑制剂的进一步研究提供参考.

Progress in the structural studies and inhibitor development of protein disulfide isomerase

Protein disulfide isomerase (PDI) can catalyze the formation, breakage and rearrangement of disulfide bonds, and promote protein folding, which is essential to stabilize the three-dimensional structure of proteins. The dysregulation of PDI expression or enzyme activity is closely related to a series of diseases, such as cancer, neurodegenerative diseases, and thrombosis. In this review, we summarized the structure of PDI, its relationship with diseases and the research progress of its inhibitors. We also pointed out the current problems and the development direction of PDI inhibitors, which will provide references for its further research.