蛋白质二硫酸异构酶（PDI）及其超家族主要是内质网（ER）定位的蛋白质，通过巯基氧化/还原循环、分子伴侣作用和客体蛋白质异构化等方式维持细胞内稳态，具有维持细胞内稳态的重要作用。由于PDI在ER稳态中的重要性，其上调有助于细胞存活，且在多种癌症类型中都有发现。尽管尚不完全了解PDI对肿瘤发生的重要性，但它正逐渐成为癌症治疗的新靶点。在过去的十年中，已经研发和商业化了一些PDI抑制剂，但尚未获得临床使用的批准。在本综述中，我们讨论了ER中PDI的特性和氧化还原调节，并概述了过去5年来有关PDI抑制剂的研究进展。版权所有© 2023 Elsevier Inc. 发表。

Protein disulfide isomerase (PDI) and its superfamilies are mainly endoplasmic reticulum (ER) resident proteins with essential roles in maintaining cellular homeostasis, via thiol oxidation/reduction cycles, chaperoning, and isomerization of client proteins. Since PDIs play an important role in ER homeostasis, their upregulation supports cell survival and they are found in a variety of cancer types. Despite the fact that the importance of PDI to tumorigenesis remains to be understood, it is emerging as a new therapeutic target in cancer. During the past decade, several PDI inhibitors has been developed and commercialized, but none has been approved for clinical use. In this review, we discuss the properties and redox regulation of PDIs within the ER and provide an overview of the last 5 years of advances regarding PDI inhibitors.Copyright © 2023. Published by Elsevier Inc.