血管硫醇异构酶：结构、调控机制及抑制剂开发
Vascular thiol isomerases: Structures, regulatory mechanisms, and inhibitor development.
作者信息
Liang Chenghui, Flaumenhaft Robert, Yuan Cai, Huang Mingdong
机构信息
College of Biological Science and Engineering, Fuzhou University, Fuzhou, Fujian 350108, China.
Division of Hemostasis and Thrombosis, Beth Israel Deaconess Medical Center, Harvard Medical School, 330 Brookline Avenue, Boston, MA 02215, USA.
出版信息
Drug Discov Today. 2022 Feb;27(2):626-635. doi: 10.1016/j.drudis.2021.10.018. Epub 2021 Oct 29.
Vascular thiol isomerases (VTIs), including PDI, ERp5, ERp57, ERp72, and thioredoxin-related transmembrane protein 1 (TMX1), have important roles in platelet aggregation and thrombosis. Research on VTIs, their substrates in thrombosis, their regulatory mechanisms, and inhibitor development is an emerging and rapidly evolving area in vascular biology. Here, we describe the structures and functions of VTIs, summarize the relationship between the vascular TIs and thrombosis, and focus on the development of VTI inhibitors for antithrombotic applications.
血管硫醇异构酶（VTI），包括蛋白二硫键异构酶（PDI）、内质网蛋白5（ERp5）、内质网蛋白57（ERp57）、内质网蛋白72（ERp72）和硫氧还蛋白相关跨膜蛋白1（TMX1），在血小板聚集和血栓形成中发挥重要作用。对VTI、其在血栓形成中的底物、其调节机制以及抑制剂开发的研究是血管生物学中一个新兴且快速发展的领域。在此，我们描述VTI的结构和功能，总结血管硫醇异构酶与血栓形成之间的关系，并着重介绍用于抗血栓应用的VTI抑制剂的开发。
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