Yang Yiyuan, Zhou Qionglin, Gao Anbo, Chen Linxi, Li Lanfang
Institute of Pharmacy and Pharmacology, Learning Key Laboratory for Pharmacoproteomics, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China.
Institute of Pharmacy and Pharmacology, Learning Key Laboratory for Pharmacoproteomics, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China.
Clin Chim Acta. 2020 May;504:125-137. doi: 10.1016/j.cca.2020.01.031. Epub 2020 Feb 1.
Endoplasmic reticulum (ER) is an intracellular membranous organelle involved in the synthesis, folding, maturation and post-translation modification of secretory and transmembrane proteins. Therefore, ER is closely related to the maintenance of intracellular homeostasis and the good balance between health and diseases. Endoplasmic reticulum stress (ERS) occurs when unfolded/misfolded proteins accumulate after disturbance of ER environment. In response to ERS, cells trigger an adaptive response called the Unfolded protein response (UPR), which helps cells cope with the stress. In recent years, a large number of studies show that ERS can aggravate cardiovascular diseases. ERS-related proteins expression in cardiovascular diseases is on the rise. Therefore, down-regulation of ERS is critical for alleviating symptoms of cardiovascular diseases, which may be used in the near future to treat cardiovascular diseases. This article reviews the relationship between ERS and cardiovascular diseases and drugs that inhibit ERS. Furthermore, we detail the role of ERS inhibitors in the treatment of cardiovascular disease. Drugs that inhibit ERS are considered as promising strategies for the treatment of cardiovascular diseases.
内质网（ER）是一种细胞内膜性细胞器，参与分泌蛋白和跨膜蛋白的合成、折叠、成熟及翻译后修饰。因此，内质网与细胞内稳态的维持以及健康与疾病之间的良好平衡密切相关。当内质网环境受到干扰后未折叠/错误折叠的蛋白质积累时，就会发生内质网应激（ERS）。作为对ERS的反应，细胞会触发一种称为未折叠蛋白反应（UPR）的适应性反应，该反应有助于细胞应对应激。近年来，大量研究表明，ERS会加重心血管疾病。心血管疾病中与ERS相关的蛋白质表达正在上升。因此，下调ERS对于缓解心血管疾病症状至关重要，这在不久的将来可能用于治疗心血管疾病。本文综述了ERS与心血管疾病之间的关系以及抑制ERS的药物。此外，我们详细阐述了ERS抑制剂在心血管疾病治疗中的作用。抑制ERS的药物被认为是治疗心血管疾病的有前景的策略。
