Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drugs Study, Hengyang Medical College, University of South China, Hengyang, China.
Department of Pharmacy, The First Affiliated Hospital, University of South China, Hengyang, China.
J Cell Physiol. 2019 Aug;234(8):12149-12160. doi: 10.1002/jcp.27942. Epub 2018 Dec 26.
APJ is a G protein-coupled receptor and its endogenous ligand is apelin. Studies have shown that apelin/APJ system is widely distributed in the body, especially highly expressed in the vascular endothelial cells (ECs). Numerous reports have demonstrated that apelin/APJ system plays an important role in the regulation of ECs function. Our lab has demonstrated that apelin-13 is able to promote adhesion of monocyte-human umbilical vein EC via 14-3-3, and reactive oxygen species-autophagy signaling pathways. In this review, we concentrate on the regulatory mechanism of apelin/APJ system in EC, including promotion of proliferation, migration, and angiogenesis. Moreover, we also analyze the role of apelin/APJ on endothelial dysfunction-related diseases including atherosclerosis, diabetes, hypertension, and myocardial infarction. Finally, we summarize the most commonly used agonists and antagonists of APJ. Therefore, apelin/APJ system is expected to be a therapeutic target for the treatment of endothelial dysfunction-related diseases.
APJ 是一种 G 蛋白偶联受体,其内源性配体是 Apelin。研究表明,Apelin/APJ 系统广泛分布于体内,尤其在血管内皮细胞(ECs)中高度表达。大量报道表明,Apelin/APJ 系统在调节 ECs 功能方面发挥着重要作用。本实验室已经证明,Apelin-13 通过 14-3-3 和活性氧物质自噬信号通路促进单核细胞与人脐静脉内皮细胞的黏附。在本综述中,我们集中讨论了 Apelin/APJ 系统在 EC 中的调节机制,包括促进增殖、迁移和血管生成。此外,我们还分析了 Apelin/APJ 在与内皮功能障碍相关的疾病中的作用,包括动脉粥样硬化、糖尿病、高血压和心肌梗死。最后,我们总结了 APJ 最常用的激动剂和拮抗剂。因此,Apelin/APJ 系统有望成为治疗与内皮功能障碍相关疾病的治疗靶点。