Drug Discovery Research Center, Southwest Medical University, Luzhou, China.
Department of Pharmacology, Laboratory for Cardiovascular Pharmacology, The School of Pharmacy, Southwest Medical University, Luzhou, China.
J Cell Mol Med. 2021 Aug;25(15):7462-7471. doi: 10.1111/jcmm.16777. Epub 2021 Jul 9.
Mitsugumin 53 (MG53), which is expressed predominantly in striated muscle, has been demonstrated to be a myokine/cardiokine secreted from striated muscle under specific conditions. The important roles of MG53 in non-striated muscle tissues have also been examined in multiple disease models. However, no previous study has implicated MG53 in the control of endothelial cell function. In order to explore the effects of MG53 on endothelial cells, human umbilical vein endothelial cells (HUVECs) were stimulated with recombinant human MG53 (rhMG53). Then, rhMG53 uptake, focal adhesion kinase (FAK)/Src/Akt/ERK1/2 signalling pathway activation, cell migration and tube formation were determined in vitro. The efficacy of rhMG53 in regulating angiogenesis was also detected in postnatal mouse retinas. The results demonstrated that rhMG53 directly entered into endothelial cells in a cholesterol-dependent manner. The uptake of rhMG53 directly bound to FAK in endothelial cells, which resulted in a significant decrease in FAK phosphorylation at Y397. Accompanied by the dephosphorylation of FAK, rhMG53 uncoupled FAK-Src interaction and reduced the phosphorylation of Src at Y416. Consequently, the activation of FAK/Src downstream signalling pathways, such as Akt and ERK1/2, was also significantly inhibited by rhMG53. Furthermore, rhMG53 remarkably decreased HUVEC migration and tube formation in vitro and postnatal mouse retinal angiogenesis in vivo. Taken together, these data indicate that rhMG53 inhibits angiogenesis through regulating FAK/Src/Akt/ERK1/2 signalling pathways. This may provide a novel molecular mechanism for the impaired angiogenesis in ischaemic diseases.
肌联蛋白 53(MG53)主要表达于横纹肌,已被证实是横纹肌在特定条件下分泌的一种肌肉因子/心脏因子。在多种疾病模型中,也研究了 MG53 在非横纹肌组织中的重要作用。然而,以前没有研究表明 MG53 参与内皮细胞功能的调控。为了研究 MG53 对内皮细胞的影响,用重组人 MG53(rhMG53)刺激人脐静脉内皮细胞(HUVEC)。然后,在体外测定 rhMG53 的摄取、粘着斑激酶(FAK)/Src/Akt/ERK1/2 信号通路的激活、细胞迁移和管形成。还检测了 rhMG53 在新生小鼠视网膜中对血管生成的调节作用。结果表明,rhMG53 以胆固醇依赖的方式直接进入内皮细胞。rhMG53 的摄取直接与内皮细胞中的 FAK 结合,导致 FAK 在 Y397 位的磷酸化显著减少。伴随着 FAK 的去磷酸化,rhMG53 解偶联了 FAK-Src 相互作用,降低了 Src 在 Y416 位的磷酸化。因此,rhMG53 还显著抑制了 FAK/Src 下游信号通路的激活,如 Akt 和 ERK1/2。此外,rhMG53 显著减少了 HUVEC 的迁移和管形成以及体内新生小鼠视网膜血管生成。总之,这些数据表明,rhMG53 通过调节 FAK/Src/Akt/ERK1/2 信号通路抑制血管生成。这可能为缺血性疾病中受损的血管生成提供了一个新的分子机制。