Department of Vascular Biology, Institute for Stroke and Dementia Research, Klinikum der Universität München, Ludwig-Maximilian-University (LMU) Munich, 81377 Munich, Germany.
Institute for Cardiovascular Prevention (IPEK), Klinikum der Universität München, Ludwig-Maximilian-University (LMU) Munich, 80336 Munich, Germany.
Cells. 2023 Jul 20;12(14):1899. doi: 10.3390/cells12141899.
Tissue inhibitor of metalloproteinases-1 (TIMP-1), an important regulator of matrix metalloproteinases (MMPs), has recently been shown to interact with CD74, a receptor for macrophage migration inhibitory factor (MIF). However, the biological effects mediated by TIMP-1 through CD74 remain largely unexplored. Using sequence alignment and in silico protein-protein docking analysis, we demonstrated that TIMP-1 shares residues with both MIF and MIF-2, crucial for CD74 binding, but not for CXCR4. Subcellular colocalization, immunoprecipitation, and internalization experiments supported these findings, demonstrating that TIMP-1 interacts with surface-expressed CD74, resulting in its internalization in a dose-dependent manner, as well as with a soluble CD74 ectodomain fragment (sCD74). This prompted us to study the effects of the TIMP-1-CD74 axis on monocytes and vascular smooth muscle cells (VSCMs) to assess its impact on vascular inflammation. A phospho-kinase array revealed the activation of serine/threonine kinases by TIMP-1 in THP-1 pre-monocytes, in particular AKT. Similarly, TIMP-1 dose-dependently triggered the phosphorylation of AKT and ERK1/2 in primary human monocytes. Importantly, Transwell migration, 3D-based Chemotaxis, and flow adhesion assays demonstrated that TIMP-1 engagement of CD74 strongly promotes the recruitment response of primary human monocytes, while live cell imaging studies revealed a profound activating effect on VSMC proliferation. Finally, re-analysis of scRNA-seq data highlighted the expression patterns of TIMP-1 and CD74 in human atherosclerotic lesions, thus, together with our experimental data, indicating a role for the TIMP-1-CD74 axis in vascular inflammation and atherosclerosis.
基质金属蛋白酶组织抑制剂-1(TIMP-1)是基质金属蛋白酶(MMPs)的重要调节剂,最近研究表明它与巨噬细胞移动抑制因子(MIF)的受体 CD74 相互作用。然而,TIMP-1 通过 CD74 介导的生物学效应在很大程度上仍未得到探索。通过序列比对和计算机蛋白-蛋白对接分析,我们证明 TIMP-1 与 MIF 和 MIF-2 共享关键的 CD74 结合残基,但不与 CXCR4 结合。亚细胞共定位、免疫沉淀和内化实验支持了这些发现,表明 TIMP-1 与表面表达的 CD74 相互作用,导致其以剂量依赖的方式内化,以及与可溶性 CD74 胞外结构域片段(sCD74)相互作用。这促使我们研究 TIMP-1-CD74 轴对单核细胞和血管平滑肌细胞(VSCMs)的影响,以评估其对血管炎症的影响。磷酸激酶阵列显示 TIMP-1 在 THP-1 前单核细胞中激活丝氨酸/苏氨酸激酶,特别是 AKT。同样,TIMP-1 剂量依赖性地触发原代人单核细胞中 AKT 和 ERK1/2 的磷酸化。重要的是,Transwell 迁移、基于 3D 的趋化性和流动黏附测定表明,TIMP-1 与 CD74 的结合强烈促进原代人单核细胞的募集反应,而活细胞成像研究显示对 VSMC 增殖有深远的激活作用。最后,对 scRNA-seq 数据的重新分析突出了 TIMP-1 和 CD74 在人类动脉粥样硬化病变中的表达模式,因此,结合我们的实验数据,表明 TIMP-1-CD74 轴在血管炎症和动脉粥样硬化中起作用。