Dantas Pedro H S, Matos Amanda O, Colmenares Mike T C, Costa Vinícius A F, Felice Andrei G, Neto José R C, Soares Siomar C, Silva-Sales Marcelle, Neves Bruno J, Sales-Campos Helioswilton
Laboratory of Mucosal Immunology and Immunoinformatics, Institute of Tropical Pathology and Public Health, Federal University of Goias, Goiânia, Goiás, Brazil.
Laboratory of Cheminformatics, Faculty of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
J Mol Graph Model. 2025 Jul;138:109058. doi: 10.1016/j.jmgm.2025.109058. Epub 2025 Apr 17.
The Triggering Receptor Expressed on Myeloid cells 2 (TREM2) is an immune receptor with three complementarity-determining regions (CDR1-3) that primarily interact with the receptor's ligands. Aside from its role in reducing inflammation, enhancing phagocytosis, and contributing to cellular maturation and survival, TREM2 also contributes to the pathophysiology of neurodegenerative disorders, cancer, and metabolic diseases. Therefore, understanding how the receptor interacts with its ligands is essential to mitigate its adverse effects and/or to foster the development of new therapeutic approaches. Thus, our research focused on understanding the interactions between TREM2 and its protein ligands: APOA1, APOA2, APOE3, APOE4, APOJ, C1q, Galectin-3, cyclophilin A, Heat shock protein 60 (HSP60), IL-34, IL-4, the SARS-CoV-2 membrane protein and the cholera toxin subunit B, TDP-43 using in silico methods, such as molecular docking and molecular dynamics simulations. TREM2 showed a higher affinity and stability with HSP60, APOA2, Cyclophilin A, Galectin-3, TDP-43 and C1q when compared to the other protein ligands. Notably, our data suggest that TREM2 interacts with its ligands predominantly through the CDR2 region by the following residues: N68, L69, W70, L71, L72, F74 and R76. Our findings indicate that the CDR2 region can be a crucial target for the development of inhibitory or agonistic approaches targeting the receptor's activity.
髓系细胞表达的触发受体2(TREM2)是一种免疫受体,具有三个互补决定区(CDR1 - 3),主要与该受体的配体相互作用。除了在减轻炎症、增强吞噬作用以及促进细胞成熟和存活方面发挥作用外,TREM2还与神经退行性疾病、癌症和代谢性疾病的病理生理学有关。因此,了解该受体如何与其配体相互作用对于减轻其不良反应和/或促进新治疗方法的开发至关重要。因此,我们的研究重点是了解TREM2与其蛋白质配体之间的相互作用:载脂蛋白A1(APOA1)、载脂蛋白A2(APOA2)、载脂蛋白E3(APOE3)、载脂蛋白E4(APOE4)、载脂蛋白J(APOJ)、补体C1q、半乳糖凝集素-3、亲环蛋白A、热休克蛋白60(HSP60)、白细胞介素-34(IL - 34)、白细胞介素-4(IL - 4)、严重急性呼吸综合征冠状病毒2(SARS-CoV-2)膜蛋白、霍乱毒素亚基B、TDP-43,采用分子对接和分子动力学模拟等计算机模拟方法。与其他蛋白质配体相比,TREM2与HSP60、APOA2、亲环蛋白A、半乳糖凝集素-3、TDP-43和C1q表现出更高的亲和力和稳定性。值得注意的是,我们的数据表明,TREM2主要通过CDR2区域与配体相互作用,涉及以下残基:N68、L69、W70、L71、L72、F74和R76。我们的研究结果表明,CDR2区域可能是开发针对该受体活性的抑制或激动方法的关键靶点。