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Stabilizing protein pharmaceuticals by imidazolium-type zwitterions
Physical Chemistry Chemical Physics ( IF 2.9 ) Pub Date : 2025-01-31 , DOI: 10.1039/d4cp04439h
Ai Tajiri, Takeru Ishizaki, Takahiro Takekiyo, Kazuaki Ninomiya, Kenji Takahashi, Kosuke Kuroda
Physical Chemistry Chemical Physics ( IF 2.9 ) Pub Date : 2025-01-31 , DOI: 10.1039/d4cp04439h
Ai Tajiri, Takeru Ishizaki, Takahiro Takekiyo, Kazuaki Ninomiya, Kenji Takahashi, Kosuke Kuroda
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An imidazolium-carboxylate-type zwitterion, OE2imC3C, thermally stabilizes the structure in the vicinity of heme in cytochrome c. However, it remains unclear whether OE2imC3C can thermally stabilize protein pharmaceuticals, which are vulnerable to heating and shaking during production and transportation. In this study, we investigated the stabilization of the entire structure and function of insulin by OE2imC3C. Insulin in the 60 wt% OE2imC3C solution did not aggregate under shaking and heating (1000 rpm and 80 °C) and retained its folded structure. The shaked and heated insulin also exhibited normal function in cell proliferation. In contrast, the secondary structure of insulin in the 40 wt% OE2imC3C solution changed, and insulin in the 20 wt% OE2imC3C solution aggregated after shaking and heating. Therefore, the 60 wt% OE2imC3C solution has potential to stabilize protein pharmaceuticals.
中文翻译:
咪唑鎓型两性离子稳定蛋白药物
咪唑羧酸酯型两性离子 OE2imC3C 在细胞色素 c 中对血红素附近的结构进行热稳定。然而,目前尚不清楚 OE2imC3C 是否能对蛋白质药物进行热稳定,因为蛋白质药物在生产和运输过程中容易受到加热和摇晃。在这项研究中,我们研究了 OE2imC3C 对胰岛素整个结构和功能的稳定性。60 wt% OE2imC3C 溶液中的胰岛素在摇动和加热(1000 rpm 和 80 °C)下没有聚集,并保留了其折叠结构。摇动和加热的胰岛素在细胞增殖中也表现出正常功能。相比之下,40 wt% OE2imC3C 溶液中胰岛素的二级结构发生了变化,20 wt% OE2imC3C 溶液中的胰岛素在摇动和加热后聚集。因此,60 wt% OE2imC3C 溶液具有稳定蛋白质药物的潜力。
更新日期:2025-01-31
中文翻译:

咪唑鎓型两性离子稳定蛋白药物
咪唑羧酸酯型两性离子 OE2imC3C 在细胞色素 c 中对血红素附近的结构进行热稳定。然而,目前尚不清楚 OE2imC3C 是否能对蛋白质药物进行热稳定,因为蛋白质药物在生产和运输过程中容易受到加热和摇晃。在这项研究中,我们研究了 OE2imC3C 对胰岛素整个结构和功能的稳定性。60 wt% OE2imC3C 溶液中的胰岛素在摇动和加热(1000 rpm 和 80 °C)下没有聚集,并保留了其折叠结构。摇动和加热的胰岛素在细胞增殖中也表现出正常功能。相比之下,40 wt% OE2imC3C 溶液中胰岛素的二级结构发生了变化,20 wt% OE2imC3C 溶液中的胰岛素在摇动和加热后聚集。因此,60 wt% OE2imC3C 溶液具有稳定蛋白质药物的潜力。