经改造的 IgG Fc 连接可延长氟苯尼考的半衰期并缓解小鼠肺炎。

Biochimie Pub Date : 2025-02-01 Epub Date: 2024-10-18 DOI:10.1016/j.biochi.2024.10.014
Shikun Ge, Mei Dang, Alberto Carlos Pires Dias, Xiaoying Zhang
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引用次数: 0

摘要

小分子药物的半衰期通常很短,需要频繁给药才能长期维持治疗浓度。众所周知,IgG 的片段可结晶(Fc)区通过与 Fc 新生受体的相互作用延长抗体的半衰期。为了解决这个问题,我们利用 IgG 的片段可结晶(Fc)区作为载体蛋白来延长小分子药物氟苯尼考的半衰期。氟苯尼考通过化学方法与在 HEK293 细胞中使用真核表达系统表达的重组 Fc 蛋白结合。与未结合的氟苯尼考相比,Fc-氟苯尼考结合体的半衰期大大延长,从3.8小时延长到9.1小时,并在治疗小鼠肺炎模型中表现出卓越的治疗特性。我们的研究结果以及对 Fc-小分子共轭物的文献分析表明,Fc 可大大延长药物的半衰期,并表明它有可能用作新型给药系统的载体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Engineered IgG Fc-conjugation prolongs the half-life of florfenicol and alleviates pneumonia in mice.

Small molecule drugs often exhibit short half-lives, requiring frequent administrations to maintain therapeutic concentrations over an extended period. To address this issue, the fragment crystallizable (Fc) region of IgG, known to prolong the half-life of antibodies via its interaction with the Fc neonatal receptor, was harnessed as a carrier protein to extend the half-life of a small molecule drug, florfenicol. Florfenicol, was chemically coupled to a recombinant Fc protein expressed using the eukaryotic expression system in HEK293 cells. The Fc-florfenicol conjugate exhibited a substantially prolonged half-life of from 3.8 to 9.1 h compared to unconjugated florfenicol and demonstrated excellent therapeutic properties in treating pneumonia in a mouse model. Our results, combined with the literature analysis on Fc-small molecule conjugates, show that Fc can substantially enhance the drug's half-life and suggest the potential for its use as a carrier in novel delivery systems.

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