Department of Biomedical Engineering, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.
Institute of Biotechnology of the Academy of Sciences of the Czech Republic, Vestec, Czech Republic.
JCI Insight. 2024 Sep 24;9(18):e173469. doi: 10.1172/jci.insight.173469.
Progress in cytokine engineering is driving therapeutic translation by overcoming these proteins' limitations as drugs. The IL-2 cytokine is a promising immune stimulant for cancer treatment but is limited by its concurrent activation of both pro-inflammatory immune effector cells and antiinflammatory regulatory T cells, toxicity at high doses, and short serum half-life. One approach to improve the selectivity, safety, and longevity of IL-2 is complexing with anti-IL-2 antibodies that bias the cytokine toward immune effector cell activation. Although this strategy shows potential in preclinical models, clinical translation of a cytokine/antibody complex is complicated by challenges in formulating a multiprotein drug and concerns regarding complex stability. Here, we introduced a versatile approach to designing intramolecularly assembled single-agent fusion proteins (immunocytokines, ICs) comprising IL-2 and a biasing anti-IL-2 antibody that directs the cytokine toward immune effector cells. We optimized IC construction and engineered the cytokine/antibody affinity to improve immune bias. We demonstrated that our IC preferentially activates and expands immune effector cells, leading to superior antitumor activity compared with natural IL-2, both alone and combined with immune checkpoint inhibitors. Moreover, therapeutic efficacy was observed without inducing toxicity. This work presents a roadmap for the design and translation of cytokine/antibody fusion proteins.
细胞因子工程的进展通过克服这些蛋白质作为药物的局限性来推动治疗性转化。IL-2 细胞因子是一种很有前途的癌症治疗免疫刺激剂,但由于其同时激活促炎免疫效应细胞和抗炎调节性 T 细胞、高剂量毒性和血清半衰期短而受到限制。提高 IL-2 的选择性、安全性和长效性的一种方法是与偏向细胞因子激活免疫效应细胞的抗 IL-2 抗体复合。尽管这种策略在临床前模型中显示出了潜力,但细胞因子/抗体复合物的临床转化受到多蛋白药物配方的挑战和对复合物稳定性的担忧的复杂化。在这里,我们引入了一种设计包含 IL-2 和偏向性抗 IL-2 抗体的单分子内组装的单药融合蛋白(免疫细胞因子,IC)的多功能方法,该抗体将细胞因子导向免疫效应细胞。我们优化了 IC 的构建并设计了细胞因子/抗体亲和力,以提高免疫偏向性。我们证明,与天然 IL-2 相比,我们的 IC 优先激活和扩增免疫效应细胞,无论是单独使用还是与免疫检查点抑制剂联合使用,都能产生更好的抗肿瘤活性。此外,观察到治疗效果而没有诱导毒性。这项工作为细胞因子/抗体融合蛋白的设计和转化提供了路线图。
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