Altor BioScience Corporation, 2810 North Commerce Parkway, Miramar, FL 33025, USA.
Cytokine. 2011 Dec;56(3):804-10. doi: 10.1016/j.cyto.2011.09.028. Epub 2011 Oct 22.
IL-15, a promising cytokine for treating cancer and viral diseases, is presented in trans by the IL-15 receptor (IL-15R) alpha-chain to the IL-15Rβγc complex displayed on the surface of T cells and natural killer (NK) cells. We previously reported that an asparagine to aspartic acid substitution at amino acid 72 (N72D) of IL-15 provides a 4-5-fold increase in biological activity compared to the native molecule. In this report, we describe Chinese hamster ovary (CHO) cell expression of a soluble complex (IL-15 N72D:IL-15RαSu/Fc) consisting of the IL-15 N72D superagonist and a dimeric IL-15Rα sushi domain-IgG1 Fc fusion protein. A simple but readily scalable affinity and ion exchange chromatography method was developed to highly purify the complex having both IL-15 binding sites fully occupied. The immunostimulatory effects of this complex were confirmed using cell proliferation assays. Treatment of mice with a single intravenous dose of IL-15N72D:IL-15RαSu/Fc resulted in a significant increase in CD8+ T cells and NK cells that was not observed following IL-15 treatment. Pharmacokinetic analysis indicated that the complex has a 25-h half-life in mice which is considerably longer than <40-min half-life of IL-15. Thus, the enhanced activity of the IL-15N72D:IL-15RαSu/Fc complex is likely the result of the increased binding activity of IL-15N72D to IL-15Rβγc, optimized cytokine trans-presentation by the IL-15RαSu domain, the dimeric nature of the cytokine domain and its increased in vivo half-life compared to IL-15. These findings indicate that this IL-15 superagonist complex could serve as a superior immunostimulatory therapeutic agent.
白细胞介素-15(IL-15)是一种有前景的细胞因子,可用于治疗癌症和病毒疾病,它通过白细胞介素-15 受体(IL-15R)α 链转呈给 T 细胞和自然杀伤(NK)细胞表面表达的 IL-15Rβγc 复合物。我们之前报道过,与天然分子相比,IL-15 第 72 位天冬酰胺(N72)突变为天冬氨酸(D)可使生物活性提高 4-5 倍。在本报告中,我们描述了中国仓鼠卵巢(CHO)细胞表达一种可溶性复合物(IL-15 N72D:IL-15RαSu/Fc),该复合物由 IL-15 N72D 超激动剂和二聚体 IL-15Rα sushi 结构域-IgG1 Fc 融合蛋白组成。开发了一种简单但易于扩展的亲和和离子交换色谱方法,可高度纯化完全占据两个 IL-15 结合位点的复合物。使用细胞增殖测定法证实了该复合物的免疫刺激作用。单次静脉注射 IL-15N72D:IL-15RαSu/Fc 可使 CD8+T 细胞和 NK 细胞显著增加,而 IL-15 治疗则没有观察到这种现象。药代动力学分析表明,该复合物在小鼠体内的半衰期为 25 小时,明显长于 IL-15 的半衰期 <40 分钟。因此,IL-15N72D:IL-15RαSu/Fc 复合物的活性增强可能是由于 IL-15N72D 与 IL-15Rβγc 的结合活性增加、IL-15RαSu 结构域优化的细胞因子转呈、细胞因子结构域的二聚化及其与 IL-15 相比在体内半衰期的延长所致。这些发现表明,这种 IL-15 超激动剂复合物可作为一种优越的免疫刺激治疗剂。