Department of Computational Biology and Medical Sciences, Graduate School of Frontier Sciences, The University of Tokyo, Kashiwa, Chiba, Japan; Biomedical Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Tsukuba, Ibaraki, Japan.
Bioproduction Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Tsukuba, Ibaraki, Japan.
J Biol Chem. 2024 Jul;300(7):107464. doi: 10.1016/j.jbc.2024.107464. Epub 2024 Jun 13.
Interferon (IFN) γ can initiate immune responses by inducing the expression of major histocompatibility complex molecules, suggesting its potential for cancer immunotherapy. However, it also has an immunosuppressive function that limits its application as a therapeutic agent. IFNγ has a characteristic domain-swapped dimer structure with two of the six α-helices exchanged with each other. As we hypothesized that the contrasting functions of IFNγ could be attributed to its unique domain-swapped structure, we designed monomeric IFNγ by transforming the domain-swapped dimer structure of WT IFNγ. We conjectured the evolution of this domain-swapped dimer and hypothesized that the current IFNγ structure emerged through shortening of the loop structure at the base of the swapped domain and the accumulation of hydrophobic amino acids at the newly generated interface during domain-swapping. We then designed and generated a stable monomeric IFNγ by retracing this evolutionary process, complementing the lost loop structure with a linker, and replacing the accumulated hydrophobic amino acids with hydrophilic ones. We determined that the designed variant was a monomer based on molecular size and number of epitopes and exhibited activity in cell-based assays. Notably, the monomeric IFNγ showed a qualitatively similar balance between immunostimulatory and immunosuppressive gene expression as WT IFNγ. This study demonstrates that the structural format of IFNγ affects the strength of its activity rather than regulating the fate of downstream gene expression.
干扰素 (IFN) γ 通过诱导主要组织相容性复合体分子的表达来启动免疫反应,这表明其在癌症免疫治疗中有潜力。然而,它也具有免疫抑制功能,限制了其作为治疗剂的应用。IFNγ 具有特征性的结构域交换二聚体结构,其中六个 α-螺旋中的两个相互交换。由于我们假设 IFNγ 的相反功能可以归因于其独特的结构域交换结构,我们通过改变 WT IFNγ 的结构域交换二聚体结构来设计单体 IFNγ。我们推测了这种结构域交换的进化,并假设当前的 IFNγ 结构是通过缩短交换结构域底部的环结构以及在结构域交换过程中在新生成的界面处积累疏水性氨基酸而产生的。然后,我们通过追溯这个进化过程设计并生成了一种稳定的单体 IFNγ,用接头补充丢失的环结构,并将积累的疏水性氨基酸替换为亲水性氨基酸。我们确定设计的变体基于分子大小和表位数量是单体,并在基于细胞的测定中显示出活性。值得注意的是,单体 IFNγ 显示出与 WT IFNγ 相似的免疫刺激和免疫抑制基因表达之间的平衡。这项研究表明,IFNγ 的结构格式影响其活性的强度,而不是调节下游基因表达的命运。