Sedlák Erik, Schaefer Jonas V, Marek Jozef, Gimeson Peter, Plückthun Andreas
Department of Biochemistry, University of Zurich, Winterthurerstrasse 190, CH-8057, Zurich, Switzerland.
Centre for Interdisciplinary Biosciences, P.J. Šafárik University, Moyzesova 11, Košice, 040 01, Slovakia.
Protein Sci. 2015 Jul;24(7):1100-13. doi: 10.1002/pro.2691. Epub 2015 Jun 11.
The stability of Immunoglobulin G (IgG) affects production, storage and usability, especially in the clinic. The complex thermal and isothermal transitions of IgGs, especially their irreversibilities, pose a challenge to the proper determination of parameters describing their thermodynamic and kinetic stability. Here, we present a reliable mathematical model to study the irreversible thermal denaturations of antibody variants. The model was applied to two unrelated IgGs and their variants with stabilizing mutations as well as corresponding non-glycosylated forms of IgGs and Fab fragments. Thermal denaturations of IgGs were analyzed with three transitions, one reversible transition corresponding to C(H)2 domain unfolding followed by two consecutive irreversible transitions corresponding to Fab and C(H)3 domains, respectively. The parameters obtained allowed us to examine the effects of these mutations on the stabilities of individual domains within the full-length IgG. We found that the kinetic stability of the individual Fab fragment is significantly lowered within the IgG context, possibly because of intramolecular aggregation upon heating, while the stabilizing mutations have an especially beneficial effect. Thermal denaturations of non-glycosylated variants of IgG consist of more than three transitions and could not be analyzed by our model. However, isothermal denaturations demonstrated that the lack of glycosylation affects the stability of all and not just of the C(H)2 domain, suggesting that the partially unfolded domains may interact with each other during unfolding. Investigating thermal denaturation of IgGs according to our model provides a valuable tool for detecting subtle changes in thermodynamic and/or kinetic stabilities of individual domains.
免疫球蛋白G(IgG)的稳定性会影响其生产、储存及可用性,在临床应用中尤为如此。IgG复杂的热转变和等温转变,尤其是其不可逆性,给准确测定描述其热力学和动力学稳定性的参数带来了挑战。在此,我们提出了一个可靠的数学模型来研究抗体变体的不可逆热变性。该模型应用于两种不相关的IgG及其具有稳定突变的变体,以及相应的非糖基化形式的IgG和Fab片段。IgG的热变性通过三个转变进行分析,一个可逆转变对应于C(H)2结构域的展开,随后是两个连续的不可逆转变,分别对应于Fab和C(H)3结构域。所获得的参数使我们能够研究这些突变对全长IgG内各个结构域稳定性的影响。我们发现,在IgG环境中,单个Fab片段的动力学稳定性显著降低,这可能是由于加热时的分子内聚集,而稳定突变具有特别有益的效果。IgG非糖基化变体的热变性由三个以上的转变组成,无法用我们的模型进行分析。然而,等温变性表明,糖基化的缺失会影响所有结构域的稳定性,而不仅仅是C(H)2结构域,这表明部分展开的结构域在展开过程中可能会相互作用。根据我们的模型研究IgG的热变性,为检测各个结构域热力学和/或动力学稳定性的细微变化提供了一个有价值的工具。