Lakbub Jude C, Clark Daniel F, Shah Ishan S, Zhu Zhikai, Go Eden P, Tolbert Thomas J, Desaire Heather
Department of Chemistry, University of Kansas, Lawrence, KS, 66047.
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence, KS, 66047.
Anal Methods. 2016 Aug 21;8(31):6046-6055. doi: 10.1039/C6AY01248E. Epub 2016 Jul 27.
The use of monoclonal antibodies (mAbs) for the manufacture of innovator and biosimilar biotherapeutics has increased tremendously in recent years. From a structural perspective, mAbs have high disulfide bond content, and the correct disulfide connectivity is required for proper folding and to maintain their biological activity. Therefore, disulfide linkage mapping is an important component of mAB characterization for ensuring drug safety and efficacy. The native disulfide linkage patterns of all four subclasses of IgG antibodies have been well established since the late 1960s. Among these IgG subtypes, disulfide mediated isoforms have been identified for IgG2 and IgG4, and to a lesser extent in IgG1, which is the most studied IgG subclass. However, no studies have been carried out so far to investigate whether different IgG3 isoforms exist due to alternative disulfide connectivity. In an effort to investigate the presence of disulfide-mediated isoforms in IgG3, we employed a bottom-up mass spectrometry approach to accurately determine the disulfide bond linkages in endogenous human IgG3 monoclonal antibody and our results show that no such alternative disulfide bonds exist. While many antibody-based drugs are developed around IgG1, IgG3 represents a new, and in some cases, more desirable drug candidate. Our data represent the first demonstration that alternative disulfide bond arrangements are not present in endogenous IgG3; and therefore, they should not be present in recombinant forms used as antibody-based therapeutics.
近年来,单克隆抗体(mAb)在创新型和生物类似物生物治疗药物制造中的应用大幅增加。从结构角度来看,单克隆抗体具有较高的二硫键含量,正确的二硫键连接对于其正确折叠和维持生物活性至关重要。因此,二硫键连接图谱分析是确保单克隆抗体药物安全性和有效性的重要表征组成部分。自20世纪60年代末以来,IgG抗体所有四个亚类的天然二硫键连接模式已得到充分确立。在这些IgG亚型中,已鉴定出IgG2和IgG4存在二硫键介导的异构体,在研究最多的IgG1亚型中也有较少程度的发现。然而,迄今为止尚未开展研究来调查IgG3是否由于二硫键连接方式不同而存在不同的异构体。为了研究IgG3中二硫键介导的异构体的存在情况,我们采用了自下而上的质谱方法来准确确定内源性人IgG3单克隆抗体中的二硫键连接,结果表明不存在此类替代二硫键。虽然许多基于抗体的药物是围绕IgG1开发的,但IgG3代表了一种新的、在某些情况下更具吸引力的候选药物。我们的数据首次证明内源性IgG3中不存在替代二硫键排列;因此,它们也不应存在于用作基于抗体的治疗药物的重组形式中。