Analytical Research & Development Mass Spectrometry, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Biologics Process Research & Development, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Anal Chem. 2021 Jun 15;93(23):8161-8169. doi: 10.1021/acs.analchem.1c00042. Epub 2021 May 25.
Polysorbate is widely used to maintain stability of biotherapeutic proteins in pharmaceutical formulation development. Degradation of polysorbate can lead to particle formation in drug products, which is a major quality concern and potential patient risk factor. Enzymatic activity from residual host cell enzymes such as lipases and esterases plays a major role for polysorbate degradation. Their high activity, often at very low concentration, constitutes a major analytical challenge in the biopharmaceutical industry. In this study, we evaluated and optimized the activity-based protein profiling (ABPP) approach to identify active enzymes responsible for polysorbate degradation. Using an optimized chemical probe, we established the first global profile of active serine hydrolases in harvested cell culture fluid (HCCF) for monoclonal antibodies (mAbs) production from two Chinese hamster ovary (CHO) cell lines. A total of eight known lipases were identified by ABPP with enzyme activity information, while only five lipases were identified by a traditional abundance-based proteomics (TABP) approach. Interestingly, phospholipase B-like 2 (PLBL2), a well-known problematic HCP was not found to be active in process-intermediates from two different mAbs. In a proof-of-concept study with downstream samples, phospholipase A2 group VII (PLA2G7) was only identified by ABPP and confirmed to contribute to polysorbate-80 degradation for the first time. The established ABBP approach is approved to be able to identify low-abundance host cell enzymes and fills the gap between lipase abundance and activity, which enables more meaningful polysorbate degradation investigations for biotherapeutic development.
聚山梨酯广泛用于药物制剂开发过程中维持生物治疗蛋白的稳定性。聚山梨酯的降解会导致药物产品中形成颗粒,这是一个主要的质量关注点和潜在的患者风险因素。残留宿主细胞酶(如脂肪酶和酯酶)的酶活性对聚山梨酯的降解起着重要作用。它们的高活性,通常在非常低的浓度下,构成了生物制药行业的主要分析挑战。在这项研究中,我们评估和优化了基于活性的蛋白质谱(ABPP)方法,以鉴定导致聚山梨酯降解的活性酶。使用优化的化学探针,我们建立了第一个用于生产单克隆抗体(mAb)的收获细胞培养液(HCCF)中活性丝氨酸水解酶的全球图谱,该 mAb 来自两种中国仓鼠卵巢(CHO)细胞系。通过 ABPP 鉴定了总共 8 种已知的脂肪酶,并提供了酶活性信息,而传统的基于丰度的蛋白质组学(TABP)方法仅鉴定了 5 种脂肪酶。有趣的是,磷脂酶 B 样 2(PLBL2)是一种众所周知的有问题的 HCP,在两种不同 mAb 的过程中间体中未被发现具有活性。在下游样品的概念验证研究中,仅通过 ABPP 鉴定了磷脂酶 A2 组 VII(PLA2G7),并首次证实其有助于聚山梨酯 80 的降解。所建立的 ABPP 方法被批准能够鉴定低丰度的宿主细胞酶,并填补了脂肪酶丰度与活性之间的空白,这使得能够更有意义地进行生物治疗开发的聚山梨酯降解研究。