Challa Dilip, de Rutte Joseph, Konu Cassady, Udani Shreya, Liang Jesse, Krohl Patrick J, Rondon Ronald, Bondensgaard Kent, Di Carlo Dino, Watkins-Yoon Jennifer
Alloy Therapeutics.
Partillion Bioscience Corporation.
bioRxiv. 2024 Aug 19:2024.08.15.608174. doi: 10.1101/2024.08.15.608174.
Antibody discovery technologies, essential for research and therapeutic applications, have evolved significantly since the development of hybridoma technology. Various in vitro (display) and in vivo (animal immunization and B cell-sequencing) workflows have led to the discovery of antibodies against diverse antigens. Despite this success, standard display and B-cell sequencing-based technologies are limited to targets that can be produced in a soluble form. This limitation inhibits the screening of function-inducing antibodies, which require the target to be expressed in cells to monitor function or signaling, and antibodies targeting proteins that maintain their physiological structure only when expressed on cell membranes, such as G-protein coupled receptors (GPCRs). A high-throughput two-cell screening workflow, which localizes an antibody-secreting cell (ASC) and a cell expressing the target protein in a microenvironment, can overcome these challenges. To make function-first plasma cell-based antibody discovery accessible and scalable, we developed hydrogel Nanovials that can capture single plasma cells, target-expressing cells, and plasma cell secretions (antibodies). The detection and isolation of Nanovials harboring the antigen-specific plasma cells are then carried out using a flow cytometry cell sorter - an instrument that is available in most academic centers and biopharmaceutical companies. The antibody discovery workflow employing Nanovials was first validated in the context of two different cell membrane-associated antigens produced in recombinant form. We analyzed over 40,000 plasma cells over two campaigns and were able to identify a diversity of binders that i) exhibited high affinity (picomolar) binding, ii) targeted multiple non-overlapping epitopes and iii) demonstrated high developability scores. A campaign using the two-cell assay targeting the immune checkpoint membrane protein PD-1 yielded cell binders with similar EC50s to clinically used Pembrolizumab and Nivolumab. The highest selectivity for binders was observed for sorted events corresponding with the highest signal bound to target cells on Nanovials. Overall, Nanovials can provide a strong foundation for function-first antibody discovery, yielding direct cell binding information and quantitative data on prioritization of hits with flexibility for additional functional readouts in the future.
抗体发现技术对于研究和治疗应用至关重要,自杂交瘤技术发展以来已取得显著进展。各种体外(展示)和体内(动物免疫和B细胞测序)工作流程已促成针对多种抗原的抗体发现。尽管取得了这一成功,但基于标准展示和B细胞测序的技术仅限于可溶形式产生的靶标。这一限制阻碍了对功能诱导抗体的筛选,这类抗体需要靶标在细胞中表达以监测功能或信号传导,也阻碍了对仅在细胞膜上表达时才维持其生理结构的蛋白质(如G蛋白偶联受体(GPCR))的靶向抗体的筛选。一种高通量双细胞筛选工作流程,可在微环境中定位抗体分泌细胞(ASC)和表达靶蛋白的细胞,能够克服这些挑战。为了使基于功能优先的浆细胞抗体发现变得可行且可扩展,我们开发了水凝胶纳米管,它能够捕获单个浆细胞、表达靶标的细胞以及浆细胞分泌物(抗体)。然后使用流式细胞分选仪对含有抗原特异性浆细胞的纳米管进行检测和分离,流式细胞分选仪在大多数学术中心和生物制药公司都有配备。采用纳米管的抗体发现工作流程首先在以重组形式产生的两种不同细胞膜相关抗原的背景下得到验证。我们在两次实验中分析了超过40,000个浆细胞,能够鉴定出多种结合物,这些结合物具有以下特点:i)表现出高亲和力(皮摩尔)结合;ii)靶向多个不重叠的表位;iii)显示出高开发潜力评分。一项针对免疫检查点膜蛋白PD - 1的双细胞检测实验,产生了与临床使用的帕博利珠单抗和纳武利尤单抗具有相似半数有效浓度(EC50)的细胞结合物。对于纳米管上与靶细胞结合信号最强的分选事件,观察到结合物具有最高的选择性。总体而言,纳米管可为功能优先的抗体发现提供坚实基础,产生直接的细胞结合信息以及关于命中优先级的定量数据,并为未来的其他功能读数提供灵活性。