Department of Biochemistry, University of Utah School of Medicine, Salt Lake City, UT, USA.
Octant Inc., Emeryville, CA, USA.
Nat Commun. 2024 Nov 28;15(1):10353. doi: 10.1038/s41467-024-54502-9.
Cellular responses to stimuli underpin discoveries in drug development, synthetic biology, and general life sciences. We introduce a library comprising 6144 synthetic promoters, each shorter than 250 bp, designed as transcriptional readouts of cellular stimulus responses in massively parallel reporter assay format. This library facilitates precise detection and amplification of transcriptional activity from our promoters, enabling the systematic development of tunable reporters with dynamic ranges of 50-100 fold. Our library proved functional in numerous cell lines and responsive to a variety of stimuli, including metabolites, mitogens, toxins, and pharmaceutical agents, generating robust and scalable reporters effective in screening assays, biomarkers, and synthetic circuits attuned to endogenous cellular activities. Particularly valuable in therapeutic development, our library excels in capturing candidate reporters to signals mediated by drug targets, a feature we illustrate across nine diverse G-protein coupled receptors (GPCRs), critical targets in drug development. We detail how this tool isolates and defines discrete signaling pathways associated with specific GPCRs, elucidating their transcriptional signatures. With its ease of implementation, broad utility, publicly available data, and comprehensive documentation, our library will be beneficial in synthetic biology, cellular engineering, ligand exploration, and drug development.
细胞对刺激的反应是药物开发、合成生物学和一般生命科学发现的基础。我们引入了一个包含 6144 个合成启动子的文库,每个启动子都短于 250bp,设计为细胞刺激反应的转录读出物,以大规模平行报告基因检测格式。这个文库有助于从我们的启动子中精确检测和放大转录活性,从而能够系统地开发具有 50-100 倍动态范围的可调式报告基因。我们的文库在许多细胞系中证明是有效的,并且对各种刺激物(包括代谢物、有丝分裂原、毒素和药物制剂)有反应,生成了在筛选测定、生物标志物和内源性细胞活动调节的合成回路中有效的强大且可扩展的报告基因。在治疗开发中特别有价值的是,我们的文库擅长捕获由药物靶标介导的候选报告基因,我们通过九个不同的 G 蛋白偶联受体(GPCR)来展示这一功能,GPCR 是药物开发的关键靶点。我们详细介绍了该工具如何分离和定义与特定 GPCR 相关的离散信号通路,阐明它们的转录特征。由于其易于实施、广泛的用途、公开可用的数据和全面的文档,我们的文库将在合成生物学、细胞工程、配体探索和药物开发中受益。