Protein arginine methyltransferases (PRMTs) are crucial epigenetic regulators in eukaryotic organisms that serve as histone writers for chromatin remodeling. PRMTs also methylate a variety of non-histone protein substrates to modulate their function and activity. The development of potent PRMT inhibitors has become an emerging and imperative research area in the drug discovery field to provide novel therapeutic agents for treating diseases and as tools to investigate the biological functions of PRMTs. PRMT1 is the major type I enzyme that catalyzes the formation of asymmetric dimethyl arginine, and PRMT1 plays important regulatory roles in signal transduction, transcriptional activation, RNA splicing, and DNA repair. Aberrant expression of PRMT1 is found in many types of cancers, pulmonary diseases, cardiovascular disease, diabetes, and renal diseases. PRMT1 is a highly promising target for therapeutic development. We created a stopped flow fluorescence-based assay for PRMT1 inhibitor detection and characterization that has the advantages of being homogeneous, nonradioactive, and mix-and-measure in nature, allowing for continuous measurement of the methylation reaction and its inhibition. To our knowledge, this is the first continuous assay for PRMT1 reaction detection and inhibitor characterization. The approach is not only capable of quantitatively determining the potency (IC₅₀) of PRMT1 inhibitors but can also distinguish cofactor-competitive inhibitors, substrate-competitive inhibitors, and mixed-type inhibitors.

精氨酸甲基转移酶（PRMT）是真核生物中至关重要的表观遗传调节剂，可作为染色质重塑的组蛋白作者。PRMT还可以甲基化多种非组蛋白的蛋白质底物，从而调节其功能和活性。有效的PRMT抑制剂的开发已经成为药物发现领域中新兴的和紧迫的研究领域，以提供用于治疗疾病的新型治疗剂并作为研究PRMT​​的生物学功能的工具。PRMT1是主要的I型酶，可催化不对称二甲基精氨酸的形成，PRMT1在信号转导，转录激活，RNA剪接和DNA修复中起着重要的调节作用。在许多类型的癌症，肺部疾病，心血管疾病，糖尿病，和肾脏疾病。PRMT1是治疗开发的高度有希望的目标。我们创建了用于PRMT1抑制剂检测和表征的基于荧光停止流的测定法，该测定法具有均质，无放射性和本质上混合测量的优势，可以连续测量甲基化反应及其抑制作用。据我们所知，这是用于PRMT1反应检测和抑制剂表征的第一个连续测定法。该方法不仅能够定量确定效力（IC 可以连续测量甲基化反应及其抑制作用。据我们所知，这是用于PRMT1反应检测和抑制剂表征的第一个连续测定法。该方法不仅能够定量确定效力（IC 可以连续测量甲基化反应及其抑制作用。据我们所知，这是用于PRMT1反应检测和抑制剂表征的第一个连续测定法。该方法不仅能够定量确定效力（IC₅₀）PRMT1抑制剂，但也可以区分辅因子竞争性抑制剂，底物竞争性抑制剂和混合型抑制剂。