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首页> 外文期刊>RSC Advances >A label-free screening approach targeted protease-activated receptor 1 based on dynamic mass redistribution in living cells
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A label-free screening approach targeted protease-activated receptor 1 based on dynamic mass redistribution in living cells

机译：基于活细胞中动态质量重新分布的无标记筛选方法靶向蛋白酶激活受体1

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Protease-activated receptor 1 (PAR-1) antagonists strongly inhibit thrombin-induced platelet aggregation and are proved to be effective as anti-thrombotic drugs. Traditional screening assays for PAR-1 antagonists require molecular labeling or cell engineering technique. Here, a label-free approach was developed for the screening of active compounds targeting PAR-1 through monitoring integrated live-cell responses in whole cells. To characterize the cellular response, the cellular dynamic mass redistribution (DMR) was detected with a resonant waveguide grating (RWG) biosensor using PAR-1 known agonists and antagonists. The human epidermoid carcinoma A431 cell line was selected to establish a cell phenotypic profiling model for screening the PAR-1 antagonists from 80 natural products. Results showed that five compounds were screened out as candidate bioactive compounds. Two compounds, parthenolide and sanguinarine, were identified to possess anti-platelet aggregation activities in vitro. These results indicate that the label-free DMR screening approach is effective and useful for screening bioactive compounds targeting PAR-1.
机译：蛋白酶激活受体1（PAR-1）拮抗剂强烈抑制凝血酶诱导的血小板凝集，并被证明是有效的抗血栓药物。 PAR-1拮抗剂的传统筛选方法需要分子标记或细胞工程技术。在这里，开发了一种无标记方法，用于通过监测全细胞中整合的活细胞反应来筛选靶向PAR-1的活性化合物。为了表征细胞反应，使用PAR-1已知激动剂和拮抗剂，通过共振波导光栅（RWG）生物传感器检测了细胞动态质量再分布（DMR）。选择人表皮样癌A431细胞系以建立细胞表型分析模型，以从80种天然产物中筛选PAR-1拮抗剂。结果表明，筛选出了五种化合物作为候选生物活性化合物。鉴定出在中具有抗血小板聚集活性的两种化合物，即小白菊内酯和sanguinarine。这些结果表明，无标记的DMR筛选方法对于筛选靶向PAR-1的生物活性化合物是有效和有用的。

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