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A label-free screening approach targeted protease-activated receptor 1 based on dynamic mass redistribution in living cells

机译：基于活细胞的动态质量再分布，无标记的筛选方法靶向蛋白酶活化受体1

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摘要

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：蛋白酶活化受体1（PAR-1）拮抗剂强烈抑制凝血酶诱导的血小板聚集，被证明是有效的抗血栓形成药物。用于PAR-1拮抗剂的传统筛选测定需要分子标记或细胞工程技术。这里，通过监测全细胞中的综合活细胞应答，开发了一种用于筛选靶向PAR-1的活性化合物的可标记方法。为了表征细胞响应，使用PAR-1已知的激动剂和拮抗剂用谐振波导光栅（RWG）生物传感器检测细胞动态质量再分配（DMR）。选择人表皮癌A431细胞系来建立一种细胞表型分析模型，用于筛选来自80天然产物的PAR-1拮抗剂。结果表明，将五种化合物作为候选生物活性化合物筛选出来。鉴定了两种化合物，阳鼠苷和血红素，以体外具有抗血小板聚集活性。这些结果表明，无标记的DMR筛选方法是有效的，可用于筛选靶向PAR-1的生物活性化合物。

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  • 来源
    《RSC Advances》 |2017年第68期|共9页
  • 作者

    Tang Weiwei; Huang Bixia; Wang Jiancheng; An Lin; Zhong Huailing; Yang Hua; Li Ping; Chen Jun;

  • 作者单位

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

    U Pharm Labs LLC 239 New Rd Suite A-107 Parsippany NJ 07054 USA;

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

    China Pharmaceut Univ State Key Lab Nat Med Nanjing 210009 Jiangsu Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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