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A long-lived peptide-conjugated iridium(iii) complex as a luminescent probe and inhibitor of the cell migration mediator, formyl peptide receptor 2†
Chemical Science ( IF 8.4 ) Pub Date : 2018-10-01 00:00:00 , DOI: 10.1039/c8sc02733a
Kasipandi Vellaisamy 1, 2, 3, 4 , Guodong Li 4, 5, 6, 7 , Wanhe Wang 1, 2, 3, 4 , Chung-Hang Leung 4, 5, 6, 7 , Dik-Lung Ma 1, 2, 3, 4
Affiliation  

Formyl peptide receptors play important biological and therapeutic roles in wound repair and inflammatory diseases. In this work, we present a luminescent iridium(III) complex (6) conjugated with the peptide agonist WKYMVm as a luminescent formyl peptide receptor 2 (FPR2) imaging probe in living cells. Complex 6 displayed ideal cell imaging characteristics, high photostability and low cytotoxicity. Competition assays with a known FPR2 antagonist, WRW4, and siRNA knockdown experiments both revealed that complex 6 selectively targeted FPR2 in living HUVEC cells. Moreover, complex 6 regulated FPR2 signalling in HUVEC cells as shown using a mechanical scratch assay. Finally, complex 6 reduced epithelial cell migration capacity and inhibited lipoxin A4 (LXA4)-triggered cell migration in HUVEC cells, demonstrating the ability of this complex to inhibit FPR2 in living cells. To our knowledge, this is the first long-lived probe for imaging FPR2 in living cells.

中文翻译:

一种长寿命的肽缀合铱(iii)复合物,可作为发光探针和细胞迁移介质甲酰肽受体的抑制剂2

甲酰基肽受体在伤口修复和炎性疾病中起重要的生物学和治疗作用。在这项工作中,我们提出了与多肽激动剂WKYMVm共轭的发光铱(III)复合物(6),作为活细胞中的发光甲酰基肽受体2(FPR2)成像探针。复合物6显示出理想的细胞成像特性,高光稳定性和低细胞毒性。用已知的FPR2拮抗剂,WRW4和siRNA敲低实验进行竞争分析均显示,复合物6在活HUVEC细胞中选择性靶向FPR2。此外,如使用机械刮擦试验所示,复合物6调节HUVEC细胞中的FPR2信号传导。最后,复数6在HUVEC细胞中降低了上皮细胞迁移能力并抑制了脂蛋白A4(LXA4)触发的细胞迁移,证明了该复合物抑制活细胞中FPR2的能力。据我们所知,这是第一个在活细胞中成像FPR2的长寿命探针。
更新日期:2018-10-01
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