Novel Europium Based Time-Resolve Fluorophore with Exceptional Intensity and Stab

描述（由申请人提供）：由于其良好的光物理和光谱特性，镧系离子（特别是铽和铕）配合物比有机荧光染料具有显著的优势。与传统的有机荧光材料相比，镧系配位化合物具有寿命长、斯托克斯位移大、荧光峰轮廓清晰等特点。由于这些吸引人的性质，基于镧系元素荧光的时间分辨试剂已经被创造出来。然而，现有的镧系产品还没有完全成功地生产出具有足够稳定性和亮度的产品，以与传统的有机荧光团竞争。在这项I期SBIR中，Lumiphore将基于新型1,2- hopo敏化单元开发一种铕（Eu）荧光报告细胞。拟议的报告基因（Lumi4-Eu）将具有卓越的光物理和稳定性特性，这将为欧盟报告基因在广泛的药物发现、诊断、快速测序和阵列应用中树立新的基准。这项研究将产生一种具有卓越稳定性、可用性和荧光特性的荧光试剂，通过提供兼容但互补的双工镧系报告器（另一种是Lumiphore的基于铽的荧光报告器- Lumi4-Tb）的第二种颜色，将扩展时间分辨率荧光诊断的能力。结合Lumi4- Eu和Lumi4- tb将实现新一代时间分辨荧光或时间分辨Fvrster共振能量转移（TR-FRET）的多路应用。Lumiphore将利用这项技术开发一个快速、多路复用的免疫分析诊断平台。该平台拥有精致的灵敏度，速度和多功能性，以满足21世纪医疗保健日益增长的需求。

DESCRIPTION (provided by applicant): Due to their favorable photophysical and spectral properties, complexes of lanthanide ions (particularly Terbium and Europium) offer significant advantages over organic fluorescent dyes. Compared with traditional organic fluorescent materials, the lanthanide coordination compounds have the following properties - long life-time, a large Stokes shift, and sharp fluorescent peak profiles. Due to these attractive properties, time-resolved reagents based on lanthanide fluorescence have been created. However, existing lanthanide products have not been fully successful in producing products with sufficient stability and brightness to compete with conventional organic fluorophores. Under this Phase I SBIR, Lumiphore will develop a Europium (Eu) fluorescent reporter based on the novel 1,2-HOPO sensitizing unit. The proposed reporter (Lumi4-Eu) will have exceptional photophysical and stability characteristics that will set a new benchmark for Eu reporters in a wide range of drug discovery, diagnostic, rapid sequencing and array applications. This research will result in a fluorescence reagent with exceptional stability, usability, and fluorescent properties that will expand the capabilities of time resolved fluorescent diagnostics by offering the second color of a duplex set of compatible, but complementary lanthanide reporters (the other being Lumiphore's terbium-based fluorescence reporter - Lumi4-Tb). Combining Lumi4- Eu and Lumi4-Tb will enable a new generation of time resolved fluorescence or time resolved Fvrster resonant energy transfer (TR-FRET) based multiplex applications. Lumiphore will use this technology to develop a rapid, multiplexed immunoassay diagnostic platform. This platform holds the promise of exquisite sensitivities, speed, and versatility for the increasing demands of 21st century healthcare. PUBLIC HEALTH RELEVANCE: The proposed research when combines with Lumiphore's existing terbium-based fluorescence reporter (Lumi4-Tb) will impact public health by enabling highly multiplexed diagnostic assay formats that combine fast turnaround times and high assay throughput efficiency. These assays will be used in high throughput screening (HTS) drug discovery, genomic screening, rapid DNA sequencing, clinical diagnostics and fluorescence microscopy applications for both basic and applied biomedical research.