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Preparation Of Near-Infrared-Labeled Targeted Contrast AgentsFor Clinical Translation

机译:临床翻译的近红外标记的靶向造影剂的制备

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Targeted fluorophore-labeled contrast agents are moving toward translation to human surgical use. To prepare for future clinical use, we examined the performance of potential ligands targeting the epidermal growth factor receptor,a5b3 integrins, and GLUT transporters for their suitability as directed contrast agents. Each agent was labeled with IRDye 800CW, and near-infrared dye with excitation/emission wavelengths of 789/805 nm, which we determined had favorable toxicity characteristics. The probe molecules examined consisted of Affibodies, nanobodies, peptides, and the sugar 2-deoxy-D-glucose. Each probe was tested for specific and non-specific binding in cell based assays. All probe types showed good performance in mouse models for detecting either spontaneous tumors or tumor xenografts in vivo. Each of the probes tested show promise for future human clinical studies.
机译:靶向荧光团标记的造影剂正在向人类手术使用转向翻译。为了为未来的临床使用做准备,我们检查了靶向表皮生长因子受体,A5B3整合蛋白和露出剂的潜在配体的性能,以便根据指导造影剂的适用性。每种试剂用IRDYE 800CW标记,近红外染料,激发/发射波长为789/805nm,我们确定具有良好的毒性特征。检查的探针分子由辅助物,纳米型,肽和糖2-脱氧-D-葡萄糖组成。在基于细胞的测定中测试每个探针的特异性和非特异性结合。所有探测类型都显示出良好的小鼠模型表现,用于检测体内自发性肿瘤或肿瘤异种移植物。每个探针都测试了未来人类临床研究的承诺。

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