Technology to visualize small prostate cancers is urgently needed because of the difficulty of discriminating prostate cancer from normal tissue with the naked eye, and a fluorescence imaging method would be advantageous. Here, we describe the design and synthesis of a fluorogenic probe (Ac–KQLR–HMRG) that is activated by hepsin and matriptase (proteases over-expressed in prostate cancer). Ac–KQLR–HMRG exhibited significant turn-on fluorogenicity in the presence of hepsin (180-fold) and matriptase (80-fold) and allowed specific fluorescence imaging of various prostate cancer cell line in vitro. In addition, the probe enabled rapid imaging (within 1–10 min) of small prostate cancer nodules in mouse models of disseminated peritoneal tumor and orthotopic tumor.

中文翻译：

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用于前列腺癌成像的可激活荧光探针的开发

由于用肉眼难以将前列腺癌与正常组织区分开，因此迫切需要可视化小的前列腺癌的技术，并且荧光成像方法将是有利的。在这里，我们描述了由庚素和matriptase（在前列腺癌中过度表达的蛋白酶）激活的荧光探针（Ac-KQLR-HMRG）的设计和合成。Ac-KQLR-HMRG在hepsin（180倍）和matriptase（80倍）的存在下表现出显着的开启荧光性，并可以在体外对各种前列腺癌细胞系进行特异性荧光成像。此外，该探针可在弥漫性腹膜肿瘤和原位肿瘤的小鼠模型中对小型前列腺癌结节进行快速成像（1-10分钟内）。