Pyropheophorbide-a (Pyro) is a promising multifunctional molecule for multimodal tumor imaging and tumor photodynamic therapy (PDT), but its clinical applications are seriously restricted by the limited tumor accumulation capability. Here, we designed and synthesized a small-molecule probe that achieved specific dual-modal tumor imaging based on Pyro. Briefly, a novel molecule combining Pyro, an RGD dimer peptide (3PRGD2 ) and 64 Cu was designed and synthesized, and the obtained molecule, 64 Cu-Pyro-3PRGD2 exhibited high tumor specificity in both positron emission tomography (PET) and optical imaging in vivo. c (RGDfk) peptide blocking significantly reduced the efficacy of the probe, which confirmed the integrin αV β3 targeting of this molecular probe. 64 Cu-Pyro-3PRGD2 had very low accumulation in normal organs and could be rapidly cleared through kidney metabolism, which prevented the potential damage to adjacent normal tissues. Overall, combining tumor targeting, dual-modal imaging and biosafety, 64 Cu-Pyro-3PRGD2 has the potential for clinical use as a molecular imaging probe for tumor diagnosis.

中文翻译：

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具有整合素 αv β3 靶向功能的 64 Cu-卟啉双模分子探针，用于肿瘤成像

Pyropheophorbide-a (Pyro) 是一种用于多模式肿瘤成像和肿瘤光动力治疗 (PDT) 的有前途的多功能分子，但其临床应用受到肿瘤积累能力有限的严重限制。在这里，我们设计并合成了一种基于 Pyro 实现特异性双模态肿瘤成像的小分子探针。简而言之，设计并合成了一种结合 Pyro、RGD 二聚体肽 (3PRGD2) 和 64 Cu 的新型分子，获得的分子 64 Cu-Pyro-3PRGD2 在正电子发射断层扫描 (PET) 和光学成像中均表现出高度的肿瘤特异性。活体。c (RGDfk) 肽阻断显着降低了探针的功效，这证实了该分子探针的整联蛋白 αV β3 靶向。64 Cu-Pyro-3PRGD2 在正常器官中的积累非常少，可以通过肾脏代谢迅速清除，从而防止对邻近正常组织的潜在损害。总体而言，结合肿瘤靶向、双模态成像和生物安全性，64 Cu-Pyro-3PRGD2 具有作为肿瘤诊断分子成像探针临床应用的潜力。