Dual‐labeled prostate‐specific membrane antigen (PSMA)‐targeting agent for preoperative molecular imaging and fluorescence‐guided surgery for prostate cancer,Journal of Labelled Compounds and Radiopharmaceuticals

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Dual‐labeled prostate‐specific membrane antigen (PSMA)‐targeting agent for preoperative molecular imaging and fluorescence‐guided surgery for prostate cancer
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-10-15 , DOI: 10.1002/jlcr.3884
Myoung Hyoun Kim ₁ , Seul-Gi Kim ₂ , Dae-Weung Kim _{1,

2}

Affiliation

The objective of this study was to report the synthesis and characteristics of a dual modality imaging agent, Tc-99m GRFLTGGTGRLLRIS-GHEG-ECG-K(-5-carboxy-X-rhodamine)-NH2 (GRFLT-ECG-ROX), and to verify its feasibility as both molecular imaging and intra-operative guidance agent. GRFLT-ECG-ROX was synthesized using Fmoc solid-phase peptide synthesis. Radiolabeling of GRFLT-ECG-ROX with Tc-99m was accomplished using ligand exchange via tartrate. Binding affinity and in vitro cellular uptake studies were performed. Gamma camera imaging, biodistribution and ex vivo imaging studies were performed using LNCaP and PC-3 tumor-bearing murine models. Surgical removal of tumor nodules in murine models with peritoneal carcinomatosis was performed under a fluorescence imaging system. After radiolabeling procedures with Tc-99m, Tc-99m GRFLT-ECG-ROX complexes were prepared in high yield (> 96%). The binding affinity value (Kd ) of Tc-99m GRFLT-ECG-ROX for LNCaP cells was estimated to be 9.5 ± 1.3 nM. In gamma camera imaging, the tumor to normal muscle uptake ratios of Tc-99m GRFLT-ECG-ROX increased with time (3.1 ± 0.2, 4.0 ± 0.4, and 6.3 ± 0.9 at 1, 2, and 3 h, respectively). Under real-time optical imaging, the removal of visible nodules was successfully performed. Thus, Tc-99m GRFLT-ECG-ROX could provide both pre-operative molecular imaging and fluorescence imaging guidance for tumor removal.

中文翻译：

双标记前列腺特异性膜抗原（PSMA）靶向剂，用于前列腺癌术前分子成像和荧光引导手术

本研究的目的是报告双模态成像剂 Tc-99m GRFLTGGTGRLLRIS-GHEG-ECG-K(-5-羧基-X-罗丹明)-NH2 (GRFLT-ECG-ROX) 的合成和特性，以及验证其作为分子成像和术中引导剂的可行性。 GRFLT-ECG-ROX是使用Fmoc固相肽合成法合成的。 GRFLT-ECG-ROX 与 Tc-99m 的放射性标记是通过酒石酸盐进行配体交换来完成的。进行了结合亲和力和体外细胞摄取研究。使用 LNCaP 和 PC-3 荷瘤小鼠模型进行伽马相机成像、生物分布和离体成像研究。在荧光成像系统下对患有腹膜癌病的小鼠模型中的肿瘤结节进行手术切除。用 Tc-99m 进行放射性标记后，以高产率 (> 96%) 制备了 Tc-99m GRFLT-ECG-ROX 复合物。 Tc-99m GRFLT-ECG-ROX 对 LNCaP 细胞的结合亲和力值 (Kd ) 估计为 9.5 ± 1.3 nM。在伽马相机成像中，Tc-99m GRFLT-ECG-ROX 的肿瘤与正常肌肉的摄取比率随时间增加（1、2 和 3 小时分别为 3.1 ± 0.2、4.0 ± 0.4 和 6.3 ± 0.9）。在实时光学成像下，成功去除可见结节。因此，Tc-99m GRFLT-ECG-ROX 可以为肿瘤切除提供术前分子成像和荧光成像指导。

更新日期：2020-10-15

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