PET imaging of prostate tumors with 18F-Al-NOTA-MATBBN
PET imaging of prostate tumors with 18F-Al-NOTA-MATBBN
复制标题
使用 18F-Al-NOTA-MATBBN 对前列腺肿瘤进行 PET 成像
DOI：
10.1002/cmmi.1583
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发表时间：
2014-09-01
影响因子：
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通讯作者：
Yang, Min
中科院分区：
文献类型：
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作者：
Pan, Donghui;Yan, Yongjun;Yang, Min
前列腺癌中胃泌素释放肽受体（GRPR）的过表达为检测前列腺癌提供了一个有希望的靶点。MATBBN是一种新的蛙皮素类似物，来源于GRPR拮抗剂，带有一个亲水性连接体。在这项研究中，通过（AlF）-F-18方法标记NOTA缀合的MATBBN，并且还评估了F-18-Al-NOTA-MATBBN用于前列腺肿瘤PET成像的潜力。使用（AlF）-F-18复合物用F-18放射性标记NOTA-MATBBN。还测定了分配系数、体外稳定性和GRPR结合亲和力。在PC-3荷瘤小鼠中用F-18-Al-NOTA-MATBBN进行PET研究。F-18-Al-NOTA-MATBBN可在30 min内制备，衰变校正产率为62.5 ± 2.1%，放化纯度> 98%。（AlF）-F-18标记的BBN类似物的logP辛醇-水值为-2.40 +/-0.07，放射性示踪剂在磷酸盐缓冲盐水和人血清中稳定2小时。F-18-Al-NOTA-MATBBN与MATBBN的位移的IC 50值为126.9 +/-2.75nm。注射标记肽后，PC-3肿瘤清晰可见，具有高对比度。在注射后60分钟，F-18-Al-NOTA-MATBBN和F-18-FDG的肿瘤摄取分别为4.59 +/- 0.43和1.98 +/- 0.35%注射剂量/g，两种示踪剂的肿瘤与肌肉摄取比率分别为6.77 +/- 1.10和1.78 +/- 0.32。动态PET显示F-18-Al-NOTA-MATBBN主要通过肾脏排泄。GRPR结合特异性还通过在注射后1小时与过量未标记的MATBBN肽共注射后F-18-Al-NOTA-MATBBN的肿瘤摄取减少来证明。用F-18一步法可快速标记NOTA-MATBBN. F-18-Al-NOTA-MATBBN有望成为前列腺癌PET显像剂。版权所有（c）2014约翰威利父子有限公司
Overexpression of the gastrin-releasing peptide receptor (GRPR) in prostate cancer provides a promising target for detection the disease. MATBBN is a new bombesin analog originating from the GRPR antagonists with a hydrophilic linker. In this study NOTA-conjugated MATBBN was labeled by the (AlF)-F-18 method and the potential of F-18-Al-NOTA-MATBBN for prostate tumor PET imaging was also evaluated. NOTA-MATBBN was radiolabeled with F-18 using (AlF)-F-18 complexes. Partition coefficient, in vitro stability and GRPR binding affinity were also determined. PET studies were performed with F-18-Al-NOTA-MATBBN in PC-3 tumor-bearing mice. F-18-Al-NOTA-MATBBN can be produced within 30min with a decay-corrected yield of 62.5 +/- 2.1% and a radiochemical purity of >98%. The logP octanol-water value for the (AlF)-F-18-labeled BBN analog was -2.40 +/- 0.07 and the radiotracer was stable in phosphate-buffered saline and human serum for 2h. The IC50 values of displacement for the F-18-Al-NOTA-MATBBN with MATBBN was 126.9 +/- 2.75nm. The PC-3 tumors were clearly visible with high contrast after injection of the labeled peptide. At 60min post-injection, the tumor uptakes for F-18-Al-NOTA-MATBBN and F-18-FDG were 4.59 +/- 0.43 and 1.98 +/- 0.35% injected dose/g, and tumor to muscle uptake radios for two tracers were 6.77 +/- 1.10 and 1.78 +/- 0.32, respectively. Dynamic PET revealed that F-18-Al-NOTA-MATBBN was excreted mainly through the kidneys. GRPR-binding specificity was also demonstrated by reduced tumor uptake of F-18-Al-NOTA-MATBBN after coinjection with excess unlabeled MATBBN peptide at 1h post-injection. NOTA- MATBBN could be labeled rapidly with F-18 using one step method. F-18-Al-NOTA-MATBBN may be a promising PET imaging agent for prostate cancer. Copyright (c) 2014 John Wiley & Sons, Ltd.