The imaging study of a small-molecular inhibitor targeting prostate specific membrane antigen

XU Xiaoping; ZHANG Jianping; HE Simin; LUO Jianmin; BAO Xiao; WANG Xiaofang; GUO Xiaomao; ZHANG Yingjian

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The imaging study of a small-molecular inhibitor targeting prostate specific membrane antigen

更新时间：2025-12-31

- The imaging study of a small-molecular inhibitor targeting prostate specific membrane antigen
- Vol. 24, Issue 3, Pages: 173-178(2015)
- 作者机构：
  
  1. 复旦大学生物医学影像研究中心,上海,200032
  2. 上海分子影像探针工程技术中心筹,上海,200032
  3. 复旦大学附属肿瘤医院核医学科，复旦大学上海医学院肿瘤学系,上海,200032
  4. 复旦大学附属肿瘤医院放疗科，复旦大学上海医学院肿瘤学系,上海,200032
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Published Online：20 October 2015，
  
  Published：20 October 2015
- 稿件说明：
移动端阅览
许晓平,张建平,何思敏,等. 前列腺特异性膜抗原小分子抑制剂显像研究[J]. 肿瘤影像学, 2015, 24(3): 173-178
DOI：

许晓平,张建平,何思敏,等. 前列腺特异性膜抗原小分子抑制剂显像研究[J]. 肿瘤影像学, 2015, 24(3): 173-178 DOI：

摘要

目的：

前列腺特异性膜抗原(PSMA)是前列腺癌诊疗的一个有效靶点。本研究组成功构建了一种新型

99m

Tc标记PSMA抑制剂

99m

Tc-HYNIC-Glu-Urea-A，本研究主要探讨该分子影像探针在前列腺癌模型中的靶向能力，并将其与目前临床常用PET显像剂

F-脱氧葡萄糖（

F-FDG）、

C-胆碱进行比较。

方法：

利用小动物SPECT/CT显像，在PC-3和LNCaP肿瘤模型中研究99mTc-HYNIC-Glu-Urea-A的靶向能力；同时在LNCaP肿瘤模型中评估

F-FDG和11C-胆碱小动物PET/CT显像效果。

结果：

99m

Tc-HYNIC-Glu-Urea-A血液清除迅速，主要通过肾代谢，肠道有少量放射性摄取，其余主要器官无明显放射性摄取。PSMA不表达的PC-3模型肿瘤没有放射性摄取，PSMA高表达的LNCaP模型肿瘤高度放射性浓聚，肿瘤/肌肉比值达20.4；经2-PMPA阻断后，LNCaP肿瘤的放射性摄取大幅度降低。LNCaP模型的

F-FDG和

C-胆碱的肿瘤/肌肉比值分别仅为2.1和2.6，远远低于

99m

Tc-HYNIC-Glu-Urea-A。

结论：

99m

Tc-HYNIC-Glu-Urea-A体内清除快，肿瘤摄取高，是一个理想的靶向PSMA的分子影像探针，对PSMA阳性肿瘤的显像优于

F-FDG和

C-胆碱。

Abstract

Objective:

Prostate specific membrane antigen (PSMA) is a well-established target for diagnosis and therapyof prostate cancer (PCa). We have synthesized an amino-functionalized PSMA inhibitor (Glu-Urea-A) and labeled technetium-99m via HYNIC. The in vivo target capacity of the new probe was evaluated in animal model and compared with

F-fluorodeoxyglucose (18F-F

DG) and

C-choline which were mostly used in clinic.

Methods:

The new probe was studied in severe combined immunodeficiency (SCID) mice bearing PC-3 and LNCaP tumor xenografts on small animal SPECT/CT. The comparative analysis of

F-FDG and

C-choline imagings was done in LNCaP tumor xenografts on small animal PET/CT. The tumor to muscle ratio wasobtained by the analysis software accompanying with small animal SPECT/CT and PET/CT respectively.

Results:

The imaging results showed that the metabolism of

99m

Tc-HYNIC-Glu-Urea-A was very fast. Kidney was the primary excretory organ and little radioactive uptake was found in intestines. There was no significant uptake in other organs. PC-3 tumor did not have any radioactive uptake. LNCaP tumor had very high radioactive uptake

and the tumor to muscle ratio was 20.4. The blocking experiment showed that the tumor uptake reduced significantly. The tumor to muscle ratio obtained from PET/CT imaging were only 2.1 and 2.6 for

F-FDG and

C-choline respectively

which were much lower than

99m

Tc-HYNIC-Glu-Urea-A.

Conclusion:

The probe

99m

Tc- HYNIC-Glu-Urea-A with fast metabolism and high tumor uptake was a promising molecular imaging probe targeting PSMA. It is superior to

F-FDG and

C-choline in prostate cancer imaging.

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