Synthesis and Evaluation of 18F-Labeled Peptide for Gonadotropin-Releasing Hormone Receptor Imaging

被引：9

作者：

Huang, Shun ^{[1
]}

Li, Hongsheng ^{[1
]}

Han, Yanjiang ^{[1
]}

Fu, Lilan ^{[1
]}

Ren, Yunyan ^{[1
]}

Zhang, Yin ^{[1
]}

Li, Youcai ^{[1
]}

Sun, Penghui ^{[1
]}

Wang, Meng ^{[1
]}

Wu, Hubing ^{[1
]}

Wang, Quanshi ^{[1
]}

Hu, Kongzhen ^{[1
]}

机构：

[1] Southern Med Univ, Nanfang Hosp, Nanfang PET Ctr, 1838 Guangzhou Ave North, Guangzhou 510515, Guangdong, Peoples R China

来源：

CONTRAST MEDIA & MOLECULAR IMAGING | 2019年

基金：

中国国家自然科学基金;

关键词：

HUMAN ENDOMETRIAL; PROSTATE CANCERS; ANALOG AN-152; OVARIAN; PET; ANTAGONISTS; EXPRESSION; BREAST; TRACER; TUMORS;

D O I：

10.1155/2019/5635269

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

The gonadotropin-releasing hormone (GnRH) receptor is overexpressed in the majority of tumors of the human reproductive system. The purpose of this study was to develop an F-18-labeled peptide for tumor GnRH receptor imaging. In this study, the GnRH (pGlu(1)-His(2)-Trp(3)-Ser(4)-Tyr(5)-Gly(6)-Leu(7)-Arg(8)-Pro(9)-Gly(10)-NH2) peptide analogues FP-d-Lys(6)-GnRH (FP=2-fluoropropanoyl) and NOTA-P-d-Lys(6)-GnRH (P=ethylene glycol) were designed and synthesized. The IC50 values of FP-d-Lys(6)-GnRH and NOTA-P-d-Lys(6)-GnRH were 2.0nM and 56.2nM, respectively. 4-Nitrophenyl-2-[F-18]fluoropropionate was conjugated to the epsilon-amino group of the d-lysine side chain of d-Lys(6)-GnRH to yield the new tracer [F-18]FP-d-Lys(6)-GnRH with a decay-corrected yield of 8 +/- 3% and a specific activity of 20-100GBq/mu mol (n=6). Cell uptake studies of [F-18]FP-d-Lys(6)-GnRH in GnRH receptor-positive PC-3cells and GnRH receptor-negative CHO-K1 cells indicated receptor-specific accumulation. Biodistribution and PET studies in nude mice bearing PC-3 xenografted tumors showed that [F-18]FP-d-Lys(6)-GnRH was localized in tumors with a higher uptake than in surrounding muscle and heart tissues. Furthermore, the metabolic stability of [F-18]FP-d-Lys(6)-GnRH was determined in mouse blood and PC-3 tumor homogenates at 1h after tracer injection. The presented results indicated a potential of the novel tracer [F-18]FP-d-Lys(6)-GnRH for tumor GnRH receptor imaging.

引用

页数：10

共 35 条

[1] Backbone metal cyclization:: novel 99mTc labeled GnRH analog as potential SPECT molecular imaging agent in cancer [J].