Synthesis and Evaluation of 18F-Labeled Peptide for Gonadotropin-Releasing Hormone Receptor Imaging
Joint Authors
Wu, Hu-bing
Wang, Quan-shi
Han, Yan-jian
Hu, Kongzhen
Huang, Shun
Li, Hongsheng
Fu, Lilan
Ren, Yunyan
Zhang, Yin
Li, Youcai
Sun, Penghui
Wang, Meng
Source
Contrast Media & Molecular Imaging
Issue
Vol. 2019, Issue 2019 (31 Dec. 2019), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2019-03-07
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
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 18F-labeled peptide for tumor GnRH receptor imaging.
In this study, the GnRH (pGlu1-His2-Trp3-Ser4-Tyr5-Gly6-Leu7-Arg8-Pro9-Gly10-NH2) peptide analogues FP-d-Lys6-GnRH (FP = 2-fluoropropanoyl) and NOTA-P-d-Lys6-GnRH (P = ethylene glycol) were designed and synthesized.
The IC50 values of FP-d-Lys6-GnRH and NOTA-P-d-Lys6-GnRH were 2.0 nM and 56.2 nM, respectively.
4-Nitrophenyl-2-[18F]fluoropropionate was conjugated to the ε-amino group of the d-lysine side chain of d-Lys6-GnRH to yield the new tracer [18F]FP-d-Lys6-GnRH with a decay-corrected yield of 8 ± 3% and a specific activity of 20−100 GBq/µmol (n=6).
Cell uptake studies of [18F]FP-d-Lys6-GnRH in GnRH receptor-positive PC-3 cells 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 [18F]FP-d-Lys6-GnRH was localized in tumors with a higher uptake than in surrounding muscle and heart tissues.
Furthermore, the metabolic stability of [18F]FP-d-Lys6-GnRH was determined in mouse blood and PC-3 tumor homogenates at 1 h after tracer injection.
The presented results indicated a potential of the novel tracer [18F]FP-d-Lys6-GnRH for tumor GnRH receptor imaging.
American Psychological Association (APA)
Huang, Shun& Li, Hongsheng& Han, Yan-jian& Fu, Lilan& Ren, Yunyan& Zhang, Yin…[et al.]. 2019. Synthesis and Evaluation of 18F-Labeled Peptide for Gonadotropin-Releasing Hormone Receptor Imaging. Contrast Media & Molecular Imaging،Vol. 2019, no. 2019, pp.1-10.
https://search.emarefa.net/detail/BIM-1130290
Modern Language Association (MLA)
Huang, Shun…[et al.]. Synthesis and Evaluation of 18F-Labeled Peptide for Gonadotropin-Releasing Hormone Receptor Imaging. Contrast Media & Molecular Imaging No. 2019 (2019), pp.1-10.
https://search.emarefa.net/detail/BIM-1130290
American Medical Association (AMA)
Huang, Shun& Li, Hongsheng& Han, Yan-jian& Fu, Lilan& Ren, Yunyan& Zhang, Yin…[et al.]. Synthesis and Evaluation of 18F-Labeled Peptide for Gonadotropin-Releasing Hormone Receptor Imaging. Contrast Media & Molecular Imaging. 2019. Vol. 2019, no. 2019, pp.1-10.
https://search.emarefa.net/detail/BIM-1130290
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1130290