PET of tumors expressing gastrin-releasing peptide receptor with an 18F-labeled bombesin analog
| Autor: | Christopher A. D’Souza, David M. Goldenberg, Gerben M. Franssen, Charles J. Smith, Otto C. Boerman, Ingrid Dijkgraaf, William J. McBride, Wim J.G. Oyen, Peter Laverman |
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| Rok vydání: | 2012 |
| Předmět: |
Male
Fluorine Radioisotopes Peptide receptor Binding Competitive chemistry.chemical_compound Mice Cell Line Tumor Gastrin-releasing peptide receptor Animals Humans Radiology Nuclear Medicine and imaging Tissue Distribution Neurotransmitter chemistry.chemical_classification Mice Inbred BALB C Chemistry Translational research Immune Regulation [ONCOL 3] Bombesin Prostatic Neoplasms Translational research Pathogenesis and modulation of inflammation [ONCOL 3] Amino acid Receptors Bombesin Biochemistry 18f labeling Isotope Labeling Positron-Emission Tomography Specific activity Radiopharmaceuticals Clearance |
| Zdroj: | The Journal of Nuclear Medicine (1978), 53, 947-52 The Journal of Nuclear Medicine (1978), 53, 6, pp. 947-52 |
| ISSN: | 1535-5667 0161-5505 |
| Popis: | Item does not contain fulltext The gastrin-releasing peptide receptor (GRPR) is overexpressed in human prostate cancer. Bombesin (BBN) is a neurotransmitter of 14 amino acids and binds with selectivity and with high affinity to GRPRs. We have synthesized a NOTA-conjugated bombesin derivative, NOTA-8-Aoc-BBN(7-14)NH(2), to label this analog with (18)F using the new Al(18)F method. In this study, the GRPR-targeting potential of (18)F-labeled NOTA-8-Aoc-BBN(7-14)NH(2) was studied using (68)Ga-NOTA-8-Aoc-BBN(7-14)NH(2) as a reference. METHODS: The NOTA-conjugated bombesin analog was synthesized and radiolabeled with (68)Ga or (18)F. For (18)F labeling, we used our new 1-pot, 1-step method. The labeled product was purified by reversed-phase high-performance liquid chromatography. The log P values of the radiotracers were determined. The tumor-targeting characteristics of the compounds were assessed in mice with subcutaneously growing PC-3 xenografts. GRPR-binding specificity was studied by coinjection of an excess of unlabeled NOTA-8-Aoc-BBN(7-14)NH(2). Small-animal PET/CT images were acquired. RESULTS: NOTA-8-Aoc-BBN(7-14)NH(2) could be efficiently labeled with (18)F or with (68)Ga. NOTA-8-Aoc-BBN(7-14)NH(2) was labeled with (18)F in a single step, with 50%-90% yield. Radiolabeling, including purification, was performed in 45 min and resulted in a specific activity of greater than 10 GBq/mumol. The log P values of (18)F- and (68)Ga-labeled NOTA-8-Aoc-BBN(7-14)NH(2) were -1.47 +/- 0.05 and -1.98 +/- 0.03, respectively. In mice, both radiolabeled compounds cleared rapidly from the blood ( |
| Databáze: | OpenAIRE |
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