ArticleMolecular imaging and biology2014
Pilot study of a novel (18)F-labeled FSHR probe for tumor imaging.
Article in Molecular imaging and biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Radiolabeled LHRH and FSH Analogues as Cancer Theranostic Agents: A Systematic Review.Journal of clinical medicine · 2025Review
- An all-in-one tetrazine reagent for cysteine-selective labeling and bioorthogonal activable prodrug construction.Nature communications · 2024Article
- Pilot Study: FSHR Expression in Neuroendocrine Tumors of the Appendix.Journal of clinical medicine · 2023Article
- Pre-treatment circulating reproductive hormones levels predict pathological and survival outcomes in breast cancer submitted to neoadjuvant chemotherapy.International journal of clinical oncology · 2022Article
- A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [Molecules (Basel, Switzerland) · 2019Review
- Targeting HER2-positive gastric cancer with a novelRSC advances · 2019Article
- Review
- Antibody Selection for Cancer Target Validation of FSH-Receptor in Immunohistochemical Settings.Antibodies (Basel, Switzerland) · 2017Article
- PET Imaging of FSHR Expression in Tumors withContrast media & molecular imaging · 2017Article
- PET of HER2 Expression with a NovelJournal of Cancer · 2017Article
- Molecular Imaging of Cancer with Nanoparticle-Based Theranostic Probes.Contrast media & molecular imaging · 2017Review
- In vivo targeting of metastatic breast cancer via tumor vasculature-specific nano-graphene oxide.Biomaterials · 2016Article
- Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals.World journal of gastrointestinal oncology · 2016Review
- An Investigation on a Novel Anti-tumor Fusion Peptide of FSH33-53-IIKK.Journal of Cancer · 2016Article
- PET of follicle-stimulating hormone receptor: broad applicability to cancer imaging.Molecular pharmaceutics · 2015Article
- Fluorine-18 radiochemistry, labeling strategies and synthetic routes.Bioconjugate chemistry · 2015Review
- Article
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10 authors.
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No grant is acknowledged in the PubMed record.
Abstract
purposeFollicle-stimulating hormone receptor (FSHR) is overexpressed in primary and metastatic tumor. Molecular imaging of FSHR is beneficial for prognosis and therapy of cancer. FSHβ(33-53) (YTRDLVYKDPARPKIQKTCTF), denoted as FSH1, is a FSHR antagonist. In the present study, maleimide-NOTA conjugate of FSH1 (NOTA-MAL-FSH1) was designed and labeled with [(18)F] aluminum fluoride. The resulting tracer, (18)F-Al-NOTA-MAL-FSH1, was preliminarily evaluated in PET imaging of FSHR-positive tumor. PROCEDURES: NOTA-MAL-FSH1 was synthesized and radiolabeled with Al(18)F complex. The tumor-targeting potential and pharmacokinetic profile of the (18)F-labeled compound were evaluated in vitro and in vivo using a PC3 human prostate tumor model.
results(18)F-Al-NOTA-MAL-FSH1 can be efficiently produced within 30 min with a non-decay-corrected yield of 48.6 ± 2.1 % and a radiochemical purity of more than 95 %. The specific activity was at least 30 GBq/μmol. The radiotracer was stable in phosphate-buffered saline and human serum for at least 2 h. The IC50 values of displacement (18)F-Al-NOTA-MAL-FSH1 with FSH1 were 252 ± 1.12 nM. The PC3 human prostate tumor xenografts were clearly visible with high contrast after injection of (18)F-Al-NOTA-MAL-FSH1 via microPET. At 30, 60 and 120 min postinjection, the tumor uptakes were 2.98 ± 0.29 % injected dose (ID)/g, 2.53 ± 0.20 %ID/g and 1.36 ± 0.12 %ID/g, respectively. Dynamic PET scanning showed that tumor uptake reached a plateau by about 6 min. Heart peaked earlier and then cleared quickly. Biodistribution studies confirmed that the normal organs except kidney uptakes were all below 1 %ID/g at 1 h p.i. The tumor-to-blood and tumor-to-muscle ratio at 10 min, 0.5, 1, and 2 h after injection were 1.64 ± 0.36, 2.97 ± 0.40, 9.31 ± 1.06, and 13.59 ± 2.33 and 7.05 ± 1.10, 10.10 ± 1.48, 16.17 ± 3.29, and 30.88 ± 4.67, respectively. The tracer was excreted mainly through the renal system, as evidenced by high levels of radioactivity in the kidneys. FSHR-binding specificity was also demonstrated by reduced tumor uptake of (18)F-Al-NOTA-MAL-FSH1 after coinjection with an excess of unlabeled FSH1 peptide.
conclusionNOTA-MAL-FSH1 could be labeled rapidly and efficiently with (18)F using one step method. Favorable preclinical data suggest that (18)F-Al-NOTA-MAL-FSH1 may be a suitable radiotracer for the non-invasive visualization of FSHR positive tumor in vivo.
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