ArticleEuropean journal of nuclear medicine and molecular imaging2009
A stable neurotensin-based radiopharmaceutical for targeted imaging and therapy of neurotensin receptor-positive tumours.
Article in European journal of nuclear medicine and molecular imaging, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 65 citations in OpenAlex.
- Synthesis and Evaluation ofACS omega · 2026Article
- Advances in neurotensin receptor 1-targeted molecular probes for tumor molecular imaging and therapy.Frontiers in oncology · 2026Review
- Single Photon Emission Computed Tomography Tracer.Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer · 2026Review
- Article
- Chelator boosted tumor-retention and pharmacokinetic properties: development ofEuropean journal of nuclear medicine and molecular imaging · 2024Article
- Development of a Neurotensin-DerivedCancers · 2022Article
- Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor.European journal of medicinal chemistry · 2019Article
- Modifications at Arg and Ile Give Neurotensin(8-13) Derivatives with High Stability and Retained NTSACS medicinal chemistry letters · 2019Article
- A Review of the Role of Neurotensin and Its Receptors in Colorectal Cancer.Gastroenterology research and practice · 2017Review
- Investigation of the Biological Impact of Charge Distribution on a NTR1-Targeted Peptide.Bioconjugate chemistry · 2016Article
- Evaluation of DOTA-chelated neurotensin analogs with spacer-enhanced biological performance for neurotensin-receptor-1-positive tumor targeting.Nuclear medicine and biology · 2015Article
- Synthesis and Evaluation of 64Cu-DOTA-NT-Cy5.5 as a Dual-Modality PET/Fluorescence Probe to Image Neurotensin Receptor-Positive Tumor.Molecular pharmaceutics · 2015Article
- Neurotensin receptors in pancreatic ductal carcinomas.EJNMMI research · 2015Article
- Facile solid phase peptide synthesis with a Re-lysine conjugate generated via a one-pot procedure.Dalton transactions (Cambridge, England : 2003) · 2014Article
- A bombesin-shepherdin radioconjugate designed for combined extra- and intracellular targeting.Pharmaceuticals (Basel, Switzerland) · 2014Article
- In vivo monitoring of the antiangiogenic effect of neurotensin receptor-mediated radiotherapy by small-animal positron emission tomography: a pilot study.Pharmaceuticals (Basel, Switzerland) · 2014Article
- Neurotensin and its high affinity receptor 1 as a potential pharmacological target in cancer therapy.Frontiers in endocrinology · 2012Article
- Article
- Neurotensin receptor 1 is expressed in gastrointestinal stromal tumors but not in interstitial cells of Cajal.PloS one · 2011Article
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeNeurotensin (NT) and its high affinity receptor (NTR1) are involved in several neoplastic processes. Thus, NT-based radiopharmaceuticals are potential tracers for targeted diagnosis and therapy of NTR-positive tumours. A new analogue based on NT(8-13), NT-XIX, with the three enzymatic cleavage sites stabilised, was synthesised and tested.
methodsThe synthesis was performed by Boc strategy. Labelling with (99m)Tc/(188)Re was performed using the tricarbonyl technique. Metabolic stability was tested in vitro and in vivo. NT-XIX was further characterised in vitro in HT-29 cells and in vivo in nude mice with HT-29 xenografts.
resultsNT-XIX showed much longer half-lives than non-stabilised analogues. Binding to NTR1 was highly specific, although the affinity was lower than that of natural NT. Bound activity rapidly internalised into HT-29 cells and 50% remained trapped after 24 h. In the time-course biodistribution, the highest uptake was found in the tumour at all p.i. times. In vivo uptake was specific, and accumulation of activity in the kidneys was low. Radioactivity clearance from healthy organs was faster than that from the tumour, resulting in improved tumour-to-tissue ratios and good SPECT/CT imaging. Treatment with (188)Re-NT-XIX (30 MBq, in three or four fractions) decreased tumour growth by 50% after 3 weeks.
conclusionThe high in vivo stability and the favourable in vivo behaviour makes NT-XIX an excellent candidate for the imaging and therapy of NTR1-positive tumours.
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