ArticlePharmaceutics2022
PET Imaging of the Neurotensin Targeting Peptide NOTA-NT-20.3 Using Cobalt-55, Copper-64 and Gallium-68.
Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 12 citations in OpenAlex.
- An Evaluation of Cage Amine Sarcophagine Ligands for the Synthesis of Cobalt Radiopharmaceuticals.Inorganic chemistry · 2026Article
- Synthesis and Evaluation ofACS omega · 2026Article
- First positronium lifetime imaging usingScientific reports · 2026Article
- Investigating the Theranostic Potential of Elementally Matched [Molecular pharmaceutics · 2026Article
- Advances in neurotensin receptor 1-targeted molecular probes for tumor molecular imaging and therapy.Frontiers in oncology · 2026Review
- Unveiling the potential of copper-61 vs. gallium-68 for SSTR PET imaging.European journal of nuclear medicine and molecular imaging · 2025Article
- Radiocobalt-Labeling of a Polypyridylamine Chelate Conjugated to GE11 for EGFR-Targeted Theranostics.Molecules (Basel, Switzerland) · 2025Article
- Radiocobalt theranostic applications: current landscape, challenges, and future directions.Frontiers in nuclear medicine · 2025Review
- Radiolabeling Diaminosarcophagine with Cyclotron-Produced Cobalt-55 and [Bioconjugate chemistry · 2024Article
- Preclinical evaluation of [Scientific reports · 2023Article
- Separation of cyclotron-produced cobalt-55/58m from iron targets using cation exchange chromatography with non-aqueous solvents and extraction chromatography.Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine · 2023Article
- Theranostic cobalt-55/58m for neurotensin receptor-mediated radiotherapy in vivo: A pilot study with dosimetry.Nuclear medicine and biologyArticle
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Introduction: Neurotensin receptor 1 (NTSR1) is an emerging target for imaging and therapy of many types of cancer. Nuclear imaging of NTSR1 allows for noninvasive assessment of the receptor levels of NTSR1 on the primary tumor, as well as potential metastases. This work focuses on a the neurotensin peptide analogue NT-20.3 conjugated to the chelator NOTA for radiolabeling for use in noninvasive positron emission tomography (PET). NOTA-NT-20.3 was radiolabeled with gallium-68, copper-64, and cobalt-55 to determine the effect that modification of the radiometal has on imaging and potential therapeutic properties of NOTA-NT-20.3. Methods: In vitro assays investigating cell uptake and subcellular localization of the radiolabeled peptides were performed using human colorectal adenocarcinoma HT29 cells. In vivo PET/CT imaging was used to determine the distribution and clearance of the peptide in mice bearing NTSR1 expressing HT29 tumors. Results: Cell uptake studies showed that the highest uptake was obtained with [55Co] Co-NOTA-NT-20.3 (18.70 ± 1.30%ID/mg), followed by [64Cu] Cu-NOTA-NT-20.3 (15.46 ± 0.91%ID/mg), and lastly [68Ga] Ga-NOTA-NT-20.3 (10.94 ± 0.46%ID/mg) (p < 0.001). Subcellular distribution was similar across the three constructs, with the membranous fraction containing the highest amount of radioactivity. In vivo PET/CT imaging of the three constructs revealed similar distribution and tumor uptake at the 1 h imaging timepoint. Tumor uptake was receptor-specific and blockable by co-injection of non-radiolabeled NOTA-NT-20.3. SUV ratios of tumor to heart at the 24 h imaging timepoint show that [55Co] Co-NOTA-NT-20.3 (20.28 ± 3.04) outperformed [64Cu] Cu-NOTA-NT-20.3 (6.52 ± 1.97). In conclusion, our studies show that enhanced cell uptake and increasing tumor to blood ratios over time displayed the superiority of [55Co] Co-NOTA-NT-20.3 over [68Ga] Ga-NOTA-NT-20.3 and [64Cu] Cu-NOTA-NT-20.3 for the targeting of NTSR1.
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Registered trials
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