ArticleBioconjugate chemistry2012
Preparation and biological evaluation of (64)Cu labeled Tyr(3)-octreotate using a phosphonic acid-based cross-bridged macrocyclic chelator.
Article in Bioconjugate chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 45 citations in OpenAlex.
- Tuning the Properties of Rigidified Acyclic DEDPAInorganic chemistry · 2024Article
- A Theranostic Small-Molecule Prodrug Conjugate for Neuroendocrine Prostate Cancer.Pharmaceutics · 2023Article
- ImmunoPET: Concept, Design, and Applications.Chemical reviews · 2020Review
- Article
- Somatostatin analogues labeled with copper radioisotopes: current status.Journal of radioanalytical and nuclear chemistry · 2017Review
- New Bifunctional Chelator p-SCN-PhPr-NE3TA for Copper-64: Synthesis, Peptidomimetic Conjugation, Radiolabeling, and Evaluation for PET Imaging.Inorganic chemistry · 2016Article
- Visualization and quantification of simian immunodeficiency virus-infected cells using non-invasive molecular imaging.The Journal of general virology · 2015Article
- Cu(I)-assisted click chemistry strategy for conjugation of non-protected cross-bridged macrocyclic chelators to tumour-targeting peptides.Dalton transactions (Cambridge, England : 2003) · 2015Article
- First-in-human uPAR PET: Imaging of Cancer Aggressiveness.Theranostics · 2015Article
- Comparison of conjugation strategies of cross-bridged macrocyclic chelators with cetuximab for copper-64 radiolabeling and PET imaging of EGFR in colorectal tumor-bearing mice.Molecular pharmaceutics · 2014Article
- Nanoparticle ligand presentation for targeting solid tumors.AAPS PharmSciTech · 2014Review
- Characterization and evaluation of (64)Cu-labeled A20FMDV2 conjugates for imaging the integrin αvβ 6.Molecular imaging and biology · 2014Article
- 64Cu-labeled somatostatin analogues conjugated with cross-bridged phosphonate-based chelators via strain-promoted click chemistry for PET imaging: in silico through in vivo studies.Journal of medicinal chemistry · 2014Article
- Chelators for copper radionuclides in positron emission tomography radiopharmaceuticals.Journal of labelled compounds & radiopharmaceuticals · 2014Review
- Pycup--a bifunctional, cage-like ligand for (64)Cu radiolabeling.Molecular pharmaceutics · 2014Article
- New cross-bridged cyclam derivative CB-TE1K1P, an improved bifunctional chelator for copper radionuclides.Chemical communications (Cambridge, England) · 2014Article
- Comparison of two cross-bridged macrocyclic chelators for the evaluation of 64Cu-labeled-LLP2A, a peptidomimetic ligand targeting VLA-4-positive tumors.Nuclear medicine and biology · 2013Article
- Improved PET imaging of uPAR expression using new (64)Cu-labeled cross-bridged peptide ligands: comparative in vitro and in vivo studies.Theranostics · 2013Article
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3 authors at 2 institutions in 1 country.
Funding
Abstract
Somatostatin receptors (SSTr) are overexpressed in a wide range of neuroendocrine tumors, making them excellent targets for nuclear imaging and therapy, and radiolabeled somatostatin analogues have been investigated for positron emission tomography imaging and radionuclide therapy of SSTr-positive tumors, especially of the subtype-2 (SSTr2). The aim of this study was to develop a somatostatin analogue, Tyr(3)-octreotate (Y3-TATE), conjugated to a novel cross-bridged macrocyclic chelator, 11-carboxymethyl-1,4,8,11-tetraazabicyclo[6.6.2]hexadecane-4-methanephosphonic acid (CB-TE1A1P). Unlike traditional cross-bridged macrocycles, such as 4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo[6.6.2]hexadecane (CB-TE2A), CB-TE1A1P-Y3-TATE was radiolabeled with (64)Cu in high purity and high specific activity using mild conditions. Saturation binding assays revealed that (64)Cu-CB-TE1A1P-Y3-TATE had comparable binding affinity but bound to more binding sites in AR42J rat pancreatic tumor cell membranes than (64)Cu-CB-TE2A-Y3-TATE. Both radiopharmaceuticals showed comparable uptake in SSTr2 positive tissues in AR42J tumor-bearing rats. (64)Cu-CB-TE1A1P-Y3-TATE demonstrated improved blood clearance compared to (64)Cu-CB-TE2A-Y3-TATE, as the tumor/blood ratios of (64)Cu-CB-TE1A1P-Y3-TATE were shown to be significantly higher than those of (64)Cu-CB-TE2A-Y3-TATE at 4 and 24 h postinjection. (64)Cu-CB-TE1A1P-Y3-TATE, in spite of a relatively high kidney uptake, accumulated less in nontarget organs such as liver, lung, and bone. Small animal PET/CT imaging of (64)Cu-CB-TE1A1P-Y3-TATE in AR42J tumor bearing rats validated significant uptake and good contrast in the tumor. This study suggests that CB-TE1A1P is a promising bifunctional chelator for (64)Cu-labeled for Y3-TATE, owing to high binding affinity and target tissue uptake, the ability to radiolabel the agent at lower temperatures, and improved tumor/nontarget organ ratios over (64)Cu-CB-TE2A-Y3-TATE.
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