ArticleJournal of medicinal chemistry2014
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.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
14 citing papers in PubMed, 40 citations in OpenAlex.
- Click chemistry: a transformative technology in nuclear medicine.Nature protocols · 2023Review
- Computer-Assisted Design of Peptide-Based Radiotracers.International journal of molecular sciences · 2023Review
- Molecular simulations of SSTR2 dynamics and interaction with ligands.Scientific reports · 2023Article
- Synthesis of a Bifunctional Cross-Bridged Chelating Agent, Peptide Conjugation, and Comparison ofChemMedChem · 2023Article
- Artificial Intelligence and the Future of Diagnostic and Therapeutic Radiopharmaceutical Development:: In Silico Smart Molecular Design.PET clinics · 2021Review
- A multi-functional polymeric carrier for simultaneous positron emission tomography imaging and combination therapy.Acta biomaterialia · 2018Article
- Article
- A Modular Dual-Labeling Scaffold That Retains Agonistic Properties for Somatostatin Receptor Targeting.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2017Article
- Somatostatin analogues labeled with copper radioisotopes: current status.Journal of radioanalytical and nuclear chemistry · 2017Review
- Click Chemistry and Radiochemistry: The First 10 Years.Bioconjugate chemistry · 2016Review
- Homology modeling, docking, and molecular dynamics simulation of the receptor GALR2 and its interactions with galanin and a positive allosteric modulator.Journal of molecular modeling · 2016Article
- Small Molecule Radiopharmaceuticals - A Review of Current Approaches.Frontiers in medicine · 2016Review
- Optimization of a Pretargeted Strategy for the PET Imaging of Colorectal Carcinoma via the Modulation of Radioligand Pharmacokinetics.Molecular pharmaceutics · 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
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
Abstract
Somatostatin receptor subtype 2 (sstr2) is a G-protein-coupled receptor (GPCR) that is overexpressed in neuroendocrine tumors. The homology model of sstr2 was built and was used to aid the design of new somatostatin analogues modified with phosphonate-containing cross-bridged chelators for evaluation of using them as PET imaging radiopharmaceuticals. The new generation chelators were conjugated to Tyr3-octreotate (Y3-TATE) through bioorthogonal, strain-promoted alkyne azide cycloaddition (SPAAC) to form CB-TE1A1P-DBCO-Y3-TATE (AP) and CB-TE1K1P-PEG4-DBCO-Y3-TATE (KP) in improved yields compared to standard direct conjugation methods of amide bond formation. Consistent with docking studies, the clicked bioconjugates showed high binding affinities to sstr2, with Kd values ranging from 0.6 to 2.3 nM. Selected isomers of the clicked products were used in biodistribution and PET/CT imaging. Introduction of the bulky dibenzocyclooctyne group in AP decreased clearance rates from circulation. However, the additional carboxylate group and PEG linker from the KP conjugate significantly improved labeling conditions and in vivo stability of the copper complex and ameliorated the slower pharmacokinetics of the clicked somatostatin analogues.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.