Evidence map›Paper›PMID 21487838›Full record

ArticleEuropean journal of nuclear medicine and molecular imaging2011

[68Ga]NODAGA-RGD for imaging αvβ3 integrin expression.

Peter A Knetsch, Milos Petrik, Christoph M Griessinger, Christine Rangger, Melpomeni Fani, Christian Kesenheimer, Elisabeth von Guggenberg, Bernd J Pichler, Irene Virgolini, Clemens Decristoforo and 1 more

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In one paragraph

Article in European journal of nuclear medicine and molecular imaging, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 62 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
62citing papers in PubMed, 1 pooled it
6.9field-weighted citation impact, top 2% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

62 citing papers in PubMed, 1 synthesis or guideline pooled it, 132 citations in OpenAlex.

  1. Pooled it
  2. Natural History of Myocardial αJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2024
    Trial
  3. Review
  4. Review
  5. From incidental positron emission uptake toFrontiers in cardiovascular medicine · 2026
    Review
  6. [European journal of nuclear medicine and molecular imaging · 2026
    Article
  7. Molecular pharmaceutics · 2025
    Article
  8. Journal of medicinal chemistry · 2024
    Article
  9. [EJNMMI radiopharmacy and chemistry · 2024
    Article
  10. Article
  11. American journal of nuclear medicine and molecular imaging · 2024
    Article
  12. Comparison of integrin αEuropean journal of hybrid imaging · 2023
    Article
  13. Review
  14. Article
  15. Review
  16. Article
  17. [International journal of molecular sciences · 2021
    Article
  18. Association between [Molecular biology reports · 2021
    Article
  19. Synthesis of a DOTA-RSC advances · 2021
    Article
  20. [Cells · 2020
    Article

2 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors at 4 institutions in 2 countries.

Peter A KnetschDepartment of Nuclear Medicine, Innsbruck Medical University, Innsbruck, Austria. peter.knetsch@i-med.ac.at
Milos Petrik
Christoph M Griessinger
Christine Rangger
Melpomeni Fani
Christian Kesenheimer
Elisabeth von Guggenberg
Bernd J Pichler
Irene Virgolini
Clemens Decristoforo
Roland Haubner
Innsbruck Medical University · ATUniversity of Tübingen · DESiemens (Germany) · DEUniversity of Freiburg · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeA molecular target involved in the angiogenic process is the α(v)β(3) integrin. It has been demonstrated in preclinical as well as in clinical studies that radiolabelled RGD peptides and positron emission tomography (PET) allow noninvasive monitoring of α(v)β(3) expression. Here we introduce a (68)Ga-labelled NOTA-conjugated RGD peptide ([(68)Ga]NODAGA-RGD) and compare its imaging properties with [(68)Ga]DOTA-RGD using small animal PET.

methodsSynthesis of c(RGDfK(NODAGA)) was based on solid phase peptide synthesis protocols using the Fmoc strategy. The (68)Ga labelling protocol was optimized concerning temperature, peptide concentration and reaction time. For in vitro characterization, partition coefficient, protein binding properties, serum stability, α(v)β(3) binding affinity and cell uptake were determined. To characterize the in vivo properties, biodistribution studies and microPET imaging were carried out. For both in vitro and in vivo evaluation, α(v)β(3)-positive human melanoma M21 and α(v)β(3)-negative M21-L cells were used.

results[(68)Ga]NODAGA-RGD can be produced within 5 min at room temperature with high radiochemical yield and purity (> 96%). In vitro evaluation showed high α(v)β(3) binding affinity (IC(50) = 4.7 ± 1.6 nM) and receptor-specific uptake. The radiotracer was stable in phosphate-buffered saline, pH 7.4, FeCl(3) solution, and human serum. Protein-bound activity after 180 min incubation was found to be 12-fold lower than for [(68)Ga]DOTA-RGD. Biodistribution data 60 min post-injection confirmed receptor-specific tumour accumulation. The activity concentration of [(68)Ga]NODAGA-RGD was lower than [(68)Ga]DOTA-RGD in all organs and tissues investigated, leading to an improved tumour to blood ratio ([(68)Ga]NODAGA-RGD: 11, [(68)Ga]DOTA-RGD: 4). MicroPET imaging confirmed the improved imaging properties of [(68)Ga]NODAGA-RGD compared to [(68)Ga]DOTA-RGD.

conclusionThe introduced [(68)Ga]NODAGA-RGD combines easy accessibility with high stability and good imaging properties making it an interesting alternative to the (18)F-labelled RGD peptides currently used for imaging α(v)β(3) expression.

Indexed as

Coordination ComplexesGene Expression RegulationOligopeptidesPeptides, CyclicAnimalsCell Line, TumorHeterocyclic CompoundsHeterocyclic Compounds, 1-RingHumansIntegrin alphaVbeta3Isotope LabelingMicePositron-Emission Tomography1,4,7-triazacyclononane-N,N',N''-triacetic acid68Ga-NODAGA-RGDarginyl-glycyl-aspartic acidCoordination ComplexesHeterocyclic CompoundsHeterocyclic Compounds, 1-RingIntegrin alphaVbeta3OligopeptidesPeptides, Cyclic

Identifiers

PMID21487838
OpenAlexW2055421103

What OpenQuestion holds

Textmetadata
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Registered trials

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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.