ArticleEJNMMI research2011
Mini-PEG spacering of VAP-1-targeting 68Ga-DOTAVAP-P1 peptide improves PET imaging of inflammation.
Article in EJNMMI research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 32 citations in OpenAlex.
- Imaging Inflammation with Positron Emission Tomography.Biomedicines · 2021Review
- Methods to Enhance the Metabolic Stability of Peptide-Based PET Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2020Review
- Antibody-Based Tracers for PET/SPECT Imaging of Chronic Inflammatory Diseases.Chembiochem : a European journal of chemical biology · 2019Review
- Adventures in radiosynthesis of clinical grade [RSC advances · 2018Article
- Prospective ofContrast media & molecular imaging · 2018Review
- Targeting of vascular adhesion protein-1 by positron emission tomography visualizes sites of inflammation in Borrelia burgdorferi-infected mice.Arthritis research & therapy · 2017Article
- Article
- Feasibility of (68)Ga-labeled Siglec-9 peptide for the imaging of acute lung inflammation: a pilot study in a porcine model of acute respiratory distress syndrome.American journal of nuclear medicine and molecular imaging · 2016Article
- 68Ga-DOTA-Siglec-9--a new imaging tool to detect synovitis.Arthritis research & therapy · 2015Article
- New radiotracers for imaging of vascular targets in angiogenesis-related diseases.Advanced drug delivery reviews · 2014Review
- (68)Ga-DOTA-Siglec-9 PET/CT imaging of peri-implant tissue responses and staphylococcal infections.EJNMMI research · 2014Article
- Prospective of ⁶⁸Ga-radiopharmaceutical development.Theranostics · 2013Review
- Peptides in receptor-mediated radiotherapy: from design to the clinical application in cancers.Frontiers in oncology · 2013Review
- Nuclear imaging of inflammation: homing-associated molecules as targets.EJNMMI research · 2013Article
- PET imaging of inflammation biomarkers.Theranostics · 2013Review
- Vascular adhesion protein 1 in the eye.Journal of ophthalmology · 2013Article
- Gallium-labelled peptides for imaging of inflammation.European journal of nuclear medicine and molecular imaging · 2012Review
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundVascular adhesion protein-1 (VAP-1) is an adhesion molecule that plays a key role in recruiting leucocytes into sites of inflammation. We have previously shown that 68Gallium-labelled VAP-1-targeting peptide (68Ga-DOTAVAP-P1) is a positron emission tomography (PET) imaging agent, capable of visualising inflammation in rats, but disadvantaged by its short metabolic half-life and rapid clearance. We hypothesised that prolonging the metabolic half-life of 68Ga-DOTAVAP-P1 could further improve its imaging characteristics. In this study, we evaluated a new analogue of 68Ga-DOTAVAP-P1 modified with a mini-polyethylene glycol (PEG) spacer (68Ga-DOTAVAP-PEG-P1) for in vivo imaging of inflammation.
methodsWhole-body distribution kinetics and visualisation of inflammation in a rat model by the peptides 68Ga-DOTAVAP-P1 and 68Ga-DOTAVAP-PEG-P1 were evaluated in vivo by dynamic PET imaging and ex vivo by measuring the radioactivity of excised tissues. In addition, plasma samples were analysed by radio-HPLC for the in vivo stability of the peptides.
resultsThe peptide with the mini-PEG spacer showed slower renal excretion but similar liver uptake as the original peptide. At 60 min after injection, the standardised uptake value of the inflammation site was 0.33 ± 0.07 for 68Ga-DOTAVAP-P1 and 0.53 ± 0.01 for 68Ga-DOTAVAP-PEG-P1 by PET. In addition, inflammation-to-muscle ratios were 6.7 ± 1.3 and 7.3 ± 2.1 for 68Ga-DOTAVAP-P1 and 68Ga-DOTAVAP-PEG-P1, respectively. The proportion of unchanged peptide in circulation at 60 min after injection was significantly higher for 68Ga-DOTAVAP-PEG-P1 (76%) than for 68Ga-DOTAVAP-P1 (19%).
conclusionThe eight-carbon mini-PEG spacer prolonged the metabolic half-life of the 68Ga-DOTAVAP-P1 peptide, leading to higher target-to-background ratios and improved in vivo PET imaging of inflammation.
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