Mini-PEG spacering of VAP-1-targeting 68Ga-DOTAVAP-P1 peptide improves PET imaging of inflammation
作者： Anu Autio , Tiina Henttinen , Henri J Sipilä , Sirpa Jalkanen , Anne Roivainen
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摘要: Vascular adhesion protein-1 (VAP-1) is an molecule that plays a key role in recruiting leucocytes into sites of inflammation. We have previously shown 68Gallium-labelled VAP-1-targeting peptide (68Ga-DOTAVAP-P1) positron emission tomography (PET) imaging agent, capable visualising inflammation rats, but disadvantaged by its short metabolic half-life and rapid clearance. hypothesised prolonging the 68Ga-DOTAVAP-P1 could further improve characteristics. In this study, we evaluated new analogue modified with mini-polyethylene glycol (PEG) spacer (68Ga-DOTAVAP-PEG-P1) for vivo Whole-body distribution kinetics visualisation rat model peptides 68Ga-DOTAVAP-PEG-P1 were dynamic PET ex measuring radioactivity excised tissues. addition, plasma samples analysed radio-HPLC stability peptides. The mini-PEG showed slower renal excretion similar liver uptake as original peptide. At 60 min after injection, standardised value site was 0.33 ± 0.07 0.53 0.01 PET. inflammation-to-muscle ratios 6.7 1.3 7.3 2.1 68Ga-DOTAVAP-PEG-P1, respectively. proportion unchanged circulation at injection significantly higher (76%) than (19%). eight-carbon prolonged peptide, leading to target-to-background improved
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