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First-in-Human Study of 68 Ga-DOTA-Siglec-9, PET Ligand Targeting Vascular Adhesion Protein 1
Sialic acid-binding immunoglubulin-like lectin 9 (Siglec-9) is a ligand of vascular adhesion protein 1 (VAP-1). A gallium 68-labeled peptide of Siglec-9, <sup>68</sup>Ga-DOTA-Siglec-9, holds promise as a novel PET tracer ...
Association between [Ga-68]NODAGA-RGDyK uptake and dynamics of angiogenesis in a human cell-based 3D model
Radiolabeled RGD peptides targeting expression of alpha(v)beta(3) integrin have been applied to in vivo imaging of angiogenesis. However, there is a need for more information on the quantitative relationships between RGD ...
Exploiting Glutamine Consumption in Atherosclerotic Lesions by Positron Emission Tomography Tracer (2S,4R)-4-F-18-Fluoroglutamine
Increased glutamine metabolism by macrophages is associated with development of atherosclerotic lesions. Positron emission tomography/computed tomography (PET/CT) with a glutamine analog (2S,4R)-4-F-18-fluoroglutamine ...
Evaluation of [68Ga]Ga-NODAGA-RGD for PET Imaging of Rat Autoimmune Myocarditis
<p>The <sup>68</sup>Gallium-labeled 1,4,7-triazacyclononane-1-glutaric acid-4,7-diacetic acid conjugated radiolabelled arginine-glycine-aspartic acid peptide ([<sup>68</sup>Ga]Ga-NODAGA-RGD) is a positron emission tomography (PET) tracer binding to cell surface receptor α<sub>v</sub>β<sub>3</sub> integrin that is upregulated during angiogenesis and inflammation. We studied whether α<sub>v</sub>β<sub>3</sub> targeting PET imaging can detect myocardial inflammation in a rat model of autoimmune myocarditis. To induce myocarditis, rats (n = 8) were immunized with porcine cardiac myosin in complete Freund's adjuvant on days 0 and 7. Control rats (n = 8) received Freund's adjuvant alone. On day 21, in vivo PET/CT imaging with [<sup>68</sup>Ga]Ga-NODAGA-RGD followed by ex vivo autoradiography and immunohistochemistry were carried out. Inflammatory lesions were detected histologically in the myocardium of 7 out of 8 immunized rats. In vivo PET images showed higher [<sup>68</sup>Ga]Ga-NODAGA-RGD accumulation in the myocardium of rats with inflammation than the non-inflamed myocardium of control rats (SUV<sub>mean</sub> 0.4 ± 0.1 vs. 0.1 ± 0.02; P = 0.00006). Ex vivo autoradiography and histology confirmed that [<sup>68</sup>Ga]Ga-NODAGA-RGD uptake co-localized with inflammatory lesions containing α<sub>v</sub>β<sub>3</sub> integrin-positive capillary-like structures. A non-specific [<sup>68</sup>Ga]Ga-DOTA-(RGE)<sub>2</sub> tracer showed 76% lower uptake than [<sup>68</sup>Ga]Ga-NODAGA-RGD in the inflamed myocardium. Our results indicate that α<sub>v</sub>β<sub>3</sub> integrin-targeting [<sup>68</sup>Ga]Ga-NODAGA-RGD is a potential PET tracer for the specific detection of active inflammatory lesions in autoimmune myocarditis.<br></p>...