Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors

Wagner, Stefan; Gatti, Fernando de Moura; Silva, Daniel G.; Zacarı́as, Natalia V. Ortiz; Zweemer, Annelien J.M.; Hermann, Sven; Maria, Monica De; Koch, Michael; Weiss, Christina; Schepmann, Dirk; Heitman, Laura H.; Tschammer, Nuška; Kopka, Klaus; Junker, Anna

doi:10.1002/cmdc.202000728

Cited by 6 publications

(3 citation statements)

References 16 publications

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“…The tracer was stable in vitro and in vivo, and showed little defluorination and a fast uptake in the liver, spleen, lungs and kidneys of healthy mice. However, preclinical evaluation of this tracer in a pathological model has not been reported so far (Wagner et al 2021 ). Another group labeled the peptide ECLi with copper-64 and used it to assess the expression of CCR2 in a rodent model of an abdominal aortic aneurysm (AAA), in which monocytes and macrophages play a critical role.…”

Section: Main Textmentioning

confidence: 99%

Potential PET tracers for imaging of tumor-associated macrophages

Fernandes

Feltes

Luft

et al. 2022

EJNMMI radiopharm. chem.

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The increasing incidence of cancer over the years is one of the most challenging problems in healthcare. As cancer progresses, the recruitment of several immune cells is triggered. Infiltration of tumor-associated macrophages (TAMs) is correlated with poor patient prognosis. Since TAMs constitute a big portion of the tumor mass, targeting these cells seems to be an attractive approach for cancer immunotherapy. Additionally, TAM assessment using non-invasive imaging techniques, such as positron emission tomography (PET), might provide a better understanding of the role of TAMs in cancer, and a means for tumor profile characterization, patient selection for individualized immunotherapy and treatment monitoring. Imaging of TAMs using PET tracers is still in its infancy. TAMs have several characteristics that could be exploited as potential targets for imaging. Various PET tracers for these TAM biomarkers have been developed, although often in the context of (neuro)inflammatory diseases rather than cancer. Since macrophages in inflammatory diseases express similar biomarkers as TAMs, these PET tracers could potentially also be applied for the assessment of TAMs in the tumor microenvironment. Therefore, the present review provides an overview of the TAM biomarkers, for which potential PET tracers are available and discusses the status of these tracers.

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Section: Main Textmentioning

confidence: 99%

Potential PET tracers for imaging of tumor-associated macrophages

Fernandes

Feltes

Luft

et al. 2022

EJNMMI radiopharm. chem.

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“…Recently, Wagner and colleagues synthetized the first small-molecule, nonpeptidic, fluorine-18-labelled CCR2-targeting radiotracer. The authors reported an exceptional target affinity and selectivity; however, further in vivo biodistribution and proof-of-concept studies are necessary to support a role for this novel tracer in the setting of inflammation imaging [ 102 ].…”

Section: Imaging Targets Of Inflammationmentioning

confidence: 99%

Imaging Inflammation with Positron Emission Tomography

et al. 2021

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The impact of inflammation on the outcome of many medical conditions such as cardiovascular diseases, neurological disorders, infections, cancer, and autoimmune diseases has been widely acknowledged. However, in contrast to neurological, oncologic, and cardiovascular disorders, imaging plays a minor role in research and management of inflammation. Imaging can provide insights into individual and temporospatial biology and grade of inflammation which can be of diagnostic, therapeutic, and prognostic value. There is therefore an urgent need to evaluate and understand current approaches and potential applications for imaging of inflammation. This review discusses radiotracers for positron emission tomography (PET) that have been used to image inflammation in cardiovascular diseases and other inflammatory conditions with a special emphasis on radiotracers that have already been successfully applied in clinical settings.

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“…Ongoing clinical studies will further evaluate the performance of 64 Cu-DOTA-ECL1i for tracking CCR21 cells in humans (23). Recently, an 18 F-radiolabeled small molecule was also developed for CCR2 preclinical imaging (24).…”

Section: Molecular Imaging Of Crosstalk Between Immune System and Fibrosis In Cvds Immune Cell Imagingmentioning

confidence: 99%

The Latest Advances in Imaging Crosstalk Between the Immune System and Fibrosis in Cardiovascular Disease

et al. 2021

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Inflammation and fibrosis are hallmarks of tissue repair processes and organ failure progression in cardiovascular diseases. Paradigm-shifting research on diverse immune cell populations within the cardiovascular system have enabled discovery of new biomarkers fostering development of diagnostic and therapeutic agents at the molecular level to better manage cardiovascular diseases. To date, a variety of molecular imaging agents have been developed to visualize the biomarkers expressed on immune cells and fibroblasts within their crosstalk network, which drives the pathogenesis of fibrosis triggered by both innate and adaptive immunity. Herein, key biomarkers upregulated in the immune-fibrosis axis are discussed. The promising molecular imaging agents to reveal this critical pathologic process are summarized.

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Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors

Cited by 6 publications

References 16 publications

Potential PET tracers for imaging of tumor-associated macrophages

Potential PET tracers for imaging of tumor-associated macrophages

Imaging Inflammation with Positron Emission Tomography

The Latest Advances in Imaging Crosstalk Between the Immune System and Fibrosis in Cardiovascular Disease

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