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Radiolabeling lipoproteins to study and manage disease.

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Abstract

Lipoproteins are endogenous nanoparticles with essential roles in lipid transport and inflammation. Lipoproteins are also valuable in diagnosing and treating disease. For instance, certain lipoproteins are overexpressed in patients with atherosclerotic cardiovascular disease, and reconstituted lipoproteins have been extensively used for drug delivery. Radiolabeling has proven an especially powerful approach for studying and therapeutically exploiting lipoproteins. This review details how radiochemistry and nuclear imaging can facilitate the study of lipoproteins in health and disease. Among other topics, we discuss approaches for radiolabeling lipoproteins and detail how these have helped advance our understanding of lipoprotein biology and the diagnosis and treatment of diseases, including atherosclerosis, cancer, and hypercholesteremia. We performed an extensive literature search on all peer-reviewed studies involving radiolabeled lipoproteins and selected representative examples to provide a high-level overview of the most important discoveries and technological advancements. More than 200 peer-reviewed papers involved radiolabeled lipoproteins, spanning mechanistic, diagnostic, and therapeutic studies across a wide range of diseases. Radiolabeling has been critical in advancing our understanding of lipoprotein biology and leveraging these nanomaterials for diagnosing and treating disease.

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Eur J Nucl Med Mol Imaging. 2025 Oct;52(12):4717-4734.

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