title: PET radioligands for in vivo visualization of neuroinflammation.
abstract: Neuroinflammation is a well-orchestrated, dynamic, multicellular process playing a major role in neurodegenerative disorders. The microglia which make up the innate immune system of the central nervous system are key cellular mediators of neuroinflammatory processes. In normal condition they exert a protective function, providing tissue repair by releasing anti-inflammatory cytokines and neurotrophic factors. Upon neuronal injury or infection, they become overactivated, thereby releasing neurotoxic substances, amplifying neuroinflammation leading to neurodegeneration. Positron emission tomography (PET) provides a sensitive non-invasive imaging technique to study and quantify receptor and enzyme expression. A radiolabeled tracer for a protein (over)expressed in neuroinflammation and more specifically for the overactivated microglia would be useful as a diagnostic tool in the follow-up of neuroinflammation progression and to study the efficacy of anti-inflammatory therapy over time. In this manuscript, an overview of potential PET tracer targets upregulated during neuroinflammation is provided together with the current radiotracers used to image these targets. In addition, lead structures to develop radiotracers for new targets are suggested.
authors.forename: Dieter
authors.initials: D
authors.lastname: Ory
authors.forename: Sofie
authors.initials: S
authors.lastname: Celen
authors.forename: Alfons
authors.initials: A
authors.lastname: Verbruggen
authors.affiliation: Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium. Guy.Bormans@pharm.kuleuven.be.
authors.forename: Guy
authors.initials: G
authors.lastname: Bormans
mesh_terms: D000818:Animals; D006801:Humans; D008024:Ligands; D019636:Neurodegenerative Diseases / Q000378:metabolism* / Q000473:pathology*; D049268:Positron-Emission Tomography; D011849:Radioactive Tracers; D011869:Radioligand Assay
chemical_list: D008024:Ligands; D011849:Radioactive Tracers