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The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.

Authors :
Chen Z
Haider A
Chen J
Xiao Z
Gobbi L
Honer M
Grether U
Arnold SE
Josephson L
Liang SH
Source :
Journal of medicinal chemistry [J Med Chem] 2021 Dec 23; Vol. 64 (24), pp. 17656-17689. Date of Electronic Publication: 2021 Dec 14.
Publication Year :
2021

Abstract

Neuroinflammation is an adaptive response of the central nervous system to diverse potentially injurious stimuli, which is closely associated with neurodegeneration and typically characterized by activation of microglia and astrocytes. As a noninvasive and translational molecular imaging tool, positron emission tomography (PET) could provide a better understanding of neuroinflammation and its role in neurodegenerative diseases. Ligands to translator protein (TSPO), a putative marker of neuroinflammation, have been the most commonly studied in this context, but they suffer from serious limitations. Herein we present a repertoire of different structural chemotypes and novel PET ligand design for classical and emerging neuroinflammatory targets beyond TSPO. We believe that this Perspective will support multidisciplinary collaborations in academic and industrial institutions working on neuroinflammation and facilitate the progress of neuroinflammation PET probe development for clinical use.

Details

Language :
English
ISSN :
1520-4804
Volume :
64
Issue :
24
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
34905377
Full Text :
https://doi.org/10.1021/acs.jmedchem.1c01571