Evidence map›Paper›PMID 34905377›Full record

ReviewJournal of medicinal chemistry2021

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

Zhen Chen, Achi Haider, Jiahui Chen, Zhiwei Xiao, Luca Gobbi, Michael Honer, Uwe Grether, Steven E Arnold, Lee Josephson, Steven H Liang

Abstract readReview
In one paragraph

Review in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.

0numbers the graph read from it
0cells of the map it votes in
31citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

31 citing papers in PubMed.

  1. Article
  2. Comparison of [Molecular imaging and biology · 2026
    Article
  3. Review
  4. Review
  5. Review
  6. Review
  7. Review
  8. Article
  9. Article
  10. Multi-tracer PET and MR imaging visualize distinct metabolic and inflammatory profiles in the white matter of NMOSD and MOGAD.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2025
    Article
  11. Article
  12. Designing a Small Molecule for PET Radiotracing: [Molecules (Basel, Switzerland) · 2025
    Review
  13. The Development of Inhibitors for NLRP3 Inflammasome.ACS medicinal chemistry letters · 2025
    Article
  14. Review
  15. Article
  16. CD45-targeted PET enables the visualization of inflammatory conditions.American journal of nuclear medicine and molecular imaging · 2025
    Article
  17. Review
  18. Article
  19. Review
  20. Automated radiosynthesis of [Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine · 2024
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Zhen ChenDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston 02114, Massachusetts, United States.ORCID 0000-0002-6289-4332
Achi HaiderDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston 02114, Massachusetts, United States.
Jiahui ChenDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston 02114, Massachusetts, United States.
Zhiwei XiaoDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston 02114, Massachusetts, United States.
Luca GobbiPharma Research and Early Development, F. Hoffmann-La Roche Ltd, Basel CH-4070, Switzerland.ORCID 0000-0002-0563-2491
Michael HonerPharma Research and Early Development, F. Hoffmann-La Roche Ltd, Basel CH-4070, Switzerland.
Uwe GretherPharma Research and Early Development, F. Hoffmann-La Roche Ltd, Basel CH-4070, Switzerland.
Steven E ArnoldDepartment of Neurology and the Massachusetts Alzheimer's Disease Research Center, Massachusetts General Hospital, Harvard Medical School, 114 16th Street, Charlestown 02129, Massachusetts, United States.
Lee JosephsonDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston 02114, Massachusetts, United States.
Steven H LiangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston 02114, Massachusetts, United States.ORCID 0000-0003-1413-6315

Funding

Supplement for Ligand discovery for delineating cholesterol homeostasis in the brainR01AG070060 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2021 to 2025
$4.2M
In vivo Probe for ionotropic glutamate signaling system: AMPA receptorsR01MH120197 · NIMH · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2021
$2.4M
AMPAR ligand discovery for Alzheimer's diseaseRF1AG073428 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2021 to 2021
$2.3M
PET ligand development for mGlu2 based on negative allosteric modulatorsR01MH117125 · NIMH · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2018 to 2020
$1.6M
AMPAR ligand discovery for Alzheimer's diseaseR01AG073428 · NIA · EMORY UNIVERSITY · PI LIANG, STEVEN H · 2024 to 2025
$1.5M
New PET tracers for neuroimaging of FAAH in endocannabinoid signalingK01DA038000 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2014 to 2018
$927k
Novel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR33DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2021
$851k
MAGL PET tracer-guided prognosis and neuroprotective therapy for Alzheimer's diseaseR03AG063290 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2020
$495k
PET Imaging for neuroinflammation in Alzheimer's diseaseR21AG074218 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2021 to 2022
$442k
Novel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR21DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2017 to 2018
$425k
NIA NIH HHS R01 AG070060NIA NIH HHS R01 AG073428NIA NIH HHS R03 AG063290NIA NIH HHS R21 AG074218NIA NIH HHS RF1 AG073428NIDA NIH HHS K01 DA038000NIDA NIH HHS R21 DA043507NIDA NIH HHS R33 DA043507NIMH NIH HHS R01 MH117125NIMH NIH HHS R01 MH120197
6 · The paper itself

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.

Indexed as

AnimalsHumansNeuroinflammatory DiseasesPositron-Emission TomographyRadiopharmaceuticalsReceptors, GABASmall Molecule LibrariesRadiopharmaceuticalsReceptors, GABASmall Molecule LibrariesTSPO protein, human

Identifiers

PMID34905377
PMCPMC9094091

What Socratic holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.