Positron-emission tomography molecular imaging of glia and myelin in drug discovery for multiple sclerosis

Matthews, Paul M; Datta, Gourab

doi:10.1517/17460441.2015.1032240

Cited by 28Medical Imaging Techniques and ApplicationsMultiple Sclerosis Research StudiesNeuroinflammation and Neurodegeneration Mechanisms

Positron-emission tomography molecular imaging of glia and myelin in drug discovery for multiple sclerosis

Matthews, Paul M, Datta, Gourab·2015·Expert Opinion on Drug Discovery

DOI 10.1517/17460441.2015.1032240

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Abstract

Introduction Therapies acting on glial cells are being explored for new drug development for multiple sclerosis. Molecular imaging using positron-emission tomography (PET) could address relevant questions in early phase clinical trials. Areas covered In this article, the authors critically review human PET methods that can be applied in specialised centres for imaging activated microglia and astrocytes and myelin. Expert opinion Strengths of PET lie in the molecular selectivity, sensitivity and potential for absolute quantitation. Even now, translocator protein PET radioligands could be used in exploratory studies for interventions targeting brain microglial activation. The clinical and neuropathological meaningfulness of signal from PET radioligands reporting on astrocyte activation through cellular expression of either monoamine oxidase B or the I2-imidazoline receptor or metabolism of [(11)C]acetate can now explored. [(11)C] N-methyl-4,4'-diaminostilbene, a PET marker for myelin, could soon enter first human trials. However, use of any of these PET glial markers demands a well-focused hypothesis and a commitment to validation in the context of use. Enhanced access to these radioligands, standardisation of analyses and lowering the costs of using them are needed if their full promise is to be realised.

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There has been very little data on which to base precise interpretations of TSPO to date.
“Surprisingly, there has been very little data on which to base precise interpretations to date (Matthews and Datta, 2015).”
From A quantitative neuropathological assessment of translocator protein expression in multiple sclerosis (2019) · cites this paper as Matthews and Datta, 2015

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Authors: Matthews, P. M., & Datta, G.
Affiliations: Imperial College London (GB)
ORCID: Matthews, Paul M
Venue: Expert Opinion on Drug Discovery
Publisher: Informa Healthcare
Published: 2015-04-05
Volume: 10
Issue: 5
Pages: 557-570
ISSN: 1746-0441 (ISSN-L)
1746-045X
DOI: 10.1517/17460441.2015.1032240
OpenAlex: W2168391482
Cited by: 28
References: 86
Citations by year: 2025: 1 · 2023: 2 · 2022: 1 · 2021: 3 · 2020: 2 · 2019: 1 · 2018: 1 · 2017: 8 · 2016: 6 · 2015: 3
FWCI: 0.95
Type: journal article
Language: en
Open access: closed
Locations: Expert Opinion on Drug Discovery (publishedVersion)
PubMed (publishedVersion)
Funders: GlaxoSmithKline
Wellcome Trust
National Institute for Health and Care Research (NF-SI-0514-10022)
Imperial College London
Imperial College Healthcare NHS Trust
Medical Research Council (MR/K501013/1)
NIHR Imperial Biomedical Research Centre
Topics: Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
Health Sciences › Medicine › Pathology and Forensic Medicine › Multiple Sclerosis Research Studies
Life Sciences › Neuroscience › Neurology › Neuroinflammation and Neurodegeneration Mechanisms
Keywords: multiple sclerosis, positron emission tomography, microglial activation, astrocyte activation, myelin imaging, monoamine oxidase B, 11C-acetate, drug discovery
MeSH terms: Animals, Astrocytes, Humans, Multiple Sclerosis, Myelin Sheath, Neuroglia, Drug Design, Microglia, Positron-Emission Tomography, Drug Discovery, Molecular Imaging

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Positron-emission tomography molecular imaging of glia and myelin in drug discovery for multiple sclerosis

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