Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
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Published version
Author(s)
Type
Journal Article
Abstract
Promoting a senescent phenotype to supress tumour progression may present an alternative strategy for treating cancer
and encourages the development of positron emission tomography (PET) imaging biomarkers for assessing response to
treatment. The accumulation of lipofuscin deposits in senescent cells are visualised using the pathology stain Sudan Black B
(SBB) and is an emerging biomarker of senescence. We describe the design, synthesis and evaluation of
[18F]fluoroethyltriazole-SBB ([18F]FET-SBB), a fluorine-18 radiolabelled derivative of SBB. The in vitro uptake of [18F]FET-SBB
in a senescent cell line corelated with lipofuscin deposits; in vivo PET imaging and metabolite analysis confirms a favourable
pharmacokinetic and metabolic profile for futher studies of in vivo models of senescence.
and encourages the development of positron emission tomography (PET) imaging biomarkers for assessing response to
treatment. The accumulation of lipofuscin deposits in senescent cells are visualised using the pathology stain Sudan Black B
(SBB) and is an emerging biomarker of senescence. We describe the design, synthesis and evaluation of
[18F]fluoroethyltriazole-SBB ([18F]FET-SBB), a fluorine-18 radiolabelled derivative of SBB. The in vitro uptake of [18F]FET-SBB
in a senescent cell line corelated with lipofuscin deposits; in vivo PET imaging and metabolite analysis confirms a favourable
pharmacokinetic and metabolic profile for futher studies of in vivo models of senescence.
Date Issued
2022-09-15
Date Acceptance
2022-09-06
Citation
RSC Advances: an international journal to further the chemical sciences, 2022, 12 (40), pp.26372-26381
ISSN
2046-2069
Publisher
Royal Society of Chemistry
Start Page
26372
End Page
26381
Journal / Book Title
RSC Advances: an international journal to further the chemical sciences
Volume
12
Issue
40
Copyright Statement
© 2022 The Author(s). Published by the Royal Society of Chemistry. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
License URL
Sponsor
Imperial College Healthcare NHS Trust- BRC Funding
Identifier
https://pubs.rsc.org/en/content/articlelanding/2022/RA/D2RA04535D
Grant Number
RDC04
Subjects
Science & Technology
Physical Sciences
Chemistry, Multidisciplinary
Chemistry
SMALL-MOLECULE INHIBITOR
AURORA-A
BIOMARKER
MLN8054
03 Chemical Sciences
Publication Status
Published
Date Publish Online
2022-09-15