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Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells

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Title: Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
Authors: Aboagye, E
Brickute, D
Allott, L
Wang, N
Barnes, C
Costa-Braga, M
Chen, C
Item 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.
Issue Date: 15-Sep-2022
Date of Acceptance: 6-Sep-2022
URI: http://hdl.handle.net/10044/1/99630
DOI: 10.1039/D2RA04535D
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.
Sponsor/Funder: Imperial College Healthcare NHS Trust- BRC Funding
Funder's Grant Number: RDC04
Keywords: Science & Technology
Physical Sciences
Chemistry, Multidisciplinary
Chemistry
SMALL-MOLECULE INHIBITOR
AURORA-A
BIOMARKER
MLN8054
03 Chemical Sciences
Publication Status: Published
Online Publication Date: 2022-09-15
Appears in Collections:Department of Surgery and Cancer
Faculty of Medicine



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