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

Promoting a senescent phenotype to suppress 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 cel...

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Autores principales: Brickute, Diana, Chen, Cen, Braga, Marta, Barnes, Chris, Wang, Ning, Allott, Louis, Aboagye, Eric O.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9475417/
https://www.ncbi.nlm.nih.gov/pubmed/36275107
http://dx.doi.org/10.1039/d2ra04535d
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author Brickute, Diana
Chen, Cen
Braga, Marta
Barnes, Chris
Wang, Ning
Allott, Louis
Aboagye, Eric O.
author_facet Brickute, Diana
Chen, Cen
Braga, Marta
Barnes, Chris
Wang, Ning
Allott, Louis
Aboagye, Eric O.
author_sort Brickute, Diana
collection PubMed
description Promoting a senescent phenotype to suppress 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 is visualised using the pathology stain Sudan Black B (SBB) which is an emerging biomarker of senescence. We describe the design, synthesis and evaluation of [(18)F]fluoroethyltriazole-SBB ([(18)F]FET-SBB), a fluorine-18 radiolabelled derivative of SBB. The in vitro uptake of [(18)F]FET-SBB in a senescent cell line corelated with lipofuscin deposits; in vivo PET imaging and metabolite analysis confirm a favourable pharmacokinetic and metabolic profile for further studies of in vivo models of senescence.
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spelling pubmed-94754172022-10-20 Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells Brickute, Diana Chen, Cen Braga, Marta Barnes, Chris Wang, Ning Allott, Louis Aboagye, Eric O. RSC Adv Chemistry Promoting a senescent phenotype to suppress 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 is visualised using the pathology stain Sudan Black B (SBB) which is an emerging biomarker of senescence. We describe the design, synthesis and evaluation of [(18)F]fluoroethyltriazole-SBB ([(18)F]FET-SBB), a fluorine-18 radiolabelled derivative of SBB. The in vitro uptake of [(18)F]FET-SBB in a senescent cell line corelated with lipofuscin deposits; in vivo PET imaging and metabolite analysis confirm a favourable pharmacokinetic and metabolic profile for further studies of in vivo models of senescence. The Royal Society of Chemistry 2022-09-15 /pmc/articles/PMC9475417/ /pubmed/36275107 http://dx.doi.org/10.1039/d2ra04535d Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by/3.0/
spellingShingle Chemistry
Brickute, Diana
Chen, Cen
Braga, Marta
Barnes, Chris
Wang, Ning
Allott, Louis
Aboagye, Eric O.
Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
title Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
title_full Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
title_fullStr Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
title_full_unstemmed Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
title_short Design, synthesis, and evaluation of a novel PET imaging agent targeting lipofuscin in senescent cells
title_sort design, synthesis, and evaluation of a novel pet imaging agent targeting lipofuscin in senescent cells
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9475417/
https://www.ncbi.nlm.nih.gov/pubmed/36275107
http://dx.doi.org/10.1039/d2ra04535d
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