Imperial College London
Alternate

ProfessorEricAboagye

Faculty of Medicine, Department of Surgery & Cancer

Professor
 
 
 
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Contact

 

+44 (0)20 3313 3759eric.aboagye

 
 
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Assistant

 

Mrs Maureen Francis +44 (0)20 7594 2793

 
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Location

 

GN1Commonwealth BuildingHammersmith Campus

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Summary

 

Publications

Citation

BibTex format

@article{Glaser:2019:10.1038/s41598-019-55992-0,
author = {Glaser, M and Rajkumar, V and Diocou, S and Gendron, T and Yan, R and Sin, PKB and Sander, K and Carroll, L and Pedley, RB and Aboagye, EO and Witney, TH and Arstad, E},
doi = {10.1038/s41598-019-55992-0},
journal = {Scientific Reports},
title = {One-pot radiosynthesis and biological evaluation of a caspase-3 selective 5-[(123,)(125) I]iodo-1,2,3-triazole derived satin SPECT tracer},
url = {http://dx.doi.org/10.1038/s41598-019-55992-0},
volume = {9},
year = {2019}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Induction of apoptosis is often necessary for successful cancer therapy, and the non-invasive monitoring of apoptosis post-therapy could assist in clinical decision making. Isatins are a class of compounds that target activated caspase-3 during apoptosis. Here we report the synthesis of the 5-iodo-1,2,3-triazole (FITI) analog of the PET tracer [18F]ICMT11 as a candidate tracer for imaging of apoptosis with SPECT, as well as PET. Labelling with radioiodine (123,125I) was achieved in 55 ± 12% radiochemical yield through a chelator-accelerated one-pot cycloaddition reaction mediated by copper(I) catalysis. The caspase-3 binding affinity and selectivity of FITI compares favourably to that of [18F]ICMT11 (Ki = 6.1 ± 0.9 nM and 12.4 ± 4.7 nM, respectively). In biodistribution studies, etoposide-induced cell death in a SW1222 xenograft model resulted in a 2-fold increase in tumour uptake of the tracer. However, the tumour uptake was too low to allow in vivo imaging of apoptosis with SPECT.
AU  - Glaser,M
AU  - Rajkumar,V
AU  - Diocou,S
AU  - Gendron,T
AU  - Yan,R
AU  - Sin,PKB
AU  - Sander,K
AU  - Carroll,L
AU  - Pedley,RB
AU  - Aboagye,EO
AU  - Witney,TH
AU  - Arstad,E
DO  - 10.1038/s41598-019-55992-0
PY  - 2019///
SN  - 2045-2322
TI  - One-pot radiosynthesis and biological evaluation of a caspase-3 selective 5-[(123,)(125) I]iodo-1,2,3-triazole derived satin SPECT tracer
T2  - Scientific Reports
UR  - http://dx.doi.org/10.1038/s41598-019-55992-0
UR  - http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000503210100005&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
UR  - http://hdl.handle.net/10044/1/76256
VL  - 9
ER  -
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