Imperial College London
Alternate

DrPhilipMiller

Faculty of Natural Sciences, Department of Chemistry

Reader in Applied Synthesis
 
 
 
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Contact

 

philip.miller Website

 
 
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Location

 

501kMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Merchant:2016:10.1039/c6ra07404a,
author = {Merchant, S and Allott, L and Carroll, L and Tittrea, V and Kealey, S and Witney, TH and Miller, PW and Smith, G and Aboagye, EO},
doi = {10.1039/c6ra07404a},
journal = {RSC Advances},
pages = {57569--57579},
title = {Synthesis and pre-clinical evaluation of a [<sup>18</sup>F]fluoromethyl-tanaproget derivative for imaging of progesterone receptor expression},
url = {http://dx.doi.org/10.1039/c6ra07404a},
volume = {6},
year = {2016}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - The estrogen receptor (ER) and progesterone receptor (PR) are over-expressed in ∼50% of breast cancer lesions, and used as biomarkers to stratify patients for endocrine therapy. Currently, immunohistochemical (IHC) assessment of these lesions from a core-needle biopsy in deep-sited metastases has limitations associated with sampling error and lack of standardization. An alternative solution is positron emission tomography (PET)-based probes, which are inherently quantitative and capable of imaging the entire tumor, including metastases. This work features the synthesis and biological evaluation of a novel fluorinated derivative of tanaproget, a high affinity non-steroidal PR ligand, as a candidate for imaging PR expression in vivo. Radiolabeling of the candidate was achieved in a 15% ± 4 radiochemical yield (non-decay corrected) in one step from [18F]fluoromethyltosylate in 30 min. Cell uptake studies showed a significant difference between the radioligand uptake in PR+ and PR- cell lines; however, in vivo imaging was confounded by defluorination hypothesized to occur via iminium salt formation. Investigation into high affinity, metabolically stable non-steroidal PR ligands is currently ongoing.
AU  - Merchant,S
AU  - Allott,L
AU  - Carroll,L
AU  - Tittrea,V
AU  - Kealey,S
AU  - Witney,TH
AU  - Miller,PW
AU  - Smith,G
AU  - Aboagye,EO
DO  - 10.1039/c6ra07404a
EP  - 57579
PY  - 2016///
SN  - 2046-2069
SP  - 57569
TI  - Synthesis and pre-clinical evaluation of a [<sup>18</sup>F]fluoromethyl-tanaproget derivative for imaging of progesterone receptor expression
T2  - RSC Advances
UR  - http://dx.doi.org/10.1039/c6ra07404a
UR  - http://hdl.handle.net/10044/1/38740
VL  - 6
ER  -
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