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Mol Imaging Biol. 2014 Jun;16(3):412-20. doi: 10.1007/s11307-013-0711-2. Epub 2013 Dec 5.

Imaging tumour ATB0,+ transport activity by PET with the cationic amino acid O-2((2-[18F]fluoroethyl)methyl-amino)ethyltyrosine.

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1
Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Institute of Pharmaceutical Sciences, ETH Zurich, Wolfgang-Pauli-Strasse 10, 8093, Zurich, Switzerland.

Abstract

PURPOSE:

The concentrative amino acid transporter ATB(0,+) (SLC6A14) is under evaluation as a target for anticancer therapy. An ATB(0,+)-selective positron emission tomography (PET) probe could advance preclinical drug development. We characterised the cationic tyrosine analogue O-2((2-[(18)F]fluoroethyl)methyl-amino)ethyltyrosine ([(18)F]FEMAET) as a PET probe for ATB(0,+) activity.

PROCEDURES:

Cell uptake was studied in vitro. ATB(0,+) expression was quantified by real-time PCR. [(18)F]FEMAET accumulation in xenografts was investigated by small animal PET with mice.

RESULTS:

[(18)F]FEMAET accumulated in PC-3 and NCI-H69 cancer cells in vitro. As expected for ATB(0,+) transport, uptake was inhibited by LAT/ATB(0,+) inhibitors and dibasic amino acids, and [(18)F]FEMAET efflux was only moderately stimulated by extracellular amino acids. ATB(0,+) was expressed in PC-3 and NCI-H69 but not MDA-MB-231 xenografts. PET revealed accumulation in PC-3 and NCI-H69 xenografts and significant reduction by ATB(0,+) inhibition. Uptake was negligible in MDA-MB-231 xenografts.

CONCLUSION:

ATB(0,+) activity can be imaged in vivo by PET with [(18)F]FEMAET.

PMID:
24307544
DOI:
10.1007/s11307-013-0711-2
[Indexed for MEDLINE]
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