The Radiolabeling of a Gly-Sar Dipeptide Derivative with Flourine-18 and Its Use as a Potential Peptide Transporter PET Imaging Agent

We have developed a novel fluorine-18 radiotracer, dipeptide , radiolabeled in two steps from mesylate . The initial radiolabeling is achieved in a short reaction time (10 min) and purified through solid-phase extraction (SPE) with modest radiochemical yields (rcy = 10 ± 2%, = 5) in excellent radioc...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2020-02, Vol.25 (3), p.643
Main Authors: Molotkov, Andrei, Castrillon, John W, Santha, Sreevidya, Harris, Paul E, Leung, David K, Mintz, Akiva, Carberry, Patrick
Format: Article
Language:English
Subjects:
Advantages
Carbon
Computed tomography
Fluorides
Fluorine
Fluorine isotopes
fluorine-18
Gene expression
Hydrochloric acid
Kinases
Medical imaging
Pancreatic cancer
Pancreatic carcinoma
Peptide transporter
peptide transporters
Peptides
Positron emission
positron emission tomography
Radioactive tracers
Radiochemical analysis
radiotracer
Reaction time
Solid phases
Solvents
Tomography
Tumor cell lines
Tumors
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Summary:We have developed a novel fluorine-18 radiotracer, dipeptide , radiolabeled in two steps from mesylate . The initial radiolabeling is achieved in a short reaction time (10 min) and purified through solid-phase extraction (SPE) with modest radiochemical yields (rcy = 10 ± 2%, = 5) in excellent radiochemical purity (rcp > 99%, = 5). The de-protection of the -butyloxycarbonyl (Boc) and trityl group was achieved with mild heating under acidic conditions to provide F-tagged dipeptide . Preliminary analysis of F-dipeptide was performed to confirm uptake by peptide transporters (PepTs) in human pancreatic carcinoma cell lines Panc1, BxPC3, and ASpc1, which are reported to express the peptide transporter 1 (PepT1) . Furthermore, we confirmed in vivo uptake of F-dipeptide tracer using microPET/CT in mice harboring subcutaneous flank Panc1, BxPC3, and Aspc1 tumors. In conclusion, we have established the radiolabeling of dipeptide with fluoride-18, and demonstrated its potential as an imaging agent which may have clinical applications for the diagnosis of pancreatic carcinomas.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25030643