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A High-Affinity Cu-64-Labeled Ligand for PET Imaging of Hepsin: Design, Synthesis, and Characterizationopen access

Authors
Park, Ji-HunZhang, XuranHa, HyunsooKim, JungChoi, JoonLee, Kyung-HanByun, YoungjooChoe, Yearn
Issue Date
9월-2022
Publisher
MDPI
Keywords
hepsin; prostate cancer; Cu-64-DOTA-conjugated ligand; Leu-Arg dipeptide derivatives; diastereomers; PET
Citation
PHARMACEUTICALS, v.15, no.9
Indexed
SCIE
SCOPUS
Journal Title
PHARMACEUTICALS
Volume
15
Number
9
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/145772
DOI
10.3390/ph15091109
ISSN
1424-8247
Abstract
Hepsin, a cell surface serine protease, is a potential biomarker for the detection of prostate cancer due to its high expression in prostate cancer but not in normal prostate. This study aimed to develop a radioligand for positron emission tomography (PET) imaging of hepsin. Six leucine-arginine (Leu-Arg) dipeptide derivatives (two diastereomers for each of three ligands) were synthesized and evaluated for their binding affinities and selectivity for hepsin. Based on the binding assay, a Cu-nat-1,4,7,10-tetraazacyclododecane-N,N',N '' N'''-tetraacetic acid (DOTA)-conjugated ligand (3B) was selected for the development of a PET radioligand. [Cu-64]3B was synthesized by labeling the DOTA-conjugated compound 11B with [Cu-64]CuCl2 at 80 degrees C for 20 min. The radioligand was evaluated for prostate cancer cell binding and PET imaging in a prostate tumor mouse model. The results demonstrated that [Cu-64]3B exhibited high binding to LNCaP cells, intermediate binding to 22Rv1 cells, and low binding to PC3 cells. PET studies of [Cu-64]3B in mice, implanted with 22Rv1 and PC3 cells on each flank, revealed that the radioligand uptake was high and persistent in the 22Rv1 tumors over time, whereas it was low in PC3 tumors. The results of this study suggest that [Cu-64]3B is a promising PET radioligand for hepsin imaging.
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약학대학 (약학과)
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