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18F‑Alanine Derivative Serves as an ASCT2 Marker for Cancer Imaging
journal contribution
posted on 2018-01-08, 00:00 authored by Hui Liu, Yuxiang Han, Jiyuan Li, Ming Qin, Qunfeng Fu, Chunhong Wang, Zhibo LiuAmino
acids derivative are well established molecular probes for
diagnosis of a variety of cancer using positron emission tomography
(PET). Recently, boramino acid (BAAs) was found as a prospective molecular
platform for developing PET tracer. The objective of this study was
to develop a 18F-labeled alanine derivative through displacing
its carboxylate by trifluoroborate as a selective ASCT2 marker for
cancer imaging. 18F-Ala-BF3 was first evaluated
in healthy FVB/N mice in vivo, exhibiting rapid renal
clearance with almost negligible uptake in stomach (1.53 ± 0.31%ID/g).
Notable uptake was observed in thyroid (3.71 ± 0.49%ID/g, 40
min post injection), of which the uptake was significantly inhibited
by co-injection with natural L-alanine. In addition, we further established 18F-Ala-BF3 on a human gastric cancer cell (BGC-823)
xenografts bearing mouse model. Dynamic PET-CT scan revealed the optimal
time window for tumor imaging, it was between 40 and 60 min post injection,
when the BGC-823 xenografts uptake was 5.49 ± 1.47%ID/g (n = 4), and the tumor-to-stomach, tumor-to-blood, tumor-to-muscle,
and tumor-to-brain ratios were 3.27 ± 1.53, 3.80 ± 1.48,
3.47 ± 1.48, and 6.20 ± 1.47, respectively.