64Cu-Labeled Ubiquitin for PET Imaging
of CXCR4 Expression in Mouse Breast Tumor
Posted on 2019-07-22 - 12:36
Ubiquitin has been recently identified
as a chemokine receptor
4 (CXCR4) natural ligand, offering great potential for positron emission
computed tomography (PET) imaging of CXCR4 expression. This study
reports the preparation and evaluation of (64Cu)-radiolabeled
ubiquitin for CXCR4 imaging. The ubiquitin was first fused with a
C-terminal GGCGG sequence, and the resulting recombinant ubiquitin
derivative UbCG4 was then functionalized with the trans-cyclooctene (TCO) moiety via thiol–maleimide click reaction,
followed by 64Cu-radiolabeling through the TCO/Tz (tetrazine)-based
Diels–Alder click reaction. In the prepared in vitro studies,
the prepared (64Cu)-UbCG4 showed significantly higher specific
uptakes in the 4T1 breast cancer cells compared with the uptakes in
the CXCR4-knockdown 4T1 cells. In the in vivo evaluation in the 4T1-xenograft
mouse model, (64Cu)-UbCG4 demonstrated a similar tumor
uptake but much lower backgrounds compared with 64Cu-labeled
AMD3465. These results suggested that (64Cu)-UbCG4 could
serve as a potent PET tracer for the noninvasive imaging of CXCR4
expression in tumors.
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Li, Huiqiang; Zhang, Xiaohui; Wu, Hsuan Yi; Sun, Lingyi; Ma, Yongyong; Xu, Junling; et al. (2019). 64Cu-Labeled Ubiquitin for PET Imaging
of CXCR4 Expression in Mouse Breast Tumor. ACS Publications. Collection. https://doi.org/10.1021/acsomega.9b00678
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AUTHORS (8)
HL
Huiqiang Li
XZ
Xiaohui Zhang
HW
Hsuan Yi Wu
LS
Lingyi Sun
YM
Yongyong Ma
JX
Junling Xu
QL
Qing Lin
DZ
Dexing Zeng
KEYWORDS
vivo evaluation4 T 1-xenograft mouse modelpositron emissionstudy reportstumor uptakePET ImagingTCOC-terminal GGCGG sequenceMouse Breast Tumor UbiquitinPET tracernoninvasive imagingCXCR 4 imaging64 Cu-radiolabelingCXCR 4-knockdown 4 T 1 cellschemokine receptor 44 T 1 breast cancer cellsubiquitinCXCR 4 Expression64 Cu-Labeled UbiquitinUbCG 464 Cu-labeled AMD 3465.CXCR 4 expression