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- Title
In vitro and in vivo evaluation of the caspase-3 substrate-based radiotracer [(18)F]-CP18 for PET imaging of apoptosis in tumors.
- Authors
Xia, Chun-Fang; Chen, Gang; Gangadharmath, Umesh; Gomez, Luis F; Liang, Qianwa; Mu, Fanrong; Mocharla, Vani P; Su, Helen; Szardenings, A Katrin; Walsh, Joseph C; Zhao, Tieming; Kolb, Hartmuth C
- Abstract
<bold>Purpose: </bold>A novel caspase-3 substrate-based probe [(18)F]-CP18 was evaluated as an in vivo positron emission tomography (PET) imaging agent for monitoring apoptosis in tumors.<bold>Methods: </bold>Uptake of [(18)F]-CP18 in cell assays and tumors was measured. Caspase-3/7 activities in cell lysates and tumor homogenates were determined. Autoradiography,Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL), and cleaved caspase-3 immunostaining were performed on adjacent tumor sections to identify areas of apoptosis.<bold>Results: </bold>The in vitro cell assays showed caspase-3-dependent uptake of [(18)F]-CP18 in tumor cells when treated with an apoptosis inducer. The in vivo microPET imaging signal of [(18)F]-CP18 in xenograft tumors correlated with the ex vivo caspase-3/7 activities in these tumors. Furthermore, tumor autoradiographies of [(18)F]-CP18 in tumor sections matched adjacent sections stained by TUNEL and caspase-3 immunohistochemistry (IHC).<bold>Conclusions: </bold>[(18)F]-CP18 demonstrated high affinity and selectivity for activated caspase-3 both in vitro and in vivo, and the results support [(18)F]-CP18 as a promising new PET imaging agent for apoptosis.
- Publication
Molecular Imaging & Biology, 2013, Vol 15, Issue 6, p748
- ISSN
1536-1632
- Publication type
journal article
- DOI
10.1007/s11307-013-0646-7