Dataset Information

(99m)Tc-3P-RGD2 micro-single-photon emission computed tomography/computed tomography provides a rational basis for integrin ?v?3-targeted therapy.

ABSTRACT:

Purpose

This study was to demonstrate the utility of (99m)Tc-3P-RGD2 micro-single-photon emission computed tomography/computed tomography (SPECT/CT) for the integrin ?v?3 expression quantification in NCI-H446 and A549 lung cancer xenografts.

Materials and methods

(99m)Tc-3P-RGD2 was prepared with high radiochemical purity (97%±2%) and showing high in vitro stability. The in vitro affinities of (99m)Tc-3P-RGD2 to NCI-H446 and A549 tumor cells were analyzed with ?-counter, while the in vivo uptakes in NCI-H446 and A549 xenografts were evaluated with micro-SPECT/CT. The region of interest was drawn over the tumor site and contralateral muscle on the SPECT/CT image, and the tumor to nontumor (T/NT) ratio was calculated to estimate ?v?3 expression and tumor uptake. The expressions of integrin ?v?3 in vitro and in vivo were analyzed using a flow cytometer and immunofluorescence.

Results

Micro-SPECT/CT demonstrated focal uptake in the tumors. T/NT ratio in NCI-H446 xenografts was significantly higher compared with the A549 tumor model, as 5.92±0.82 and 3.62±0.91, respectively, with p<0.05. In addition, integrin ?v?3 expression in NCI-H446 cells was significantly higher compared with the A549 cells, which was consistent with the imaging data. A linear relationship was observed between (99m)Tc-3P-RGD2 uptake and ?v?3 expression (R(2)=0.7667, p<0.001).

Conclusion

(99m)Tc-3P-RGD2 SPECT/CT could be used to quantify integrin ?v?3 expression within tumors, providing a rational basis for integrin ?v?3-targeted cancer therapy.

SUBMITTER: Fu T

PROVIDER: S-EPMC4224041 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature

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Publications

(99m)Tc-3P-RGD2 micro-single-photon emission computed tomography/computed tomography provides a rational basis for integrin αvβ3-targeted therapy.

Fu Tong T Qu Wei W Qiu Fan F Li Yan Y Shao Guoqiang G Tian Wei W Hua Zichun Z Zhang Yingjian Y Wang Feng F

Cancer biotherapy & radiopharmaceuticals 20141006 9

<h4>Purpose</h4>This study was to demonstrate the utility of (99m)Tc-3P-RGD2 micro-single-photon emission computed tomography/computed tomography (SPECT/CT) for the integrin αvβ3 expression quantification in NCI-H446 and A549 lung cancer xenografts.<h4>Materials and methods</h4>(99m)Tc-3P-RGD2 was prepared with high radiochemical purity (97%±2%) and showing high in vitro stability. The in vitro affinities of (99m)Tc-3P-RGD2 to NCI-H446 and A549 tumor cells were analyzed with γ-counter, while the ...[more]

PMID: 25286251

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