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Merck
  • ⁹⁹mTc-labeled single-domain antibody EG2 in targeting epidermal growth factor receptor: an in-vitro and mouse model in-vivo study.

⁹⁹mTc-labeled single-domain antibody EG2 in targeting epidermal growth factor receptor: an in-vitro and mouse model in-vivo study.

Nuclear medicine communications (2015-01-16)
Chongjiao Li, Bing Wen, Lifei Wang, Hongyan Feng, Xiaotian Xia, Zhiling Ding, Bin Gao, Yongxue Zhang, Xiaoli Lan
摘要

The aim of this study was to explore the targeting ability and metabolic characteristics of the technetium-99m-labeled single-domain antibody (⁹⁹mTc-sdAb) EG2 targeting epidermal growth factor receptor (EGFR) through an in-vitro and in-vivo study. The sdAb EG2 was radiolabeled with Tc using a tricarbonyl kit. The EGFR expression level of A431 and OCM-1 cells was confirmed using immunofluorescence staining. Cell binding, blocking, uptake, and efflux studies were performed to investigate the binding specificity of ⁹⁹mTc-sdAb EG2 in vitro. Single-photon emission computed tomography imaging and biodistribution studies were used to explore the targeting abilities and metabolic characteristics of Tc-sdAb EG2 in vivo. ⁹⁹mTc-sdAb EG2 was successfully prepared with labeling yields of 60-71% and specific activity of 1.83±0.29 GBq/mg (n=3). Immunofluorescence staining revealed high and low EGFR expression on the surface of A431 and OCM-1 cells, respectively. The binding affinity of ⁹⁹mTc-sdAb EG2 to A431 cells was 43.53±1.89 nmol/l. ⁹⁹mTc-sdAb EG2 uptake in A431 cells in vitro could be blocked by ∼19, 40, and 66% in the presence of excess unlabeled sdAb EG2 at 100, 500, and 1000 nmol/l, respectively. Single-photon emission computed imaging indicated that A431 tumor images could be clearly displayed at early scan time points after ⁹⁹mTc-sdAb EG2 injection, even as early as 1 h. Biodistribution study showed that the A431 tumor uptake of ⁹⁹mTc-sdAb EG2 was blocked by about 51% at 3 h after coinjecting excess of sdAb EG2. However, there were almost no OCM-1 tumor images at the corresponding scan time points and the OCM-1 tumor uptake was only 0.40±0.13% injected dose per gram of tissue (n=5) at 3 h. This study demonstrated that sdAb EG2 can effectively target EGFR in vitro and in vivo in tumors, suggesting that it could be used as a molecular probe for EGFR detection.

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