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99mTc‐labeled rHuEpo for imaging of the erythropoietin receptor in tumors
Authors:Xiaoqing Zhuang  Dan Zhao  Pengfei Yang  Yingqin Jia  Rui Liang  Qian Zhao  Chunlei Han  Joseph M. Kinsella  Ruilong Sheng  Juan Li
Affiliation:1. General Hospital of Ningxia Medical University, Yinchuan, China;2. Turku PET Centre, Turku University Hospital and University of Turku, Turku, Finland;3. Department of Bioengineering, McGill University, Quebec, Canada;4. CAS Key Laboratory for Organic Functional Materials, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, China;5. CQM‐Centrode Quimica da Madeira, Universidade da Madeira, Funchal, Madeira, Portugal
Abstract:To analyze erythropoietin receptor (EpoR) status in tumors, recombinant human erythropoietin (rHuEpo) was labeled with 99mTc by 99mTc‐centered 1‐pot synthesis, resulting in high radiochemical purity, stability, and biological activity. Both in vitro cell culture experiments and biodistribution studies of normal rats demonstrated successful EpoR targeting. The biodistribution of labeled rHuEpo in a NCI‐H1975 xenograft model showed tumor accumulation (tumor‐to‐muscle ratio, 4.27 ± 1.77), confirming the expression of active EpoR in tumors. Thus, as a novel single positron emission computerized tomography tracer for the imaging of EpoR expression in vivo, 99mTc‐rHuEpo is effective for exploring the role of EpoR in cancer growth, metastasis and angiogenesis.
Keywords:99mTc  erythropoietin receptor  molecular imaging  radiotracer  rHuEpo
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