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Comparative cell uptake study of FITC-/177Lu-labeled RM26 monomer, dimer and trimer on PC-3: improving binding affinity of gastrin releasing peptide receptor (GRPR) antagonist via bivalency/trivalency

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Abstract

The gastrin releasing peptide receptors (GRPRs) overexpress in various tumors, which provided the opportunity for GRPR targeted tumor radiological diagnosis and therapy. In recent reports, the GPPR antagonists presented superior specific targeting affinity over the agonists. However, antagonists suffer from many shortcomings regarding their binding affinity and biodistribution properties. In this study, we designed the dimer/trimer antagonists to address the radiotherapy requirements. The results showed both of dimer and trimer RM26 derivatives appeared a progressive improvement. This study provided an efficient strategy to improve the tumor accumulation properties for the GRPR antagonist analogs.

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Acknowledgements

This work was funded from the National Natural Science Foundation of China (Grant Nos. 21502178 and 21701155).

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Authors and Affiliations

  1. Institute of Nuclear Physics and Chemistry (INPC), China Academy of Engineering Physics (CAEP), Mianyang, 621999, People’s Republic of China

    Liangang Zhuo, Xia Yang, Wei Liao, Jing Wang, Hailin Wang, Guanquan Wang, Hu Song, Hongyuan Wei, Yuchuan Yang & Peng Zhao

  2. Department of Nuclear Medicine, The Affiliated Hospital Southwest of Medical University, Luzhou, 646000, People’s Republic of China

    Minli Lv, Yue Feng & Yue Chen

  3. Collaborative Innovation Center of Radiation Medicine of Jiangsu, Higher Education Institutions, Suzhou, 215123, People’s Republic of China

    Liangang Zhuo, Xia Yang, Hongyuan Wei, Yuchuan Yang & Peng Zhao

  4. Key Laboratory of Nuclear Medicine and Molecular Imaging of Sichuan Province, Mianyang, 621999, People’s Republic of China

    Liangang Zhuo, Xia Yang, Wei Liao, Jing Wang, Minli Lv, Guanquan Wang, Hu Song, Yue Feng, Yue Chen, Hongyuan Wei, Yuchuan Yang & Peng Zhao

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  1. Liangang Zhuo
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  2. Xia Yang
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Zhuo, L., Yang, X., Liao, W. et al. Comparative cell uptake study of FITC-/177Lu-labeled RM26 monomer, dimer and trimer on PC-3: improving binding affinity of gastrin releasing peptide receptor (GRPR) antagonist via bivalency/trivalency. J Radioanal Nucl Chem 319, 881–889 (2019). https://doi.org/10.1007/s10967-018-6396-x

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