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Synthesis and preclinical evaluation of the 99mTc-/177Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting


This research aimed to prepare 99mTc-/177Lu-CXCR4-L radiotracers and evaluate their in vitro and in vivo capability to detect the chemokine-4 receptor. Molecular docking calculations, Kd values (< 10 nM) of 99mTc-/177Lu-CXCR4-L (radiochemical purities > 98.5%) estimated by saturation binding assays, as well as biodistribution studies in mice with induced tumors, confirmed the affinity of radiotracers towards CXCR4, expressed in DU-4475 breast cancer cells and C6 glioblastoma cells. Micro-SPECT/CT images showed that 99mTc-CXCR4-L and 177Lu-CXCR4-L could work as a theranostic pair for CXCR4 targets. Results warrant additional research to assess the therapeutic efficacy and dosimetry of 177Lu-CXCR4-L.

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This research received financial support from the Mexican National Council of Science and Technology (CONACyT-Mexico, Grant CB2017-2018-A1-S-36841). This work was performed as part of the activities of the ‘‘Laboratorio Nacional de Investigación y Desarrollo de Radiofármacos, CONACyT’’.

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Correspondence to Guillermina Ferro-Flores or Nallely Jiménez-Mancilla.

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The authors declare no potential conflicts of interest with regard to the research, authorship, and/or publication of this article.

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All applicable international, national and/or institutional guidelines for the care and use of animals were followed. This research was approved by the CICUAL-ININ Ethics Committee (Internal Committee of Care and Use of Laboratory Animals of the National Institute of Nuclear Research, Approval No. 02-2018).

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Ávila-Sánchez, M., Ferro-Flores, G., Jiménez-Mancilla, N. et al. Synthesis and preclinical evaluation of the 99mTc-/177Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting. J Radioanal Nucl Chem (2020).

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  • 99mTc-CXCR4-L
  • 177Lu-CXCR4-L
  • Chemokine-4 receptor
  • Theranostic pair