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

Marcela Ávila-Sánchez, Guillermina Ferro-Flores, Nallely Jiménez-Mancilla, Blanca Ocampo-García, Gerardo Bravo-Villegas, Myrna Luna-Gutiérrez, Clara Santos-Cuevas, Erika Azorín-Vega, Liliana Aranda-Lara, Keila Isaac-Olivé, Laura Melendez-Alafort

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)21-32
Number of pages12
JournalJournal of Radioanalytical and Nuclear Chemistry
Volume324
Issue number1
DOIs
Publication statusPublished - Apr 1 2020

Keywords

  • Lu-CXCR4-L
  • Tc-CXCR4-L
  • Chemokine-4 receptor
  • DOTA-HYNIC-CXCR4-L
  • HYNIC-CXCR4-L
  • Theranostic pair

ASJC Scopus subject areas

  • Analytical Chemistry
  • Nuclear Energy and Engineering
  • Radiology Nuclear Medicine and imaging
  • Pollution
  • Spectroscopy
  • Public Health, Environmental and Occupational Health
  • Health, Toxicology and Mutagenesis

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