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

• DOI: 10.1007/s10967-020-07043-6
• Publication Date: 2020-02-06T21:05:01Z
• Authors: Marcela Ávila-Sán...; Guillermina Ferro...; Nallely Jiménez-M...; Blanca Ocampo-García; Gerardo Bravo-Vil...; Myrna Luna-Gutiérrez; Clara Santos-Cuevas; Erika Azorín-Vega; Liliana Aranda-Lara; Keila Isaac-Olivé; Laura Melendez-Al...
• Keywords: 03 medical and health sciences; 0302 clinical medicine; 01 natural sciences; 3. Good health; 0104 chemical sciences

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 ( 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.