TY - JOUR
T1 - Synthesis and preclinical evaluation of the 99mTc-/177Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting
AU - Ávila-Sánchez, Marcela
AU - Ferro-Flores, Guillermina
AU - Jiménez-Mancilla, Nallely
AU - Ocampo-García, Blanca
AU - Bravo-Villegas, Gerardo
AU - Luna-Gutiérrez, Myrna
AU - Santos-Cuevas, Clara
AU - Azorín-Vega, Erika
AU - Aranda-Lara, Liliana
AU - Isaac-Olivé, Keila
AU - Melendez-Alafort, Laura
N1 - Funding Information:
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’’.
Publisher Copyright:
© 2020, Akadémiai Kiadó, Budapest, Hungary.
Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.
PY - 2020/4/1
Y1 - 2020/4/1
N2 - 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.
AB - 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.
KW - Lu-CXCR4-L
KW - Tc-CXCR4-L
KW - Chemokine-4 receptor
KW - DOTA-HYNIC-CXCR4-L
KW - HYNIC-CXCR4-L
KW - Theranostic pair
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U2 - 10.1007/s10967-020-07043-6
DO - 10.1007/s10967-020-07043-6
M3 - Article
AN - SCOPUS:85078986547
VL - 324
SP - 21
EP - 32
JO - Journal of Radioanalytical Chemistry
JF - Journal of Radioanalytical Chemistry
SN - 0022-4081
IS - 1
ER -