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

doi:10.1007/s10967-020-07043-6

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

Istituto Oncologico Veneto

Research output: Contribution to journal › Article › peer-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, K_d 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 language	English
Pages (from-to)	21-32
Number of pages	12
Journal	Journal of Radioanalytical and Nuclear Chemistry
Volume	324
Issue number	1
DOIs	https://doi.org/10.1007/s10967-020-07043-6
Publication status	Published - 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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Ávila-Sánchez, M., Ferro-Flores, G., Jiménez-Mancilla, N., Ocampo-García, B., Bravo-Villegas, G., Luna-Gutiérrez, M., Santos-Cuevas, C., Azorín-Vega, E., Aranda-Lara, L., Isaac-Olivé, K., & Melendez-Alafort, L. (2020). Synthesis and preclinical evaluation of the ^99mTc-/¹⁷⁷Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting. Journal of Radioanalytical and Nuclear Chemistry, 324(1), 21-32. https://doi.org/10.1007/s10967-020-07043-6

Synthesis and preclinical evaluation of the ^99mTc-/¹⁷⁷Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting. / Ávila-Sánchez, Marcela; Ferro-Flores, Guillermina; Jiménez-Mancilla, Nallely; Ocampo-García, Blanca; Bravo-Villegas, Gerardo; Luna-Gutiérrez, Myrna; Santos-Cuevas, Clara; Azorín-Vega, Erika; Aranda-Lara, Liliana; Isaac-Olivé, Keila; Melendez-Alafort, Laura.

In: Journal of Radioanalytical and Nuclear Chemistry, Vol. 324, No. 1, 01.04.2020, p. 21-32.

Research output: Contribution to journal › Article › peer-review

Ávila-Sánchez, M, Ferro-Flores, G, Jiménez-Mancilla, N, Ocampo-García, B, Bravo-Villegas, G, Luna-Gutiérrez, M, Santos-Cuevas, C, Azorín-Vega, E, Aranda-Lara, L, Isaac-Olivé, K & Melendez-Alafort, L 2020, 'Synthesis and preclinical evaluation of the ^99mTc-/¹⁷⁷Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting', Journal of Radioanalytical and Nuclear Chemistry, vol. 324, no. 1, pp. 21-32. https://doi.org/10.1007/s10967-020-07043-6

Ávila-Sánchez, Marcela ; Ferro-Flores, Guillermina ; Jiménez-Mancilla, Nallely ; Ocampo-García, Blanca ; Bravo-Villegas, Gerardo ; Luna-Gutiérrez, Myrna ; Santos-Cuevas, Clara ; Azorín-Vega, Erika ; Aranda-Lara, Liliana ; Isaac-Olivé, Keila ; Melendez-Alafort, Laura. / Synthesis and preclinical evaluation of the ^99mTc-/¹⁷⁷Lu-CXCR4-L theranostic pair for in vivo chemokine-4 receptor-specific targeting. In: Journal of Radioanalytical and Nuclear Chemistry. 2020 ; Vol. 324, No. 1. pp. 21-32.

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

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.",

keywords = "Lu-CXCR4-L, Tc-CXCR4-L, Chemokine-4 receptor, DOTA-HYNIC-CXCR4-L, HYNIC-CXCR4-L, Theranostic pair",

author = "Marcela {\'A}vila-S{\'a}nchez and Guillermina Ferro-Flores and Nallely Jim{\'e}nez-Mancilla and Blanca Ocampo-Garc{\'i}a and Gerardo Bravo-Villegas and Myrna Luna-Guti{\'e}rrez and Clara Santos-Cuevas and Erika Azor{\'i}n-Vega and Liliana Aranda-Lara and Keila Isaac-Oliv{\'e} and Laura Melendez-Alafort",

note = "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 {\textquoteleft}{\textquoteleft}Laboratorio Nacional de Investigaci{\'o}n y Desarrollo de Radiof{\'a}rmacos, CONACyT{\textquoteright}{\textquoteright}. Publisher Copyright: {\textcopyright} 2020, Akad{\'e}miai Kiad{\'o}, Budapest, Hungary. Copyright: Copyright 2020 Elsevier B.V., All rights reserved.",

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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.

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KW - Tc-CXCR4-L

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KW - Theranostic pair

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