Selective depletion of metastatic stem cells as therapy for human colorectal cancer

Abstract Selective elimination of metastatic stem cells (MetSCs) promises to block metastatic dissemination. Colorectal cancer (CRC) cells overexpressing CXCR4 display trafficking functions and metastasis‐initiating capacity. We assessed the antimetastatic activity of a nanoconjugate (T22‐GFP‐H6‐FdU...

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Main Authors: María Virtudes Céspedes, Ugutz Unzueta, Anna Aviñó, Alberto Gallardo, Patricia Álamo, Rita Sala, Alejandro Sánchez‐Chardi, Isolda Casanova, María Antònia Mangues, Antonio Lopez‐Pousa, Ramón Eritja, Antonio Villaverde, Esther Vázquez, Ramón Mangues
Format: Article
Language:English
Published: Springer Nature 2018-09-01
Series:EMBO Molecular Medicine
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Online Access:https://doi.org/10.15252/emmm.201708772
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author María Virtudes Céspedes
Ugutz Unzueta
Anna Aviñó
Alberto Gallardo
Patricia Álamo
Rita Sala
Alejandro Sánchez‐Chardi
Isolda Casanova
María Antònia Mangues
Antonio Lopez‐Pousa
Ramón Eritja
Antonio Villaverde
Esther Vázquez
Ramón Mangues
author_facet María Virtudes Céspedes
Ugutz Unzueta
Anna Aviñó
Alberto Gallardo
Patricia Álamo
Rita Sala
Alejandro Sánchez‐Chardi
Isolda Casanova
María Antònia Mangues
Antonio Lopez‐Pousa
Ramón Eritja
Antonio Villaverde
Esther Vázquez
Ramón Mangues
author_sort María Virtudes Céspedes
collection DOAJ
description Abstract Selective elimination of metastatic stem cells (MetSCs) promises to block metastatic dissemination. Colorectal cancer (CRC) cells overexpressing CXCR4 display trafficking functions and metastasis‐initiating capacity. We assessed the antimetastatic activity of a nanoconjugate (T22‐GFP‐H6‐FdU) that selectively delivers Floxuridine to CXCR4+ cells. In contrast to free oligo‐FdU, intravenous T22‐GFP‐H6‐FdU selectively accumulates and internalizes in CXCR4+ cancer cells, triggering DNA damage and apoptosis, which leads to their selective elimination and to reduced tumor re‐initiation capacity. Repeated T22‐GFP‐H6‐FdU administration in cell line and patient‐derived CRC models blocks intravasation and completely prevents metastases development in 38–83% of mice, while showing CXCR4 expression‐dependent and site‐dependent reduction in foci number and size in liver, peritoneal, or lung metastases in the rest of mice, compared to free oligo‐FdU. T22‐GFP‐H6‐FdU induces also higher regression of established metastases than free oligo‐FdU, with negligible distribution or toxicity in normal tissues. This targeted drug delivery approach yields potent antimetastatic effect, through selective depletion of metastatic CXCR4+ cancer cells, and validates metastatic stem cells (MetSCs) as targets for clinical therapy.
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spelling doaj-art-22f73e7198844bf5873e6fa6e08b45a42025-08-20T03:46:13ZengSpringer NatureEMBO Molecular Medicine1757-46761757-46842018-09-01101012210.15252/emmm.201708772Selective depletion of metastatic stem cells as therapy for human colorectal cancerMaría Virtudes Céspedes0Ugutz Unzueta1Anna Aviñó2Alberto Gallardo3Patricia Álamo4Rita Sala5Alejandro Sánchez‐Chardi6Isolda Casanova7María Antònia Mangues8Antonio Lopez‐Pousa9Ramón Eritja10Antonio Villaverde11Esther Vázquez12Ramón Mangues13Institut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauInstitut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauCIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER‐BBN)CIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER‐BBN)Institut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauInstitut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauServei de Microscòpia, Universitat Autònoma de BarcelonaInstitut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauInstitut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauCIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER‐BBN)CIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER‐BBN)CIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER‐BBN)CIBER de Bioingeniería, Biomateriales y Nanomedicina (CIBER‐BBN)Institut d'Investigacions Biomèdiques Sant Pau, Hospital de Santa Creu i Sant PauAbstract Selective elimination of metastatic stem cells (MetSCs) promises to block metastatic dissemination. Colorectal cancer (CRC) cells overexpressing CXCR4 display trafficking functions and metastasis‐initiating capacity. We assessed the antimetastatic activity of a nanoconjugate (T22‐GFP‐H6‐FdU) that selectively delivers Floxuridine to CXCR4+ cells. In contrast to free oligo‐FdU, intravenous T22‐GFP‐H6‐FdU selectively accumulates and internalizes in CXCR4+ cancer cells, triggering DNA damage and apoptosis, which leads to their selective elimination and to reduced tumor re‐initiation capacity. Repeated T22‐GFP‐H6‐FdU administration in cell line and patient‐derived CRC models blocks intravasation and completely prevents metastases development in 38–83% of mice, while showing CXCR4 expression‐dependent and site‐dependent reduction in foci number and size in liver, peritoneal, or lung metastases in the rest of mice, compared to free oligo‐FdU. T22‐GFP‐H6‐FdU induces also higher regression of established metastases than free oligo‐FdU, with negligible distribution or toxicity in normal tissues. This targeted drug delivery approach yields potent antimetastatic effect, through selective depletion of metastatic CXCR4+ cancer cells, and validates metastatic stem cells (MetSCs) as targets for clinical therapy.https://doi.org/10.15252/emmm.201708772colorectal cancerCXCR4 receptormetastatic stem cellsprotein nanoconjugatetargeted drug delivery
spellingShingle María Virtudes Céspedes
Ugutz Unzueta
Anna Aviñó
Alberto Gallardo
Patricia Álamo
Rita Sala
Alejandro Sánchez‐Chardi
Isolda Casanova
María Antònia Mangues
Antonio Lopez‐Pousa
Ramón Eritja
Antonio Villaverde
Esther Vázquez
Ramón Mangues
Selective depletion of metastatic stem cells as therapy for human colorectal cancer
EMBO Molecular Medicine
colorectal cancer
CXCR4 receptor
metastatic stem cells
protein nanoconjugate
targeted drug delivery
title Selective depletion of metastatic stem cells as therapy for human colorectal cancer
title_full Selective depletion of metastatic stem cells as therapy for human colorectal cancer
title_fullStr Selective depletion of metastatic stem cells as therapy for human colorectal cancer
title_full_unstemmed Selective depletion of metastatic stem cells as therapy for human colorectal cancer
title_short Selective depletion of metastatic stem cells as therapy for human colorectal cancer
title_sort selective depletion of metastatic stem cells as therapy for human colorectal cancer
topic colorectal cancer
CXCR4 receptor
metastatic stem cells
protein nanoconjugate
targeted drug delivery
url https://doi.org/10.15252/emmm.201708772
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