Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives

One of the most appealing approaches for cancer treatment is targeted therapy, which is based on the use of drugs able to target cancer cells without affecting normal ones. This strategy lets to overcome the major limitation of conventional chemotherapy, namely the lack of specificity of anticancer...

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Autores: Benigno, Daniela, Navarro, Natalia, Aviñó, Anna, Esposito, Veronica, Galeone, Aldo, Virgilio, Antonella, Fàbrega, Carme, Eritja Casadellà, Ramón
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2024
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/360493
Acceso en línea:http://hdl.handle.net/10261/360493
https://api.elsevier.com/content/abstract/scopus_id/85195556385
Access Level:acceso abierto
Palabra clave:T30923 aptamer
5-fluoro-2′-deoxyuridine
Aptamer-drug
Cancer therapy
G-quadruplex
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
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spelling Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives Benigno, Daniela Navarro, Natalia Aviñó, Anna Esposito, Veronica Galeone, Aldo Virgilio, Antonella Fàbrega, Carme Eritja Casadellà, Ramón T30923 aptamer 5-fluoro-2′-deoxyuridine Aptamer-drug Cancer therapy G-quadruplex http://metadata.un.org/sdg/3 Ensure healthy lives and promote well-being for all at all ages One of the most appealing approaches for cancer treatment is targeted therapy, which is based on the use of drugs able to target cancer cells without affecting normal ones. This strategy lets to overcome the major limitation of conventional chemotherapy, namely the lack of specificity of anticancer drugs, which often leads to severe side effects, decreasing the therapy effectiveness. Delivery of cell-killing substances to tumor cells is one-way targeted drug therapy can work. Generally, monoclonal antibodies are combined with chemotherapeutic drugs, allowing cellular uptake through the binding to their targets on the surface of cancer cells. Aptamer-drug conjugates represent a promising alternative solution to antibodies to minimize off-target effects, considering the remarkable selective binding capabilities of aptamers. In this study, to enhance the therapeutic efficacy of the antineoplastic agent 5-fluoro-2'-deoxyuridine (FdU) in various cancer cells, we focused on the development of a novel conjugate using the antiproliferative aptamer T30923 (INT) as a drug vehicle. Three derivatives composed of T30923 conjugated with a different number of FdU units were synthesized, and their structural and biological properties were thoroughly characterized, highlighting their potential for targeted and synergistic anticancer responses. We acknowledge Dr. Mireia Casasampere and Prof. Gemma Fabriàs for kindly providing HCT116 and Fibroblasts cell lines. We also thank Arnau Domínguez for assistance with oligonucleotides synthesis and CD measurements. Oligonucleotide synthesis was performed by the ICTS ‘‘NANBIOSIS” and specifically by the oligonucleotide synthesis platform (OSP) U29 at IQAC-CSIC (https://www.nanbiosis.es/portfolio/u29-oligonucleotide-synthesis-platform-osp/). Peer reviewed Elsevier http://hdl.handle.net/10261/360493 https://api.elsevier.com/content/abstract/scopus_id/85195556385
title Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
spellingShingle Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
Benigno, Daniela
T30923 aptamer
5-fluoro-2′-deoxyuridine
Aptamer-drug
Cancer therapy
G-quadruplex
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
title_short Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
title_full Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
title_fullStr Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
title_full_unstemmed Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
title_sort Aptamer-Drug conjugates for a targeted and synergistic anticancer Response: Exploiting T30923-5-fluoro-2'-deoxyuridine (INT-FdU) derivatives
author Benigno, Daniela
author_facet Benigno, Daniela
Navarro, Natalia
Aviñó, Anna
Esposito, Veronica
Galeone, Aldo
Virgilio, Antonella
Fàbrega, Carme
Eritja Casadellà, Ramón
author_role author
author2 Navarro, Natalia
Aviñó, Anna
Esposito, Veronica
Galeone, Aldo
Virgilio, Antonella
Fàbrega, Carme
Eritja Casadellà, Ramón
author2_role author
author
author
author
author
author
author
topic T30923 aptamer
5-fluoro-2′-deoxyuridine
Aptamer-drug
Cancer therapy
G-quadruplex
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
topic_facet T30923 aptamer
5-fluoro-2′-deoxyuridine
Aptamer-drug
Cancer therapy
G-quadruplex
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
description One of the most appealing approaches for cancer treatment is targeted therapy, which is based on the use of drugs able to target cancer cells without affecting normal ones. This strategy lets to overcome the major limitation of conventional chemotherapy, namely the lack of specificity of anticancer drugs, which often leads to severe side effects, decreasing the therapy effectiveness. Delivery of cell-killing substances to tumor cells is one-way targeted drug therapy can work. Generally, monoclonal antibodies are combined with chemotherapeutic drugs, allowing cellular uptake through the binding to their targets on the surface of cancer cells. Aptamer-drug conjugates represent a promising alternative solution to antibodies to minimize off-target effects, considering the remarkable selective binding capabilities of aptamers. In this study, to enhance the therapeutic efficacy of the antineoplastic agent 5-fluoro-2'-deoxyuridine (FdU) in various cancer cells, we focused on the development of a novel conjugate using the antiproliferative aptamer T30923 (INT) as a drug vehicle. Three derivatives composed of T30923 conjugated with a different number of FdU units were synthesized, and their structural and biological properties were thoroughly characterized, highlighting their potential for targeted and synergistic anticancer responses.
publishDate 2024
format article
status_str publishedVersion
url http://hdl.handle.net/10261/360493
https://api.elsevier.com/content/abstract/scopus_id/85195556385
eu_rights_str_mv openAccess
publisher Elsevier
institution Consejo Superior de Investigaciones Científicas (CSIC)
collection DIGITAL.CSIC. Repositorio Institucional del CSIC
reponame_str DIGITAL.CSIC. Repositorio Institucional del CSIC
instname_str Consejo Superior de Investigaciones Científicas (CSIC)
_version_ 1878439552008323072
publishDateSort 2024
author_browse Aviñó, Anna
Benigno, Daniela
Eritja Casadellà, Ramón
Esposito, Veronica
Fàbrega, Carme
Galeone, Aldo
Navarro, Natalia
Virgilio, Antonella
publisherStr Elsevier
score 6,9303427

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