Aptamer Therapeutics in Cancers: New Advances and Future Trends

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Molecular Medicine".

Deadline for manuscript submissions: 31 May 2025 | Viewed by 2889

Special Issue Editors


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Guest Editor
Institute Experimental Endocrinology and Oncology "Gaetano Salvatore" (IEOS), National Research Council (CNR), 80145 Naples, Italy
Interests: aptamers; targeted delivery; targeted therapy; non-coding RNAs; cancer

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Guest Editor
IRCCS SDN, 80100 Naples, Italy
Interests: aptamers; non-coding RNAs; cancer; targeted therapy; cancer diagnosis

Special Issue Information

Dear Colleagues,

Nucleic acid aptamers represent a revolutionary and winning approach in the field of precision anticancer medicine. Based on their unique three-dimensional shapes, aptamers recognize specific target molecules with high affinity, acting as selective inhibitory agents and/or carriers for targeted delivery. Therefore, aptamers allow the specific recognition of diseased tissues, strongly reducing the occurrence of undesirable off-target effects.

Due to their mode of action, they are called "chemical antibodies", but, thanks to their chemical nature, they exhibit many advantageous features over antibodies, including fast and easy production, high batch fidelity, high tissue penetration, low costs, easy chemical modification, low toxicity and immunogenicity.

To Date, many reports describe the application of aptamers or aptamer-based conjugates as anticancer drugs, also proposing multimodal approaches to improve therapeutic efficacy. Furthermore, several aptamer-based approaches have shown promise in clinical trials.

This Special Issue aims to summarize recent advances in aptamer-based technology and application in major cancer types, discussing advantages, limitations and possible improvements to optimize aptamer development in the near future.

We are pleased to invite you to participate in this Special Issue in Biomolecules by submitting an original or a review article relevant to the field.

I am looking forward to receiving your contributions.

Dr. Silvia Catuogno
Dr. Silvia Nuzzo
Guest Editors

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Keywords

  • aptamers
  • cancer
  • targeted therapy
  • aptamer-based conjugates
  • aptamer-conjugated nanoparticles

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Published Papers (2 papers)

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Research

14 pages, 1149 KiB  
Article
Targeting Glioblastoma Stem Cells: A40s Aptamer-NIR-Dye Conjugate for Glioblastoma Visualization and Treatment
by Alessandra Affinito, Francesco Ingenito, Sara Verde, Emanuele Musella, Birlipta Pattanayak, Danilo Fiore, Cristina Quintavalle, Aurelia Fraticelli, Martina Mascolo, Gianluca Petrillo, Claudia Pignataro, Giada De Luca, Laura Mezzanotte and Gerolama Condorelli
Biomolecules 2025, 15(6), 768; https://doi.org/10.3390/biom15060768 (registering DOI) - 27 May 2025
Abstract
Glioblastoma (GBM) is the most aggressive and challenging brain cancer, in terms of diagnosis and therapy. The highly infiltrative glioblastoma stem cells (GSCs) are difficult to visualize and surgically remove with the current diagnostic tools, which often lead to misdiagnosis and false-positive results. [...] Read more.
Glioblastoma (GBM) is the most aggressive and challenging brain cancer, in terms of diagnosis and therapy. The highly infiltrative glioblastoma stem cells (GSCs) are difficult to visualize and surgically remove with the current diagnostic tools, which often lead to misdiagnosis and false-positive results. In this study, we focused on a groundbreaking tool for specifically visualizing and removing GSCs. We exploited the specific binding of A40s aptamer to EphA2 for the selective delivery of Near-Infrared Dyes (NIR-Dyes), like IR700DX and ICG, both in vitro and in vivo. The A40s aptamer, engineered through the NIR-Dye conjugation, did not affect aptamer binding ability; indeed, A40s-NIR-Dye conjugates bound GLI261 stem-like cells and patient-derived GSCs in vitro; moreover, they induced cell death upon photodynamic therapy treatment (PDT). Additionally, when systemically administrated, the A40s-NIR-Dye conjugates allowed GSC visualization and accumulated in tumor mass. This allows GSCs detection and treatment. Our findings demonstrate the potential use of A40s aptamer as a targeted therapeutic approach and imaging tool in vivo for GSCs, paving the way for improved, more effective, and less invasive GBM management. Full article
(This article belongs to the Special Issue Aptamer Therapeutics in Cancers: New Advances and Future Trends)
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18 pages, 6100 KiB  
Article
Selection of Aptamers for Use as Molecular Probes in AFM Detection of Proteins
by Maria O. Ershova, Amir Taldaev, Petr V. Konarev, Georgy S. Peters, Anastasia A. Valueva, Irina A. Ivanova, Sergey V. Kraevsky, Andrey F. Kozlov, Vadim S. Ziborov, Yuri D. Ivanov, Alexander I. Archakov and Tatyana O. Pleshakova
Biomolecules 2023, 13(12), 1776; https://doi.org/10.3390/biom13121776 - 12 Dec 2023
Cited by 1 | Viewed by 1970
Abstract
Currently, there is great interest in the development of highly sensitive bioanalytical systems for diagnosing diseases at an early stage, when pathological biomarkers are present in biological fluids at low concentrations and there are no clinical manifestations. A promising direction is the use [...] Read more.
Currently, there is great interest in the development of highly sensitive bioanalytical systems for diagnosing diseases at an early stage, when pathological biomarkers are present in biological fluids at low concentrations and there are no clinical manifestations. A promising direction is the use of molecular detectors―highly sensitive devices that detect signals from single biomacromolecules. A typical detector in this class is the atomic force microscope (AFM). The high sensitivity of an AFM-based bioanalysis system is determined by the size of the sensing element of an atomic force microscope―the cantilever―the radius of the curvature of which is comparable to that of a biomolecule. Biospecific molecular probe–target interactions are used to ensure detection system specificity. Antibodies, aptamers, synthetic antibodies, and peptides can be used as molecular probes. This study has demonstrated the possibility of using aptamers as molecular probes for AFM-based detection of the ovarian cancer biomarker CA125. Antigen detection in a nanomolar solution was carried out using AFM chips with immobilized aptamers, commercially available or synthesized based on sequences from open sources. Both aptamer types can be used for antigen detection, but the availability of sequence information enables additional modeling of the aptamer structure with allowance for modifications necessary for immobilization of the aptamer on an AFM chip surface. Information on the structure and oligomeric composition of aptamers in the solution was acquired by combining small-angle X-ray scattering and molecular modeling. Modeling enabled pre-selection, before the experimental stage, of aptamers for use as surface-immobilized molecular probes. Full article
(This article belongs to the Special Issue Aptamer Therapeutics in Cancers: New Advances and Future Trends)
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