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Advances in Aptamers for Cancer Targeting

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Biology".

Deadline for manuscript submissions: closed (28 February 2022) | Viewed by 5614

Special Issue Editor

Institute Experimental Endocrinology and Oncology “Gaetano Salvatore” (IEOS), National Research Council (CNR), 80145 Naples, Italy
Interests: aptamers; SELEX; cancer; targeted therapy; targeted delivery; non-coding RNAs
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

A Special Issue on the hot topic of “Advances in Aptamers for Cancer Targeting” is being prepared for the IJMS. This Special Issue is aimed at summarizing the most recent applications of aptamers for the classification/characterization, diagnosis, and/or treatment of the major cancer types.

Given their ability to bind with high-affinity and high-specificity cancer biomarkers, nucleic acid aptamers represent promising candidates as tools for new target discovery as well as for imaging probes, capture agents, and anticancer drug development. Aptamers exhibit similar functionality to antibodies but show several advantages over them, including easy and fast production, low costs, low immunogenicity, and high versatility. Due to their chemical nature, aptamers are suitable for receiving various chemical modifications to improve their features for clinical development. In addition, aptamers against cell surface receptors upon binding to their target may undergo receptor-mediated intracellular uptake; thus, they represent effective carriers for the targeted delivery of secondary reagents (e.g., fluorophores, magnetic nanoparticles, small interfering RNAs, microRNAs, antimiRs, small drugs, and toxins) for both diagnostic and therapeutic purposes.

Original manuscripts and reviews dealing with the selection, characterization, development, and/or application of aptamers for the selective targeting of tumors are welcomed from experts of the topic.

Dr. Silvia Catuogno
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • aptamers
  • cancer
  • SELEX
  • biomarker discovery
  • diagnosis
  • tumors
  • targeted therapy
  • targeted delivery

Published Papers (2 papers)

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Research

22 pages, 2616 KiB  
Article
Inhibition of Human Urokinase-Type Plasminogen Activator (uPA) Enzyme Activity and Receptor Binding by DNA Aptamers as Potential Therapeutics through Binding to the Different Forms of uPA
by Nico Dreymann, Julia Wuensche, Wiebke Sabrowski, Anja Moeller, Denise Czepluch, Dana Vu Van, Susanne Fuessel and Marcus M. Menger
Int. J. Mol. Sci. 2022, 23(9), 4890; https://doi.org/10.3390/ijms23094890 - 28 Apr 2022
Cited by 6 | Viewed by 2417
Abstract
Urokinase-type plasminogen activator is widely discussed as a marker for cancer prognosis and diagnosis and as a target for cancer therapies. Together with its receptor, uPA plays an important role in tumorigenesis, tumor progression and metastasis. In the present study, systematic evolution of [...] Read more.
Urokinase-type plasminogen activator is widely discussed as a marker for cancer prognosis and diagnosis and as a target for cancer therapies. Together with its receptor, uPA plays an important role in tumorigenesis, tumor progression and metastasis. In the present study, systematic evolution of ligands by exponential enrichment (SELEX) was used to select single-stranded DNA aptamers targeting different forms of human uPA. Selected aptamers allowed the distinction between HMW-uPA and LMW-uPA, and therefore, presumably, have different binding regions. Here, uPAapt-02-FR showed highly affine binding with a KD of 0.7 nM for HMW-uPA and 21 nM for LMW-uPA and was also able to bind to pro-uPA with a KD of 14 nM. Furthermore, no cross-reactivity to mouse uPA or tissue-type plasminogen activator (tPA) was measured, demonstrating high specificity. Suppression of the catalytic activity of uPA and inhibition of uPAR-binding could be demonstrated through binding with different aptamers and several of their truncated variants. Since RNA aptamers are already known to inhibit uPA-uPAR binding and other pathological functions of the uPA system, these aptamers represent a novel, promising tool not only for detection of uPA but also for interfering with the pathological functions of the uPA system by additionally inhibiting uPA activity. Full article
(This article belongs to the Special Issue Advances in Aptamers for Cancer Targeting)
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14 pages, 2968 KiB  
Article
Tumor Cell-Specific 2′-Fluoro RNA Aptamer Conjugated with Closo-Dodecaborate as A Potential Agent for Boron Neutron Capture Therapy
by Mariya A. Vorobyeva, Maya A. Dymova, Darya S. Novopashina, Elena V. Kuligina, Valentina V. Timoshenko, Iaroslav A. Kolesnikov, Sergey Yu. Taskaev, Vladimir A. Richter and Alya G. Venyaminova
Int. J. Mol. Sci. 2021, 22(14), 7326; https://doi.org/10.3390/ijms22147326 - 07 Jul 2021
Cited by 17 | Viewed by 2219
Abstract
Boron neutron capture therapy (BNCT) is a binary radiotherapeutic approach to the treatment of malignant tumors, especially glioblastoma, the most frequent and incurable brain tumor. For successful BNCT, a boron-containing therapeutic agent should provide selective and effective accumulation of 10B isotope inside [...] Read more.
Boron neutron capture therapy (BNCT) is a binary radiotherapeutic approach to the treatment of malignant tumors, especially glioblastoma, the most frequent and incurable brain tumor. For successful BNCT, a boron-containing therapeutic agent should provide selective and effective accumulation of 10B isotope inside target cells, which are then destroyed after neutron irradiation. Nucleic acid aptamers look like very prospective candidates for carrying 10B to the tumor cells. This study represents the first example of using 2′-F-RNA aptamer GL44 specific to the human glioblastoma U-87 MG cells as a boron delivery agent for BNCT. The closo-dodecaborate residue was attached to the 5′-end of the aptamer, which was also labeled by the fluorophore at the 3′-end. The resulting bifunctional conjugate showed effective and specific internalization into U-87 MG cells and low toxicity. After incubation with the conjugate, the cells were irradiated by epithermal neutrons on the Budker Institute of Nuclear Physics neutron source. Evaluation of the cell proliferation by real-time cell monitoring and the clonogenic test revealed that boron-loaded aptamer decreased specifically the viability of U-87 MG cells to the extent comparable to that of 10B-boronophenylalanine taken as a control. Therefore, we have demonstrated a proof of principle of employing aptamers for targeted delivery of boron-10 isotope in BNCT. Considering their specificity, ease of synthesis, and large toolkit of chemical approaches for high boron-loading, aptamers provide a promising basis for engineering novel BNCT agents. Full article
(This article belongs to the Special Issue Advances in Aptamers for Cancer Targeting)
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