Special Issue "Aptamers: Promising Tools for Cancer Diagnosis and Therapy"

A special issue of Cancers (ISSN 2072-6694).

Deadline for manuscript submissions: closed (15 December 2017)

Special Issue Editor

Guest Editor
Dr. Laura Cerchia

Institute of Experimental Endocrinology and Oncology "G. Salvatore" (IEOS) – National Research Council of Italy (CNR), Via S. Pansini 5, 80131 Naples, Italy
Website | E-Mail
Phone: + 39 0815455751
Interests: oligonucleotide aptamer, cell-SELEX technology, targeting delivery system, cancer biomarker discovery, cancer cell biology and signaling, targeted therapy, chemotherapy resistance, glioblastoma, triple-negative breast cancers

Special Issue Information

Dear Colleagues,

Precision cancer medicines that act specifically at the diseased site with the aim of reducing unwanted side effects on oncologic patients, are now achieving significant progress, especially through the development of active targeting agents.

Aptamers, isolated by the Systematic Evolution of Ligands by EXponential enrichment (SELEX) process, are highly structured, short, single-stranded oligonucleotides that, because of their complex tridimensional shapes, interact at high affinity and specificity with their targets. For their mode of action, aptamers are also called chemical antibodies, however, unlike antibodies, they display high tissue penetration due to their small size and are no or poor immunogenic. Further, aptamers are characterized by ready synthesis and chemical modifications designed to improve their stability, reduce their toxicity and allow conjugation to secondary reagents (including therapeutics and molecular imaging probes). Aptamers have so far demonstrated great potential as recognition elements in a number of applications, including cancer biomarkers discovery, targeted therapy, in vitro diagnosis and in vivo imaging modalities.

This Special Issue will provide an updated overview of the progress of SELEX technology and highlight perspectives and challenges for the use of aptamers as diagnostic and therapeutic agents, and as active targeting agents to enhance the therapeutic efficacy of nanomedicines in cancer.

Dr. Laura Cerchia
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 papers will be 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. Cancers is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). 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.

Published Papers (7 papers)

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Editorial

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Open AccessEditorial Aptamers: Promising Tools for Cancer Diagnosis and Therapy
Cancers 2018, 10(5), 132; https://doi.org/10.3390/cancers10050132
Received: 25 April 2018 / Revised: 2 May 2018 / Accepted: 2 May 2018 / Published: 3 May 2018
Cited by 2 | PDF Full-text (148 KB) | HTML Full-text | XML Full-text
Abstract
The most common approaches to cancer treatment have been, for decades, based on surgical excision, radio- and/or chemotherapy, which, in spite of their modest survival benefits, still encounter several limitations, in part due to their lack of specificity.[...] Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)

Review

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Open AccessFeature PaperReview Aptamer Therapeutics in Cancer: Current and Future
Received: 11 February 2018 / Revised: 13 March 2018 / Accepted: 15 March 2018 / Published: 19 March 2018
Cited by 10 | PDF Full-text (919 KB) | HTML Full-text | XML Full-text
Abstract
Aptamer-related technologies represent a revolutionary advancement in the capacity to rapidly develop new classes of targeting ligands. Structurally distinct RNA and DNA oligonucleotides, aptamers mimic small, protein-binding molecules and exhibit high binding affinity and selectivity. Although their molecular weight is relatively small—approximately one-tenth [...] Read more.
Aptamer-related technologies represent a revolutionary advancement in the capacity to rapidly develop new classes of targeting ligands. Structurally distinct RNA and DNA oligonucleotides, aptamers mimic small, protein-binding molecules and exhibit high binding affinity and selectivity. Although their molecular weight is relatively small—approximately one-tenth that of monoclonal antibodies—their complex tertiary folded structures create sufficient recognition surface area for tight interaction with target molecules. Additionally, unlike antibodies, aptamers can be readily chemically synthesized and modified. In addition, aptamers’ long storage period and low immunogenicity are favorable properties for clinical utility. Due to their flexibility of chemical modification, aptamers are conjugated to other chemical entities including chemotherapeutic agents, siRNA, nanoparticles, and solid phase surfaces for therapeutic and diagnostic applications. However, as relatively small sized oligonucleotides, aptamers present several challenges for successful clinical translation. Their short plasma half-lives due to nuclease degradation and rapid renal excretion necessitate further structural modification of aptamers for clinical application. Since the US Food and Drug Administration (FDA) approval of the first aptamer drug, Macugen® (pegaptanib), which treats wet-age-related macular degeneration, several aptamer therapeutics for oncology have followed and shown promise in pre-clinical models as well as clinical trials. This review discusses the advantages and challenges of aptamers and introduces therapeutic aptamers under investigation and in clinical trials for cancer treatments. Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)
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Open AccessFeature PaperReview Bioapplications of Cell-SELEX-Generated Aptamers in Cancer Diagnostics, Therapeutics, Theranostics and Biomarker Discovery: A Comprehensive Review
Received: 17 December 2017 / Revised: 24 January 2018 / Accepted: 25 January 2018 / Published: 9 February 2018
Cited by 13 | PDF Full-text (6315 KB) | HTML Full-text | XML Full-text
Abstract
Currently, functional single-stranded oligonucleotide probes, termed aptamers, generated by an iterative technology, Systematic Evolution of Ligands by Exponential Enrichment (SELEX), are utilized to selectively target molecules or cells with high affinity. Aptamers hold considerable promise as multifunctional molecules or conjugates for challenging nanotechnologies [...] Read more.
Currently, functional single-stranded oligonucleotide probes, termed aptamers, generated by an iterative technology, Systematic Evolution of Ligands by Exponential Enrichment (SELEX), are utilized to selectively target molecules or cells with high affinity. Aptamers hold considerable promise as multifunctional molecules or conjugates for challenging nanotechnologies or bioapplications now and in the future. In this review, we first describe recent endeavors to select aptamers towards live cancer cells via cell-SELEX. We then introduce several characteristic applications of selected aptamers, especially in imaging, drug delivery and therapy. In part, these advances have been made possible via synthesis of aptamer-based nanomaterials, which, by their sizes, shapes, and physicochemical properties, allow such aptamer-nanomaterial complexes to function as signal reporters or drug carriers. We also describe how these aptamer-based molecular tools contribute to cancer biomarker discovery through high-affinity recognition of membrane protein receptors. Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)
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Open AccessReview EpCAM Immunotherapy versus Specific Targeted Delivery of Drugs
Received: 18 December 2017 / Revised: 8 January 2018 / Accepted: 8 January 2018 / Published: 12 January 2018
Cited by 6 | PDF Full-text (1832 KB) | HTML Full-text | XML Full-text
Abstract
The epithelial cell adhesion molecule (EpCAM), or CD326, was one of the first cancer associated biomarkers to be discovered. In the last forty years, this biomarker has been investigated for use in personalized cancer therapy, with the first monoclonal antibody, edrecolomab, being trialled [...] Read more.
The epithelial cell adhesion molecule (EpCAM), or CD326, was one of the first cancer associated biomarkers to be discovered. In the last forty years, this biomarker has been investigated for use in personalized cancer therapy, with the first monoclonal antibody, edrecolomab, being trialled in humans more than thirty years ago. Since then, several other monoclonal antibodies have been raised to EpCAM and tested in clinical trials. However, while monoclonal antibody therapy has been investigated against EpCAM for almost 40 years as primary or adjuvant therapy, it has not shown as much promise as initially heralded. In this review, we look at the reasons why and consider alternative targeting options, such as aptamers, to turn this almost ubiquitously expressed epithelial cancer biomarker into a viable target for future personalized therapy. Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)
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Open AccessFeature PaperReview Current Advances in Aptamers for Cancer Diagnosis and Therapy
Received: 14 December 2017 / Revised: 22 December 2017 / Accepted: 26 December 2017 / Published: 3 January 2018
Cited by 18 | PDF Full-text (4543 KB) | HTML Full-text | XML Full-text
Abstract
Nucleic acid aptamers are single-stranded oligonucleotides that interact with target molecules with high affinity and specificity in unique three-dimensional structures. Aptamers are generally isolated by a simple selection process called systematic evolution of ligands by exponential enrichment (SELEX) and then can be chemically [...] Read more.
Nucleic acid aptamers are single-stranded oligonucleotides that interact with target molecules with high affinity and specificity in unique three-dimensional structures. Aptamers are generally isolated by a simple selection process called systematic evolution of ligands by exponential enrichment (SELEX) and then can be chemically synthesized and modified. Because of their high affinity and specificity, aptamers are promising agents for biomarker discovery, as well as cancer diagnosis and therapy. In this review, we present recent progress and challenges in aptamer and SELEX technology and highlight some representative applications of aptamers in cancer therapy. Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)
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Open AccessFeature PaperReview Fluorescence Sensing Using DNA Aptamers in Cancer Research and Clinical Diagnostics
Cancers 2017, 9(12), 174; https://doi.org/10.3390/cancers9120174
Received: 30 November 2017 / Revised: 14 December 2017 / Accepted: 16 December 2017 / Published: 20 December 2017
Cited by 8 | PDF Full-text (8433 KB) | HTML Full-text | XML Full-text
Abstract
Among the various advantages of aptamers over antibodies, remarkable is their ability to tolerate a large number of chemical modifications within their backbone or at the termini without losing significant activity. Indeed, aptamers can be easily equipped with a wide variety of reporter [...] Read more.
Among the various advantages of aptamers over antibodies, remarkable is their ability to tolerate a large number of chemical modifications within their backbone or at the termini without losing significant activity. Indeed, aptamers can be easily equipped with a wide variety of reporter groups or coupled to different carriers, nanoparticles, or other biomolecules, thus producing valuable molecular recognition tools effective for diagnostic and therapeutic purposes. This review reports an updated overview on fluorescent DNA aptamers, designed to recognize significant cancer biomarkers both in soluble or membrane-bound form. In many examples, the aptamer secondary structure switches induced by target recognition are suitably translated in a detectable fluorescent signal using either fluorescently-labelled or label-free aptamers. The fluorescence emission changes, producing an enhancement (“signal-on”) or a quenching (“signal-off”) effect, directly reflect the extent of the binding, thereby allowing for quantitative determination of the target in bioanalytical assays. Furthermore, several aptamers conjugated to fluorescent probes proved to be effective for applications in tumour diagnosis and intraoperative surgery, producing tumour-type specific, non-invasive in vivo imaging tools for cancer pre- and post-treatment assessment. Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)
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Open AccessReview Current and Prospective Protein Biomarkers of Lung Cancer
Cancers 2017, 9(11), 155; https://doi.org/10.3390/cancers9110155
Received: 12 October 2017 / Revised: 2 November 2017 / Accepted: 6 November 2017 / Published: 13 November 2017
Cited by 13 | PDF Full-text (1671 KB) | HTML Full-text | XML Full-text
Abstract
Lung cancer is a malignant lung tumor with various histological variants that arise from different cell types, such as bronchial epithelium, bronchioles, alveoli, or bronchial mucous glands. The clinical course and treatment efficacy of lung cancer depends on the histological variant of the [...] Read more.
Lung cancer is a malignant lung tumor with various histological variants that arise from different cell types, such as bronchial epithelium, bronchioles, alveoli, or bronchial mucous glands. The clinical course and treatment efficacy of lung cancer depends on the histological variant of the tumor. Therefore, accurate identification of the histological type of cancer and respective protein biomarkers is crucial for adequate therapy. Due to the great diversity in the molecular-biological features of lung cancer histological types, detection is impossible without knowledge of the nature and origin of malignant cells, which release certain protein biomarkers into the bloodstream. To date, different panels of biomarkers are used for screening. Unfortunately, a uniform serum biomarker composition capable of distinguishing lung cancer types is yet to be discovered. As such, histological analyses of tumor biopsies and immunohistochemistry are the most frequently used methods for establishing correct diagnoses. Here, we discuss the recent advances in conventional and prospective aptamer based strategies for biomarker discovery. Aptamers like artificial antibodies can serve as molecular recognition elements for isolation detection and search of novel tumor-associated markers. Here we will describe how these small synthetic single stranded oligonucleotides can be used for lung cancer biomarker discovery and utilized for accurate diagnosis and targeted therapy. Furthermore, we describe the most frequently used in-clinic and novel lung cancer biomarkers, which suggest to have the ability of differentiating between histological types of lung cancer and defining metastasis rate. Full article
(This article belongs to the Special Issue Aptamers: Promising Tools for Cancer Diagnosis and Therapy)
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Graphical abstract

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