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Gambari et al. J Cancer Metastasis Treat 2019;5:55 Journal of Cancer
DOI: 10.20517/2394-4722.2019.18 Metastasis and Treatment

Review Open Access

Peptide nucleic acid-based targeting of microRNAs:
possible therapeutic applications for glioblastoma

Roberto Gambari , Jessica Gasparello , Alessia Finotti 1
1
1,2
1 Department of Life Sciences and Biotechnology, University of Ferrara, Ferrara 44121, Italy.
2 Interuniversity Consortium for Biotechnology (CIB), Trieste 34149, Italy.
Correspondence to: Prof. Roberto Gambari, Department of Life Sciences and Biotechnology, University of Ferrara, Via Fossato di
Mortara 74, Ferrara 44121, Italy. E-mail: gam@unife.it

How to cite this article: Gambari R, Gasparello J, Finotti A. Peptide nucleic acid-based targeting of microRNAs: possible
therapeutic applications for glioblastoma. J Cancer Metastasis Treat 2019;5:55. http://dx.doi.org/10.20517/2394-4722.2019.18

Received: 25 Feb 2019 First Decision: 2 Apr 2019 Revised: 17 May 2019 Accepted: 29 May 2019 Published: 11 Jul 2019
Science Editor: Ciro Isidoro; Gianluca Gaidano Copy Editor: Cai-Hong Wang Production Editor: Jing Yu

Abstract

A large and incremental number of non-coding RNAs, including microRNAs (miRNAs) have been recently
demonstrated to play a very important role in human pathologies, including cancer. Therefore, microRNAs have
been proposed as therapeutic targets and molecules exhibiting anti-miRNA activity or mimicking functional
miRNAs have been developed. Among biomolecules proposed in anti-miRNA therapy, peptide nucleic acids
(PNAs) are appealing, in consideration of their stability and efficacy in recognizing RNA targets. PNAs against
tumor associated miRNAs have proven to be efficient in inducing anti-tumor effects both in vitro and in vivo. For
instance, PNAs targeting miR-155-5p are able to induce apoptosis in glioma cell lines and to enhance the sensitivity
to temozolomide (TMZ) in TMZ resistant glioma cells. In vivo, PNAs anti-miR-21 were found to exhibit anti-tumor
effects associated with improved survival when administered to animals with intracranial gliomas.

Keywords: Peptide nucleic acids, glioma, microRNAs, miRNA targeting, delivery, apoptosis, temozolomide

MICRORNAS IN ONCOLOGY
MicroRNAs (miRNAs) are a family of evolutionary conserved small (19 to 25 nucleotides in length)
non-coding RNAs playing important roles in the post-transcriptional control of gene expression. This control
is operated at the level of mRNA translation and is based on the miRNA-dependent recognition of 3’UTR,
CDS and 5’UTR mRNA sequences. This molecular recognition leads to a reduction of protein synthesis .
[1-4]
Single or multiple mRNAs can be targeted by a single miRNA, while a single mRNA can be recognized and

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