Mir-221/222 are promising targets for innovative anticancer therapy

ABSTRACT

Introduction: MicroRNAs (miRNAs) are key non-coding RNA post-transcriptional regulators of messenger RNAs (mRNAs), and are deeply dysregulated in human cancer. A rising body of evidence indicates that miRNAs represent valuable therapeutic targets. In this light, the cluster miR-221/222 are of particular relevance, given that they are strongly upregulated in a variety of solid and hematologic malignancies.

Area covered: This review summarizes recent findings on the roles played by miR-221/222 in human cancer and their potential clinical value as promising targets for therapeutic studies.

Expert opinion: The rising body of advanced preclinical evidence on the biological significance of miR-221/222 in a variety of malignancies indicates that they will play a crucial role in the future of innovative therapeutic strategies, both as validated biomarkers and targets.

KEYWORDS:

• MicroRNA
• miRNA
• miRNA inhibitors
• miR-221
• miR-221/222
• oligonucleotide-based therapy
• cancer
• myeloma

Article highlights

• MicroRNAs (miRNAs) are non-coding RNAs, key post-transcriptional regulators of messenger RNAs, and deeply dysregulated in human cancer.

• Dysregulated miRNAs may provide novel and valuable therapeutic targets.

• miR-221/222 are of relevant interest since they are strongly upregulated in a variety of solid and hematologic malignancies.

• The wide biological relevance of miR-221/222 in human cancer and their potential clinical value make them promising targets for therapeutic studies.

• A growing body of evidence indicates that miR-221/222 inhibitors exert antitumor activity against different malignancies and overcome resistance to cytotoxic agents.

• Promising results on circulating miR-221/222 point further investigation for diagnostic and predictive purposes.

• All the reported findings strongly support the role of miR-221/222 as a promising target for innovative therapeutics and at the same time as a promising biomarker for precision medicine approaches in cancer management.

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Declaration of interest

This paper was supported with funding from the AIRC (the Italian Association for Cancer Research, a non profit organization, PI: PT. ‘Special Program Molecular Clinical Oncology - 5 per mille’ n. 9980, 2010/15). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.