MicroRNA (miRNA) is an important class of small non-coding RNAs that act as post-transcriptional modulators of gene expression, and whose dysregulation has been implicated in various stages of cancer development. Although promising experimental evidences point toward a potential use of miRNA as targets for cancer treatment, to date, technical challenges have hindered the translation of this information from bench to bedside. Here, we review some of the most promising approaches that have been explored to develop new anti-cancer therapies based on the regulation of miRNA function.

The objective of this review is to draw the attention on recent observations suggesting that global inhibition of miRNA function may inhibit tumor development, and which may set the stage for new therapeutic avenues. We discuss the characteristics of some of the most promising strategies to inhibit miRNA function and describe their advantages as well as their potential drawbacks.

Although pharmacologic interventions aimed to modulate miRNA activity are still at the primordial stage, exciting new evidences highlight the need to persist in studying the relationship between miRNA function and cancer. Information gathered from these studies may have the potential to lead to new opportunities of treatment of cancer.