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The Therapeutic Potential of MicroRNAs in Cancer

Thorsen, Stine B. MSc*; Obad, Susanna PhD; Jensen, Niels F. MSc*; Stenvang, Jan PhD*; Kauppinen, Sakari PhD†‡

doi: 10.1097/PPO.0b013e318258b5d6

MicroRNAs (miRNAs) have been uncovered as important posttranscriptional regulators of nearly every biological process in the cell. Furthermore, mounting evidence implies that miRNAs play key roles in the pathogenesis of cancer and that many miRNAs can function either as oncogenes or tumor suppressors. Thus, miRNAs have rapidly emerged as promising targets for the development of novel anticancer therapeutics. The development of miRNA-based cancer therapeutics relies on restoring the activity of tumor suppressor miRNAs using double-stranded miRNA mimics or inhibition of oncogenic miRNAs using single-stranded antisense oligonucleotides, termed antimiRs. In the present review, we focus on recent advancements in the discovery and development of miRNA-based cancer therapeutics using these 2 approaches. In addition, we summarize selected studies, in which modulation of miRNA activity in preclinical cancer models in vivo has demonstrated promising therapeutic potential.

From the *Sino-Danish Breast Cancer Research Centre and Institute of Veterinary Disease Biology, Faculty of Health and Medical Sciences, University of Copenhagen, Frederiksberg; †Santaris Pharma, Hørsholm; and ‡Aalborg University Copenhagen, Ballerup, Denmark.

Conflict of Interest and Source of Funding: This work was supported by grants from the Danish National Advanced Technology Foundation and the Danish National Research Foundation. S.O. and S.K. are employees of Santaris Pharma, a clinical stage biopharmaceutical company that develops RNA-targeted therapeutics. For the remaining authors, none were declared.

Reprints: Sakari Kauppinen, PhD, Santaris Pharma, Kogle Allé 6, DK-2970 Hørsholm, Denmark. E-mail:;

© 2012 Lippincott Williams & Wilkins, Inc.