Advances in the role of microRNAs in lipid metabolism-related anti-atherosclerotic drug discovery.

INTRODUCTION: Atherosclerosis is one of the leading causes of mortality in industrialized and developing nations and there remains a large unmet medical need for new therapeutic approaches. Therefore, efforts are continuing needed to discover and develop novel drugs based on the advances in the understanding of molecular basis in lipid metabolism, especially a critical role of miRNAs in regulating lipid metabolism. miRNAs are endogeneous non-coding small RNAs that regulate gene expression on the post-transcriptional level. Some miRNAs have been proposed as potential targets in anti-atherosclerotic drug discovery.

AREAS COVERED: This review provides a summary of recently reported miRNAs which are functioning in various pathways of lipid metabolism. Furthermore, this review describes the strategies currently employed for the miRNA-based drug discovery, including: the development of antisense oligonucleotides targeting the specific miRNAs directly and the discovery of small molecules targeting the miRNA activity or biogenesis by application of biochemical or cell-based screening assays.

EXPERT OPINION: miRNAs play a prominent role in lipid metabolism and provide intriguing therapeutic targets, which add a new dimension for anti-atherosclerotic drug discovery. Translation of these targets and strategies for drug discovery, although still challenging, has shown a promising potential for a more effective reduction in atherosclerotic risk in the future.