MicroRNAs (miRNAs) are remarkable molecules that appear to have a fundamental role in the biology of the cell. They constitute a class of non-protein encoding RNA molecules which have now emerged as key players in regulating the activity of mRNA. miRNAs are small RNAmolecules around 22 nucleotides in length, which affect the activity of specific mRNA, directly degrading it and/or preventing its translation into protein. The science of miRNAs holds them as candidate biomarkers for the early detection and management of cancer. There is also considerable excitement for the use of miRNAs as a novel class of therapeutic targets and as a new class of therapeutic agents for the treatment of cancers. From a clinical perspective, miRNAs can induce a number of effects and may have a diverse application in biomedical research. This review highlights the general mode of action of miRNAs, their biogenesis, the effect of diet on miRNA expression and the impact of miRNAs on cancer epigenetics and drug resistance in various cancers. Further we also provide emphasis on bioinformatics software which can be used to determine potential targets of miRNAs.