Alteration in expression levels of genes as well as their regulatory components, such as those levels of miRNAs in cancer cells will likely reflect in the enrichment of unique cellular functions and biological processes in their corresponding cell systems. By employing systems biology approaches, and instead of examining individual gene, we will directly and unambiguously identify the regulatory pathways and biological processes that are distinctive to specific disease states or responses to therapeutic treatment. In this study, we employ gene set enrichment analysis inspired method to explore the functional regulation of miRNAs. The analysis integrated a mathematic model that associates miRNAs to gene sets through miRNA target genes with a statistic test of enrichment to study the regulation change at a specific pathway. Different from conventional individual miRNA processing procedures, our method enables researchers to construct regulation hypothesis at pathway and functional levels.