Despite considerable advances in early diagnosis, prostate cancer (PCa) remains the second leading cause of cancer-related deaths in men in western countries. In fact, although efficient therapies exist for early-stage disease, the treatment of advanced PCa remains unsuccessful mainly due to its poor responsiveness to anti-cancer agents. This evidence underlines the urgent need for the development of novel and more effective therapeutic approaches. In this context, the documented dysregulation of microRNAs (miRNAs)--which are short non-coding RNAs that regulate gene expression at post-transcriptional level- in PCa, together with their potential to simultaneously regulate multiple oncogenic/ tumor-suppressive pathways, has stimulated interest in defining a functional association between altered expression of specific miRNAs and the response of PCa to anti-cancer agents. The purpose of this review is to provide an overview on PCa-related miRNAs as potential novel therapeutic targets/tools, with a special focus on the role that they may play in conditioning the responsiveness of PCa to anti-cancer drugs.