During the last 3 decades, oncogenic Ras has been recognized as one of the potent causes of human cancer. But until now, there is no safe and effective Ras inhibitor, because alternative pathway is turned on when Ras inhibitor is treated. So there were many attempts to inhibit the post-translational modification termed farnesylation, which is essential for Ras anchorage into the membrane. Previous attempts to target farnesylation have focused on the development of farnesyltransferase inhibitors, but the performance of such agents in cancer clinical trials has not been as good as hoped. Here, we review novel therapeutic approaches targeting prenylation and prospect the future of using prenylation inhibitors as cancer therapy