The process by which cells change from an epithelial phenotype to a mesenchymal phenotype is called epithelial–mesenchymal Transition (EMT). This event occurs during normal development in many cell types. However, it has been observed that EMT can also occur in various types of cancer, where it has disastrous consequences, as it plays an integral part in invasion and metastasis. Hence, targeting EMT can be a viable and feasible option for cancer therapy. However, many signaling pathways interact with each other in complex cross talk to make this phenomenon possible, making it a very difficult goal to achieve. This chapter attempts to give the reader a brief insight into the process of EMT, the pathways that control it, as well as some important, druggable target candidate genes and proteins that can be used to modulate EMT in cancer.