Pharmacogenomic profiling of cancer has recently seen much activity with the accessibility of the newest generation of high-throughput platforms & technologies. Myriad mechanistic studies have been devoted to identifying dietary phytochemicals from fruit or vegetables that can help prevent cancer, with evidence suggesting an inverse correlation between intake & risk of certain cancers. To develop a comprehensive understanding of cancer pathogenesis, & potential for chemopreventive intervention with dietary factors, an integrated approach that encompasses both pharmacogenomic & mechanistic aspects is desirable. This work discusses the identification of germane molecular targets by expression profiling using dietary factors, synergistic effects in combinatorial use of dietary factors in colon cancer, regulatory studies in prostate cancer, concerted modulation of key players in inflammation & carcinogenesis, & delineation of prostate cancer biological networks. This will greatly enhance our understanding of the transcriptional circuitry in cancer & important master regulators in the cell that may potentially be exploited for preventive intervention using dietary phytomedicines.