Many investigators have embarked upon the search for novel cellular targets for the treatment of cancer. A popular therapeutic strategy is to intervene with the components of cellular signalling systems that are altered during malignancy. The molecular heterogeneity of the protein kinase C (PKC) family and their functional divergence make them attractive targets for anticancer drug development. PKC can also influence the sensitivity of tumor tissue to conventional cytotoxic drugs. As discussed in this review, a complete understanding of the PKC signal transduction pathway is obligatory for the selective destruction of tumor tissue by exploiting PKC as either a target or a modulator of cancer chemotherapeutic agents.