Since the original identification of a transmissible agent responsible for the development of tumors in chickens, now known to be a retrovirus encoding the v-src gene, significant progress has been made in defining the potential functions of its human homolog, SRC. The product of the human SRC gene, c-Src, is found to be over-expressed and highly activated in a wide variety of human cancers. The relationship between Src activation and cancer progression appears to be significant. Moreover, Src may have an influence on the development of the metastatic phenotype. This review discusses the data supporting a role for c-Src as a critical component of the signal transduction pathways that control cancer cell development and growth, and provides the rationale for targeting Src in drug discovery efforts.