cutting-edge researchers describe their efforts to design, synthesize, and evaluate the biological activities of farensyltransferase inhibitors (ftis); geranylgeranyltransferase inhibitors (ggtis) are also discussed as potential anticancer drugs. the authors survey in detail such inhibitors as caax box peptidomimetics, fpp mimics, and bisubstrate transition state analogs, and critically review their uses in combination with radiation and other cytotoxic agents, such as gemcitabine, cisplatin, and taxanes. illuminating and richly detailed, farnesyltransferase inhibitors in cancer therapy constitutes todays standard reference for the pathbreaking use of ftis and ggtis in anticancer therapy and offers basic and clinical investigators a comprehensive treatment of the scientific and medical aspects of farnesyltransferase inhibitors.