Purpose: The fundamental role of gene transcription and the recognition of transcription factors as important control elements of cell growth, differentiation, and programmed cell death (apoptosis) aroused an ever-increasing interest for these proteins as potential pharmaceutical targets for therapeutic intervention in various diseases, among them cancer. EXPERIMENTAL DESIGN-RESULTS: The vast array of information available for their molecular architecture and mode of action in various biological contexts, combined with the new opportunities offered by the flourishing technologies of structure-based drug design, computer-aided modeling, and functional genomics/proteomics, are creating an exciting scenery for the development of a novel generation of highly selective drugs.
Conclusions: This transcription factor-based therapeutic approach may revolutionize the anticancer drug options and will add significantly to the current clinical armamentarium.