Transcription factors play an important role in regulating gene expression by binding to specific DNA sequences. However, once deregulated several transcription factors can mediate ontogenesis and mediate tumor initiation, promotion and progression. They can regulate a number of genes involved in abnormal proliferation, survival, angiogenesis, and metastasis of tumor cells. A number of pharmacological strategies have been employed to target the aberrant activation of transcription factors to control tumorigenesis. These include approaches to affect their expression, by mitigating protein/protein interactions, and by preventing their DNA binding at specific DNA-interacting sites. This special issue will highlight these strategies and the potential utility of these transcription factors as “druggable targets”.

Keywords: transcription factors; cancer; gene expression; apoptosis; small molecules