Recent patents on therapeutic applications of the transcription factor decoy approach

Transcription is considered as an important target of drugs employed in biomedicine. Therefore, novel strategies to inhibit the biological effects of transcription factors (TFs) are of interest, such as targeting promoters with triple-helix-forming oligonucleotides and antisense targeting of mRNAs coding for TFs.

The objective of this review is to describe studies considering inhibition of TF functions with molecules mimicking TF binding sites (transcription factor decoy approach, TFD) and to summarize the patents on possible clinical applications of this approach.

Treatment of cells with TFD molecules leads to inhibition (or activation) of genes regulated by the target transcription factors. The studies and patents on this specific issue have taken in great consideration the delivery strategy, which is a very important parameter. The TFD strategy has been proven effective in vivo. The stability of the TFD molecules in vivo should be carefully considered, as well as the possible toxicity and/or possible effects on innate and adaptive immune response. In order to improve clinical parameters, many patents suggest the use of the TFD molecules in combination with drugs already employed in therapy. We are expecting in the near future relevant clinical trials based on the TFD strategy.