Activation of the p53 tumour suppressor is predicted to have therapeutically beneficial effects. Many current anti-cancer therapies activate the p53 response via DNA damage. Non-genotoxic activation of the p53 pathway would open the way to long-term and possibly prophylactic treatments. We have established a simple protocol to screen small compound libraries for activators of p53-dependent transcription, and to select and characterise the most interesting hits, which include non-genotoxic activators. These compounds or their derivatives are of potential clinical interest. This approach may also lead to the identification of novel p53-activating compound families and possibly to the description of novel molecular pathways regulating p53 activity.
Berkson, R. G., Hollick, J. J., Westwood, N. J., Woods, J. A., Lane, D. P., & Lain, S. (2005). Pilot screening programme for small molecule activators of p53. International Journal of Cancer, 115(5), 701-710. https://doi.org/10.1002/ijc.20968