p53 is inactivated in all types of cancer either by mutation or inhibition by endogenous negative regulators. The high prevalence of mutant p53 forms in human tumors (50%), associated with poor response to conventional chemotherapy and radiotherapy, makes mutant p53 a highly appealing target for novel cancer therapy. Together, activators of these human proteins are promising antitumor agents. The high complexity of p53 family and the requirement of new drugs that target these proteins led us to the development of yeast-based assays to study the biology and pharmacology of p53 family proteins. Similarly to human cells, mutant p53 is inactive in yeast (Leão M. et al., Exp Cell Res 2015).

To date, an activator of wild-type and mutant p53, with potent antitumor activity in vivo, was identified using the yeast target-directed screening assay (Soares et al., Oncotarget 2016; European patent PCT/IB2014/062617, US patent WO2014/207688 A1).