Terphenyl-Based Helical Mimetics That Disrupt the p53/HDM2 Interaction

摘要

The p53 protein plays a key role in the apoptosis pathway.Increased expression of wild-type p53 in stressed cells leads to cell-cycle arrest or apoptosis,whereas in normal cells p53 is present at very low levels owing to regulation by human double minute 2(HDM2),which promotes the degradation of p53 through an ubiquitin-dependent proteasome pathway.The p53 protein is found in a mutated or inactive state in over 50% of cancerous tumors.