(±)-Nutlin-3 is a small-imidazoline-based mouse double minute 2 (MDM2) protein antagonist which disrupts MDM2-p53 interaction (IC50 = 0.09 μM; Vassilev et al.) MDM2 binds the p53 tumor suppressor protein with high affinity and negatively modulates its transcriptional activity and stability
By disrupting this interaction, (±)-Nutlin-3 therefore promotes the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells with mutated p53 (Vassilev et al.), Gu et al.)
