MDM2-PROTAC versus MDM2 Inhibitors: Beyond p53 Reactivation
Sylvain Peuget, Galina Selivanova
Abstract
SUMMARY: In this issue of Cancer Discovery, Adams and colleagues present the discovery of a potent PROTAC, MDM2 degrader, which activates wild-type p53 leading to cancer cell death. Importantly, in a number of in vitro and in vivo experiments, the authors show that the depletion of MDM2 by PROTAC kills p53-mutant or p53-null cancer cells. See related article by Adams et al., p. 1210 (5).
Topics & Concepts
Mdm2CancerIn vivoCancer researchBiologyProgrammed cell deathDrug discoveryCancer cellMutantComputational biologyBioinformaticsCell cultureApoptosisGeneticsGeneProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysCancer-related Molecular Pathways