A two-faced selectivity solution to target SMARCA2 for cancer therapy
John D. Harling, Christopher P. Tinworth
Abstract
Two new studies exploring PROTAC-mediated degradation of SMARCA2 for cancer therapy solve an apparently intractable selectivity challenge with SMARCA4 by utilising the requirement for a productive ternary complex between the protein, PROTAC and ligase complex.
Topics & Concepts
Ubiquitin ligaseCancer therapyTernary complexSelectivityCancer researchChemistryComputational biologyCancerDegradation (telecommunications)UbiquitinComputer scienceBiochemistryBiologyGeneGeneticsEnzymeCatalysisTelecommunicationsProtein Degradation and InhibitorsPeptidase Inhibition and AnalysisChromatin Remodeling and Cancer