PROTAC degraders as chemical probes for studying target biology and target validation
Václav Němec, Martin P. Schwalm, Susanne Müller, Stefan Knapp
Abstract
), confirmation of a proteasome dependent degradation mechanism and, importantly, also kinetic parameters of POI degradation. The kinetic aspects are particularly relevant for PROTACs that harbor covalent binding moieties. Here, we review recent progress in the development of assay systems for PROTAC characterization and suggest a set of criteria for PROTACs as high quality chemical probes.
Topics & Concepts
Biochemical engineeringComputational biologyProteolysisNanotechnologyChemistryComputer scienceBiologyBiochemistryMaterials scienceEngineeringEnzymeProtein Degradation and InhibitorsPeptidase Inhibition and AnalysisUbiquitin and proteasome pathways