Click chemistry enables rapid development of potent sEH PROTACs using a direct-to-biology approach
Julia Schoenfeld, Nick Liebisch, Steffen Brunst, Lilia Weizel, Stefan Knapp, Aimo Kannt, Ewgenij Proschak, Kerstin Hiesinger
Abstract
). Thus, we established a scalable, cost-effective and time-saving D2B platform for the discovery of PROTACs in very small quantities. This methodology is particularly suitable for early-stage screening and hit validation assessing the degradability of a target.
Topics & Concepts
ChemistryEpoxide hydrolase 2Click chemistryCombinatorial chemistryDrug discoveryCycloadditionComputational biologyCell permeabilityNanotechnologyDegradation (telecommunications)HomogeneousAnalyteChemical synthesisProtein Degradation and InhibitorsClick Chemistry and ApplicationsUbiquitin and proteasome pathways