Description

• Application: Protein degrader building block Pomalidomide-C6-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand and an alkyl-chain crosslinker with pendant amine for reactivity with an acid on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
• Other Notes: Technology Spotlight: Degrader Building Blocks for Targeted Protein DegradationPortal: Building PROTAC® Degraders for Targeted Protein DegradationProteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding LigandsChemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation ReactionIdentification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) DegradationDiscovery of MD-224 as a First-in-Class, Highly Potent and Efficacious PROTAC MDM2 Degrader Capable of Achieving Complete and Durable Tumor Regression
• Legal Information: PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license