Protein degrader builiding block (S,R,S)-AHPC-C6-PEG3-butyl Chloride enables the synthesis of molecules fortargeted protein degradation andPROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel–Lindau (VHL)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant chloroalkane for reactivity with a nucleophilic group on a 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 blockswith a pendant chloro group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
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英文别名
Protein degrader building block for PROTAC research, Crosslinker−E3 Ligase ligand conjugate, VH032 conjugate, (S,R,S)-AHPC-6-2-2-6-Cl, (2S,4R)-1-((S)-2-(tert-Butyl)-22-chloro-4-oxo-10,13,16-trioxa-3-azadoco