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PROTAC Linkers

PROTAC (Proteolysis Targeting Chimeric Molecules) consists of three key components: the protein of interest (POI) binding ligand, the E3 ligase binding ligand, and the linker linking them. To date, the design of most PROTAC molecules has relied on a combination of a known target protein-binding ligand and a small number of E3 ligase-binding ligands.

The linker plays an important role in PROTAC. The characteristics of the linker (type, length, attachment position) can influence the formation of the ternary complex of the ligase:PROTAC:target, influencing the efficient ubiquitination of the target protein and its ultimate degradation. The optimal length of PROTAC linkers has been reported to vary from 12 to 20+ carbons, and the linkers commonly used in the development of PROTAC are PEG linkers, alkyl chains, and alkyl/ethers.

Compared with traditional small molecule inhibitors, PROTAC technology has advantages in activity, selectivity, targeting of "non-druggable" proteins, overcoming drug resistance and drug delivery routes.

Huateng Pharma, as a leading PEG linker supplier, has over 3,000 high purity PEG linkers kept in stock to empower your development of PROTAC.