PROTAC (proteolysis targeting chimeras) is a kind of dual functional molecules. The PROTAC molecule is composed of three parts: one end is a ligand molecule binding to the target protein to be degraded, the other side is a ligand molecule binding to the E3 ubiquitination ligase, and the middle  is connected by a specific Linker. PROTAC molecules connect the target protein to be degraded with E3 ubiquitination ligases through the above ligands, thus enabling the target protein to be ubiquitinated and further degraded by proteasomes. PROTAC, on the other hand, is not degraded by the proteasome and can be reused. 

Compared with common small molecule inhibitors, PROTAC molecule catalyzes protein degradation function in a way independent of occupation-driven, showing excellent high selectivity and low toxicity, and can effectively overcome the resistance of traditional small molecule inhibitors. PEG has been widely used as PROTAC Linker! The monodisperse polyethylene glycol derivative producedSINOPEG is the high quality choice of this kind of PROTAC Linker! Welcome to communicate with us!

PROTAC Linker

PROTACs (Proteolysis Targeting Chimeric Molecules) are heterobifunctional protein degraders and promising targeted therapeutics candidates for cancer. The PROTAC linker connects two functional motifs of a PROTAC, a target protein binder and an E3 ligase recruiter.

The linker plays an important role in a PROTAC. The features of the linker (type, length, attachment position) can affect the formation of ligase:PROTAC:target ternary complex, resulting in influencing the efficient ubiquitination of the target protein and its ultimate degradation. The optimal lengths of the PROTAC linkers are reported varying from 12-carbon to over 20-carbon, and the commonly used linkers in the development of PROTACs are PEGs, Alkyl-Chain and Alkyl/ether.

The peg linker produced SINOPEG is the high quality choice of this kind of protac linker! Welcome to communicate with us!