E3 Ligase Ligand-Linker Conjugate


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The E3 ligase ligand-linker conjugate is part of proteolysis targeting chimera (PROTAC) that targets proteolysis and combines the E3 ubiquitin ligase ligand and a linker. After binding to the ligand of the target protein (such as JQ1 of BRD4 protein, Molibresib of BET protein), these conjugates can be used to build PROTAC for ubiquitination and degradation of proteins. Currently, several PROTACs have been found to exhibit good biological activity by specifically targeting BET, estrogen receptor (ER) and androgen receptors (AR).

E3 Ligase Ligand-Linker Conjugate

A PROTAC molecule includes two key domains: a domain that specifically binds to the target protein that needs to be degraded, and a domain that binds to E3 ubiquitin ligase. Two domains are connected by specific linkers. The PROTAC molecule links the protein to be degraded to the E3 ubiquitinated ligase through the two key domains described above, thereby achieving polyubiquitination and proteasome degradation of the target protein. Common E3 ligase ligands ((VHL) ligands, MDM2 ligands, Cereblon (CRBN) ligands and cIAP1 ligands) can be coupled to different linkers (PEG, alkyl chain, alkyl / ether, etc.). The use of the high-quality E3 ligase ligand-linker conjugate is very convenient and time-saving. Researchers can use this conjugate to design and synthesize various new PROTACs (such as ARV-825, dBET1, MT-802, etc.). For example: halidomide-O-amido-C4-N3 is a synthetic E3 ligase ligand-linker conjugate, which contains Thalidomide-based cereblon ligand and a linker.

Different E3 ligase ligand-linker conjugate will provide different selectivity, which can expand the application of PROTAC in the treatment for cancer, autoimmune disease, and inflammation. E3 ligase ligand-linker conjugate accelerates the PROTAC discovery. Researchers usually use techniques such as immunoblotting and mass spectrometry to measure protein levels to screen for active PROTACs, and then combine these molecules with E3 Ligase Ligand-Linker Conjugate to build a PROTAC. E3 Ligase Ligand-Linker Conjugate Kit is available on the market, which greatly shortens the research time. Other than containing the E3 Ligase Ligand-Linker Conjugate, the kit also provides a series of compounds required in the PROTAC technology.

Reference:

  1. Xiuyun Sun et al. PROTACs: great opportunities for academia and industry. Signal Transduction and Targeted Therapy(2019).

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