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As a leading service provider in drug discovery and development, BOC Sciences is fully qualified and committed to providing one-stop PROTAC development services, which has become a promising strategy in the field of small molecular drug discovery. With a comprehensive and advanced platform, we provide Ligand Design for E3 Ligase to customers around the world to meet new drug discovery goals.
Ubiquitin (UB) is a protein modifier that regulates many important cellular processes. In order to initiate protein modification through UB, E1 enzyme activates the C-terminal carboxylate of UB to transfer to the target protein through E1-E2-E3 cascade. E3 is a ubiquitous protein ligase, which directly or indirectly catalyzes the transfer of ubiquitous proteins to target proteins (substrates) to form heteropeptide bonds. By using small molecular ligands to recruit target proteins and E3 ligand, all small molecular PROTAC has achieved rapid target degradation and better cell permeability. Various small molecules that have been shown to bind to several E3 ligase or substrate receptor proteins of the CRL E3 ligase complex, such as MDM2,cIAP1,CRBN and VHL, have been used in PROTAC development.