Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ubiquitin–proteasome system. The advent of nonpeptidic small-molecule E3 ligase ligands revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity.
PROTAC (Proteolysis-Targeting Chimeras) is a promising approach in drug discovery that involves the use of small molecules to target specific proteins for degradation by the cellular machinery.
E3 ligase ligand is an important biochemical molecule, which plays an important role in cells. It can bind to E3 ligase, thus promoting protein degradation and cell metabolism. In vivo, the stability and activity of E3 ligase ligands are very important for the normal function of cells. Studies have shown that E3 ligase ligands play an important role in cell cycle, apoptosis, DNA repair and other aspects.
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