Ligand for E3 Ligase

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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, notably for von Hippel–Lindau (VHL) and cereblon (CRBN), revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity.During the past few years, these efforts have resulted in improved small-molecule-based PROTACs recruiting cereblon (CRBN), von Hippel–Lindau (VHL), and inhibitors of apoptosis proteins (IAPs). By leveraging these small-molecule E3 ligase ligands, the field has since extensively demonstrated that PROTACs can induce degradation of a variety of proteins, even at sub-nanomolar concentrations, and has validated their applications not only as biological tools but also as a new chemical modality for treatment of diseases in the clinic.

产品编号	产品名称
T17916	Pomalidomide-PEG4-C2-NH2	Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) 是一种合成的 E3 连接酶配体- linker 偶联物，用于 PROTAC 技术中。