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
T17920	(S,R,S)-AHPC-PEG1-N3	(S,R,S)-AHPC-PEG1-N3 (E3 ligase Ligand-Linker Conjugates 3) 是 E3 连接酶配体和linker 连接得到的偶联物，包含基于 (S,R,S)-AHPC 的 VHL 配体和 1 个单元 PEG linker。