(S,R,S)-AHPC-PEG3-NH2

Background Introduction

(S,R,S)-AHPC-PEG3-NH2 is a specialized E3 ligase ligand-linker conjugate widely used in the development of PROTACs (Proteolysis Targeting Chimeras). PROTAC technology is revolutionizing targeted protein degradation by leveraging the ubiquitin-proteasome system to eliminate disease-causing proteins, offering a promising therapeutic strategy for various diseases including cancer, neurodegenerative disorders, and immune conditions.

Mechanism

(S,R,S)-AHPC-PEG3-NH2 functions as a bifunctional molecule, where the AHPC moiety selectively binds to the Von Hippel-Lindau (VHL) E3 ligase. The PEG3 linker provides optimal spatial orientation and flexibility, enabling the other end of the molecule (the amine group, NH2) to be conjugated with a ligand targeting the protein of interest (POI). When incorporated in a PROTAC structure, this conjugate recruits the VHL E3 ligase to the POI, facilitating its ubiquitination and subsequent degradation by the proteasome.

Applications

(S,R,S)-AHPC-PEG3-NH2 is a versatile building block for the synthesis of novel PROTAC molecules targeting a wide range of undruggable proteins. It is ideal for use in drug discovery and development, mechanistic studies of protein degradation, and generation of chemical biology tools. Researchers leverage (S,R,S)-AHPC-PEG3-NH2 to develop selective protein degraders, enabling advanced therapeutic strategies and functional studies in oncology, neurology, and immunology.

• PEG3 linker provides improved aqueous solubility and enhanced pharmacokinetic properties for optimal PROTAC performance.
• Amine-terminated ligand is precisely designed for efficient conjugation and targeted recruitment of the VHL E3 ligase.