A 410099.1 amide-PEG3-amine-Boc

Background Introduction

A 410099.1 amide-PEG3-amine-Boc is a specialized E3 ligase ligand-linker conjugate designed for use in targeted protein degradation technologies, particularly PROTAC (Proteolysis Targeting Chimera) development. As interest in targeted protein degradation grows, such linkers play a crucial role in connecting E3 ligase recruiting ligands with ligands for proteins of interest, forming functional PROTACs. The incorporation of PEG3 (triethylene glycol) enhances solubility and flexibility, while the Boc-protected amine provides convenient functionalization for synthetic manipulation.

Mechanism

A 410099.1 amide-PEG3-amine-Boc operates as a modular component in the synthesis of PROTAC molecules. The molecule features an E3 ligase ligand, a PEG3 linker providing optimal spacing and solubility, and a terminal amine protected by a Boc group. Upon removal of the Boc protecting group, the amine can be selectively conjugated to small molecule inhibitors, peptides, or other proteins of interest. The resulting bifunctional molecule recruits the E3 ubiquitin ligase complex to the target protein, promoting ubiquitination and subsequent proteasomal degradation. This targeted degradation approach enables precise control over protein homeostasis, which is invaluable in functional studies and drug discovery.

Applications

A 410099.1 amide-PEG3-amine-Boc is broadly applied in the synthesis of PROTACs for targeted protein degradation research. It facilitates the rapid development of novel PROTAC degraders against disease-relevant targets, particularly in oncology, neurodegenerative diseases, and immunology. The Boc-protected amine allows for versatile synthetic strategies, making this conjugate suitable for high-throughput screening, mechanism-of-action studies, and the development of next-generation therapeutics. By enabling the design of highly selective PROTACs, it accelerates the discovery and validation of new drug targets and expands the potential treatment landscape for previously undruggable proteins.

• Amide-PEG3-amine-Boc provides excellent aqueous solubility for improved PROTAC bioavailability.
• Versatile amine-Boc group enables efficient conjugation with diverse E3 ligase ligands and target proteins.