Background Introduction
(2S,4R)-4-hydroxy-N-[(1S)-3-(methylamino)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxopropyl]-1-[(2R)-3-methyl-2-(3-methyl-1,2-oxazol-5-yl)butanoyl]pyrrolidine-2-carboxamide is a sophisticated small-molecule ligand designed for the modulation of E3 ubiquitin ligase activity in PROTAC (Proteolysis Targeting Chimera) technology. As an advanced and highly selective E3 ligase ligand, this compound is based on well-characterized scaffolds utilized in targeted protein degradation research. Its complex structure enables precise interaction with specific subtypes of E3 ligases, thereby enhancing the toolbox available for next-generation targeted therapeutics and chemical biology studies.
Mechanism
This ligand acts by selectively binding to a particular E3 ubiquitin ligase, facilitating the assembly of a ternary complex when linked to a suitable target protein ligand via a chemical linker. Upon formation of the ternary complex, the E3 ligase is brought into close proximity to the target protein, leading to the transfer of ubiquitin molecules to the target and marking it for proteasomal degradation. The dual recognition moieties and finely tuned conformational properties of this ligand enable improved selectivity and efficiency in targeted protein elimination compared to traditional E3 ligase ligands.
Applications
(2S,4R)-4-hydroxy-N-[(1S)-3-(methylamino)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxopropyl]-1-[(2R)-3-methyl-2-(3-methyl-1,2-oxazol-5-yl)butanoyl]pyrrolidine-2-carboxamide is ideally suited for the development of novel PROTACs leveraging diverse E3 ubiquitin ligase systems. Key applications include:
• Construction of customized E3 ligase ligands in PROTAC development platforms
• Design and synthesis of heterobifunctional degraders targeting previously 'undruggable' proteins
• Investigating E3 ligase-substrate specificity and optimizing ternary complex stability
• Structure-activity relationship (SAR) studies in chemical biology and drug discovery
• Enabling targeted protein degradation for therapeutic target validation and pathway elucidation
This ligand is a valuable asset for researchers engaged in medicinal chemistry, synthetic biology, and drug discovery efforts focused on harnessing the full potential of targeted protein degradation technologies.
CAS No.: 2308497-42-7
![(2S,4R)-4-hydroxy-N-[(1S)-3-(methylamino)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxopropyl]-1-[(2R)-3-methyl-2-(3-methyl-1,2-oxazol-5-yl)butanoyl]pyrrolidine-2-carboxamide](https://resource.bocsci.com/structure/2308497-42-7.gif)
