PROTAC Ternary Complex Assays
Advanced validation services to characterize PROTAC efficiency through ternary complex formation and ubiquitination potential analysis
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- Overview
PROTACs (PROteolysis TArgeting Chimeras) are heterobifunctional molecules that combine a target-binding warhead with an E3 ligase-binding moiety, resulting in the formation of a ternary complex between the target protein and the E3 ligase to induce ubiquitination and degradation.
- Technology Background
It is increasingly clear that the length and composition of the linker connecting the two ligands plays a crucial role in the physiochemical properties and biological activity of PROTACs. The PROTAC field is rapidly evolving and is currently undergoing an important transition from synthetically manageable alkyl and polyethylene glycol linkers to more complex functional linkers.
Traditionally, ternary complex formation has been assessed using cell-free proximity ligand assays such as TR-FRET, ALPHA screening assays, and SPR-based methods.
Key Insight:
LifeSensors offers a wide array of services to validate PROTAC ternary complex, PROTAC ubiquitination and determining binding affinities (SPR).
- Service Highlights
Multiple Ranking Approaches
Multiple approaches to rank PROTAC variants
Fast & Sensitive
Rapid results with high sensitivity detection
Orthogonal Correlation
Correlate activity with orthogonal assays
Complex Evaluation
Evaluate relative population of ternary complexes and correlate with ubiquitination potential
Extensive E3 Ligase Access
Access to ~30 E3 ligases to study selectivity
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- TUBEs
Tandem Ubiquitin Binding Entities