E3 TR-FRET Biochemical Assay
Advanced high-throughput screening solutions for E3 ligase drug discovery powered by our proprietary TUBE technology
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- E3 TR-FRET Biochemical Assay
E3 ligases remain among the most difficult enzyme targets to assay and discover potent therapeutic applications, possibly due to their dependence on upstream E1 and E2 enzymes for the activation and transfer of ubiquitin. As a result, traditional assays for E3 ligases are complex and prone to off-target false positives.
At LifeSensors, we have developed reagents and assays encompassing both traditional and non-traditional approaches for E3 ligase screening and profiling. Quickly distinguishing true hits from false positives, developing structure-activity relationships, and establishing rank order potency from purified enzymes to cellular models are key steps to success. LifeSensors brings together the tools and expertise necessary to overcome the many pitfalls in the E3 ligase field.
- Assay Technology: TUBE-powered TR-FRET Detection System
Our E3 TR-FRET detection system utilizes our TUBE technology to monitor E3 ligase activity by fluorescence signal. This assay involves donor-labeled TUBEs that bind to acceptor-labeled polyubiquitin chains synthesized by the target E3 ligase. When donor-labeled TUBEs come in close proximity to polyubiquitin chains containing acceptor-labeled ubiquitin will yield in a FRET signal. This signal can be monitored over time in a homogenous, high-throughput format, making it ideal for small-molecule screening to find tool compounds for E3 ligases.
Homogenous Format
Real-Time Monitoring
High-Throughput
- Service Highlights
High-Throughput Screening
Using compound libraries to discover novel inhibitors/activators/binders for E3 ligases
Automated Liquid Handling
Amenable to large library screening with precision and efficiency
Extensive E3 Ligase Access
~50 E3 ligases available for discovery and selectivity studies in rapid homogenous assay format
Customized Compound Libraries
Access to ligase-centric small molecule libraries for reference in drug discovery efforts
Ultrasensitive Detection
Robust signal-to-noise ratio powered by proprietary TUBE technology
Extensive UPS Experience
Complementary biochemical and biophysical validation studies to exclude off-target hits
- Resources
Unlocking the Impact of E3 Ligases in Drug Discovery
Comprehensive guide to E3 ligase targeting and screening methodologies
- Related Products
- E1-E2-E3 Assays
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- E1-E2-E3 Ligases
- TUBEs