E3 Ligase Screening and PROTAC Profiling Services
Ubiquitin E3 ligases are the largest family of proteins in human genome (about 800 members). LifeSensors has developed platform of technologies to characterize and profile compounds that modulate E3 ligase activity. The vast library of ubiquitin ligase proteins allows LifeSensors to adapt and customize unique assays that fits your need. Selective ligase inhibitors will not be discovered by testing compounds in one assay platform but will require that the compound be evaluated in number of assays and evaluated for selectivity by screening against the same family of ligases (HECT or Ring Finger).
The LifeSensors proprietary E3 ligase activity assay involves Terbium-labeled Tandem Ubiquitin Binding Entities (TUBEs) that bind to polyubiquitn chains synthesized by E3 ligases. Terbium and fluorescein are a FRET pair, so polyubiquitin chains containing fluorescein-labeled ubiquitin will yield a FRET signal when bound by terbium-TUBE. This signal can be monitored over time in a homogenous, high-throughput format, making it ideal for small-molecule screening.
As a LifeSensors customer you will be consulting with a member of our team to discuss the scope of work relating to your project. LifeSensors will identify the best screening platform for
your project, predict and overcome potential pitfalls, and provide you with
rapid results. Our team’s combined
experience in the ubiquitin field will enable us to understand your project at
a deep level, accelerate your data collection, and aid you in interpreting the
results. We will accelerate and enhance
your drug discovery efforts, allowing you identify the most promising hit
compounds and advance them based on potency and selectivity to cellular and in vivo studies.