PROTAC & DUBTAC Drug Discovery

Advanced Targeted Protein Degradation Technology

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PROTACs (PROtein TArgeting Chimeras) artificially hijack the components of the UPS (Ubiquitin Proteasome System) to degrade a target protein, founding the concept of PROTAC Drug Discovery. PROTAC drugs are hetero-bifunctional small molecules that contain two functional ligands connected via a linker; one ligand binds to a target protein and the other ligand binds to an E3 ligase.

Bringing these two entities into proximity theoretically leads to polyubiquitylation and proteasomal degradation of the target protein. However, given the complexity this scenario does not always play out, and the PROTAC discovery platform faces several challenges.

With tremendous excitement surrounding the field of targeted protein degradation, there is an unmet need for functional assays that can study the effects of PROTACs on the ubiquitination of a target(s) and subsequent degradation. Traditional methods such as western blotting and reporter gene assays have been at the forefront to study PROTAC mediated degradation. However, these methods are extremely low throughput, time-consuming, and/or prone to artifacts.

LifeSensors has developed technology to specifically isolate polyubiquitylated proteins from cell lysates and tissues. TUBEs are tandem ubiquitin binding domains (UBDs) that bind poly-ubiquitin with Kds in the nanomolar range. TUBEs have also been demonstrated to protect ubiquitylated proteins from both deubiquitylation and proteasome-mediated degradation, even in the absence of inhibitors normally required to block such activities.

Simultaneous Monitoring

Study PROTAC mediated ubiquitination and degradation simultaneously with our integrated assay platforms

Complete Validation Suite

Comprehensive validation studies to establish binding, ternary complex formation, and cellular degradation

Novel E3 Ligase Experience

Experience with ~30 E3 ligases amenable to PROTAC discovery, expanding beyond traditional systems

Proteomics Characterization

Advanced proteomics to characterize protein degradation and establish selectivity profiles

High-Throughput Screening

Rapid screening of compound libraries with our optimized high-throughput assay platforms

15+ Years Expertise

Deep expertise in ubiquitin-based drug discovery accumulated over 15 years of focused research

With deep and diverse expertise in medicinal chemistry, biochemistry, and cell-biology specializing in ubiquitin based drug discovery for the last 15 years, LifeSensors is proud to offer efficient methods to accelerate your discovery of novel molecules facilitating targeted protein degradation.

Design & Synthesis

Custom design and synthesis of novel PROTACs tailored to your target

Binding Assays

Biochemical and biophysical monitoring of PROTAC binding to targets and E3 ligases

Functional Assays

Comprehensive ubiquitination and degradation assays in cellular systems

PROTAC-mediated ubiquitylation in vitro permits rapid screening of compound libraries and allows simplification of the medicinal chemistry approach to rationally design potent molecules. Your biochemists can focus on new PROTAC targets as LifeSensors will translate its core technologies for in vitro and cellular PROTAC screens.