Enabling Protein Degradation Drug Discovery

Custom Drug Discovery Services

As pathways and functions are unravelled, new and attractive ubiquitin/Ubl cascade drug discovery targets are coming to light with relevance across many key therapeutic areas.

We have now successfully developed and delivered a number of HTS-compatible assays and kits enabling leading pharmaceutical companies to conduct screening campaigns against ubiquitin cascade targets (DUBs, E3s and others) of high therapeutic value.

Projects completed include the design and development of E3 ligases HTS assays and the delivery of a reagent kit to conduct a screening campaign versus 1m+ compounds.  Various hit deconvolution assays have also been delivered to dissect the mechanism of action of the hits identified from these screens.

Below is a summary of some of the assays we have developed so far and others that are under development.

HTS Assay Development Status E3 Ligase Family Assay Type
IDOL/LDLR Ready RING Substrate Ubiquitylation
IDOL/MRLC Ready (Deconvolution assay) RING Substrate Ubiquitylation
IDOL Ready RING Auto-ubiquitylation
MuRF1/ MyLC1 Ready RING Substrate Ubiquitylation
MuRF1/ MyLC2 Ready (Deconvolution assay) RING Substrate Ubiquitylation
MuRF1 Ready RING Auto-ubiquitylation
BIRC2 Ready IAP-RING Auto-ubiquitylation
ITCH in development HECT Auto-ubiquitylation
RNF8 in development RING Auto-ubiquitylation
RNF11 in development RING Auto-ubiquitylation
SMURF1 in development HECT Auto-ubiquitylation
CHIP Ready U-BOX Auto-ubiquitylation

 

The combination of our extensive experience in working with these pathways and our access to one of the widest collections of Research Tools allows our Custom Assay Development team to support pharmaceutical and biotechnology companies in translating discoveries into lead programmes.

Many of our assays have been developed from first principles starting with little or no data from the literature to guide the construction of the assay.  Ubiquigent can research, design, manage and deliver the entire programme to help you to achieve success in your ubiquitin system HTS campaigns.

To learn more about our custom drug discovery services and to discuss your specific requirements, either email us at services@ubiquigent.com or contact us here.