E3 Ligase Drug Discovery Services

LifeSensors offers many custom services to the drug discovery industry and this page will cover those services for targeting E3 ligases.

The basic services that we offer for E3 ligases are as follows:

  1. E3 ligase expression – View the growing list of E3 ligases in our catalog, or ask about our protein on demand service for any ligase (or other protein) that you would like expressed and purified.
  2. E3 ligase activity assays, in vitro
    1. ELISA-based autoubiquitylation or substrate ubiquitylation
    2. TR-FRET autoubiquitylation or substrate ubiquitylation
    3. E1/E2 assays to confirm that inhibitors do not hit the E1 or E2 enzymes
  3. Binding affinities of E3 ligase inhibitors
    1. Thermal shift assay
    2. Surface plasmon resonance (SPR)
  4. E3 substrate ubiquitylation assays, in cells
    1. ELISA-based substrate ubiquitylation
    2. AlphaLISA®-based substrate ubiquitylation

Also choose from our growing list of ubiquitin pathway small molecule inhibitors.  These assays take you from ligase expression to low- or high-throughput in vitro assays to cellular assays, allowing you to confirm compound activity against your target ligase in multiple contexts and formats.

We have validated these assays by targeting well established model ligases, and some examples of the initial data can be found here:

TR-FRET ligase titration

UbiQuant S inhibition data