Ubiquitination Screening & Profiling

Ubiquitination is a post-translational modification in which one or more ubiquitin proteins are added to a substrate protein by a stepwise reaction requiring the sequential activity of 3 enzymes: ubiquitin-activating enzymes (E1), ubiquitin-conjugating enzymes (E2), and ubiquitin ligases (E3). While originally described as the process that labels proteins for degradation by the proteasome, ubiquitination was later found to have distinct functions such as altering protein localization, modulation of protein-protein interaction, and activation or inactivation of target proteins. In addition to the highly studied proteasomal degradation pathway and autophagy, ubiquitin modifications have been linked to the regulation of other important cellular processes, including inflammation, response to stress or viral infections, DNA repair, and stem cell differentiation. Dysfunctions in the pathway are known to result in developmental, neurodegenerative, immunological and metabolic disorders, as well as cancer.

Deubiquitinating enzymes (DUBs) remove ubiquitin molecules from proteins, counteracting ubiquitination effects. Since the balance between conjugating and deconjugating systems determines the result of the various ubiquitination signals, both processes are now targets for therapeutics that either enhance or prevent ubiquitination. Notably, the ubiquitin-driven proteasomal pathway is now used to specifically target proteins for degradation using Proteolysis Targeting Chimeras (PROTACs®) as a therapeutic approach.

Ubiquitination Screening and Profiling Services

We offer an extensive selection of screening and profiling services for ubiquitinating and deubiquitinating enzymes. Our team of experts, using our in-house developed biochemical assay kits, can provide:

  • Screening for activity and selectivity across our full panel or just select targets
  • Determination of IC50
  • Determination of functional E2 partners for your E3 ligase of interest using our ChoosE2-Opti™ Intrachain TR-FRET Assay Kit
  • Project guidance and questions answered in a timely manner
  • Delivery of detailed results promptly and on time

If follow-up studies are required, we can provide the same active proteins as the ones used in our assays.

Learn more about the process and deliverables.

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Note: Not all targets will have a commercially available reference control. Please inquire with our team if you need to furnish your own controls for specific targets.