PROTACs
Proteolysis targeting chimera (PROTAC) is a paradigm shifting novel drug discovery strategy providing opportunity to transform the way small molecule drug discovery programs are planned and executed. PROTAC reduces the need for target occupancy as necessitated with traditional small molecule inhibitors and is being actively explored for Oncology and Inflammatory Disorders.
Eviogen can support you from the very start of your protein degradation journey all the way through to the clinic. We have a pool of scientists with extensive experience working in the space of heterobifunctional degraders. We can support our clients from early discovery to candidate selection, for multiple targets, specifically oncology and inflammation disorders .
Key assays to support degrader programs need to take into consideration the key aspects of ubiquitin proteasomal machinery and E3 ligases involved to make hetero-bifunctional degraders or molecular glues.
Binding assay/Binding:
SPR, TR-FRET/AlphaLISA, fluorescence polarization and CETSA based competitive binding assay to evaluate binary binding affinity
Ternary complex formation assay:
AlphaScreen®, AlphaLISA®, or TR-FRET based assay to determine the formation of ternary complex between PROTAC, E3 ligase and target protein .
Protein degradation assay:
Reporter complementation assays with customized stable cell lines to determine intracellular protein degradation in presence of degraders and DC50 and Dmax generation
