Next-Generation Drug Discovery: Leveraging E3 Ligases for Targeted Protein Degradation
Date: Wednesday, August 19, 2020
Time: 9:00am PDT / 12:00pm EDT
Duration: 1 hour
E3 ligases have emerged as pivotal targets for drug discovery using the promising new paradigm of targeted protein degradation. This new paradigm includes both ligand binding-directed “reprogramming” of E3 substrate specificity approaches and a more directed approach, using small molecule proteolysis-targeting chimeras (PROTACs), to selectively degrade disease-driving proteins. As there are hundreds of diverse putative E3 ligases with differentiated tissue expression, this new paradigm may well define a next dimension of precision medicine defined by an axis of tissue-specific activity.
While there have been some early successes, the E3 drug discovery field has experienced significant challenges developing a standardized biochemical ligand binding assay platform. A platform is required that:
1) Can measure ligand binding across the E3 family using a standardized method enabling “apples to apples” comparisons
2) Is highly scalable and rapid
3) Has an exquisite dynamic range for the measurement of accurate KD values as low as single digit picomolar (pM)
In this webinar, Eurofins Discovery will present the novel E3scan™ technology that overcomes and meets each of these challenges. The E3scan platform, based upon the industry-leading KINOMEscan® technology, has been successfully applied to diverse E3 ligases, including CRBN, VHL, MDM2, cIAP1, cIAP2, and XIAP, with many other E3 assays in progress. Learn how the E3scan platform enables accelerated screening and SAR analysis in the E3 drug discovery field, with rapid turnaround times for discovery library screens and the largest assay panel available on a single technology platform.
This webinar provides an overview of a new platform for E3 ligases and targeted protein degradation.
We will share and review:
- The development and validation of the E3scan platform
- Our robust & high throughput assay library
- Correct control inhibitors testing
- Tight binding limits
- Assays that can support screening and SAR campaigns
Speaker:
Ksenya Cohen Katsenelson, Ph.D.
R&D Group Leader
Eurofins Discovery