Pre-Conference Workshop Day

9.00-10.00 Registration & Welcome Coffee

Workshop A

Multiplexed Proteome Dynamics Profiling to Characterize PROTACs & Cullin-ring Ubiquitin Ligases

Tuesday, May 25 | 10:00-12:00 EST

As harnessing E3’s for a viable therapeutic application becomes increasingly evident, characterization and application of identified E3’s is a major stepping stone for the translation into effective degradation. As technology advances, mass-spectrometry-based proteomics has become a powerful tool across drug discovery platforms and has given experts a considerable advantage for drug discovery efforts.

  • Mass spectrometry-based proteomics is a key tool in the characterization of E3 ligases and provides insights into their application for targeted degraders
  • Multiplexed proteome dynamics profiling (mPDP) a combination of dynamic SILAC and tandem mass tags provides insights into proteome homeostasis differentiation regulation of protein synthesis from degradation
  • Application examples of mPDP for Cullin-ring ubiquitin ligases and PROTACs

Workshop Leaders

Markus-Queisser

Markus Queisser
Scientific Director Protein Degradation Group
GlaxoSmithKline

Nico Zinn, Cellzome

Nico Zinn
Group Leader Mass Spectrometry
Cellzome

12.00-1.00 Morning Break & Speed Networking

Workshop B

The Vital Role of Proteomics in Characterizing Novel Protein Degraders

Tuesday, May 25 | 1.00-3.00 EST

Over the last few years, the targeted protein degradation field has developed at an astonishing rate. AstraZeneca has invested substantial resources into keeping up with the pace and as a result has acquired a deep collective knowledge of the unique challenges posed by this relatively new modality. We have come to learn that for PROTACs these include early mechanistic investigations such as characterizing degrader selectivity, determining target protein turnover rates and quantifying the target and requisite E3 ligases in selected models of efficacy and safety. In this workshop, members of the Chemical Biology and Proteomics department at AstraZeneca will review and discuss the impact of mass spectrometry based proteomics on the field of protein degraders and offer their perspectives on where the field of proteomics needs to develop in order to meet these challenges.

  • Assessment of target protein turnover rate via proteomic methods : an essential early activity in the degrader drug discovery process
  • Outlining proteomics strategies to assess E3 ligase (and POI) levels across efficacy and safety models to drive degradation selectivity
  • Discussing global proteomics and genetic knockouts: powerful tools for degrader target identification and validation and for gaining insights into distal pathway effects to inform on degrader selectivity

Workshop Leaders

Katelyn Cassidy

Katelyn Cassidy
Senior Scientist
AstraZeneca

Andrew Zhang, AZ

Andrew Zhang
Team Leader
AstraZeneca

Fiona Pachl, AZ

Fiona Pachl
Senior Scientist
AstraZeneca

Picture1

Meha Singh
Senior Scientist
AstraZeneca

3.00 End of Workshop Day