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Targeted protein degradation: developing a toolbox for the next generation of drug discovery

Twenty years ago, Craig Crews (Yale University; CT USA) and Raymond Deshaies (Amgen; CA USA) had the idea to target a protein of interest for proteasomal degradation by linking it to an E3 ligase, through a heterobifunctional small molecule termed a Proteolysis Targeting Chimera (PROTAC). Today, targeted protein degradation has become one of the hottest fields in drug discovery with its ability to ‘drug the undruggable.’

Over the last 5 years, the field has seen exponential growth, underscoring the need to assess the efficiency of degradation and functional consequences of novel protein degraders.

What will you learn?Who may this interest?Speaker

What will you learn?

  • What targeted protein degradation is and how it is different than current small molecule therapies
  • Considerations of degrader design
  • Current methodologies used to assess degrader efficiency
  • Functional assays to understand the physiological consequences of protein degradation on cell health
  • Alternative mechanisms of protein degradation and novel degraders used to target these systems

Who may this interest?

  • Drug discovery and development scientists
  • Biotechnology research scientists interested in methods for assessing protein degraders

Speaker

Ryan Holly
Staff Scientist, Cell Biology
Thermo Fisher Scientific (MA, USA)

Ryan received his doctorate in Chemistry and Biochemistry from the University of Oregon (OR, USA) with a focus on molecular biology, where he studied the underlying mechanisms of animal cell polarity using biochemical techniques to interrogate the regulation of atypical protein kinase C.

Ryan joined Thermo as an R&D Staff Scientist in 2020 to help drive the development of next-generation protein and cell analysis tools, particularly for imaging and flow cytometry.

Currently, Ryan’s technical leadership includes methods for assessing therapeutic potential and cell function within emerging drug discovery areas such as targeted protein degradation.

This webinar was recorded on Wednesday 24th August 2022

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