Ligand Finding and Chemistry Workflows for Targeted Protein Degradation

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Published on ‎01-05-2023 03:38 PM by | Updated on ‎01-05-2023 03:39 PM

Proteolysis-targeting chimeras (PROTACs) are a class of bifunctional molecules which are enabling the development of drugs against targets once considered inaccessible.  PROTACs bring a protein of interest into close-proximity to an E3 ubiquitin ligase, resulting in the degradation of the target protein by the ubiquitin-proteasome system.  The design, synthesis, and optimization of PROTACs can be quite challenging due to their complicated mechanism of action and relatively high molecular weight and size.
This webinar will focus on aspects related to PROTAC discovery and chemistry workflows, such as ligand finding strategies, synthesis optimization, and linker design.  Successful development of bifunctional molecules requires a deep understanding of multiple processes, including biophysical events which dictate induced proximity and how technologies such as DNA-encoded libraries (DEL) can be leveraged to identify binders of target proteins.  These topics will be discussed within the context of PROTAC lead optimization.
Key Learning Objectives:
  • Leveraging DNA-encoded libraries (DEL) to identify binders to target proteins
  • Accelerating the optimization of PROTACs towards preclinical candidate selection
  • PROTAC Discovery and Chemistry Workflows
Who Should Attend:
  • Scientists and researchers interested in protein degradation workflows

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%7B57a06c7a-67f9-4bfb-9b44-af7cbdf47ce8%7D_Kris_100x100Kris Rutten
WuXi AppTec

%7Ba32c5089-747f-4dd9-b894-7102c2aed79b%7D_Jason_100x100Jason Deng
Senior Director, DEL Biology,
WuXi AppTec

%7B84d2252e-4cee-47db-91ef-7f0c7390c7d8%7D_Lei_100x100Lei Zhou
Executive Director,
WuXi AppTec

%7B2ca08302-9b4a-4f05-9567-32b5c3f9f223%7D_AnnThayer_100x100Ann Thayer
Contributing Editor,
C&EN Media Group

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