Exploring Targeted Protein Degradation: Concepts and Applications - Sponsored by Promega

Targeted Protein Degradation (TPD) is an innovative approach in drug discovery that harnesses the cell's natural protein disposal system to eliminate disease-causing proteins. This short course provides a comprehensive overview of TPD, focusing on its mechanisms, applications, and potential in addressing targets that cannot be inhibited with traditional approaches (so-called "undruggable").

Participants will learn about the ubiquitin-proteasome system and key components of TPD, including proteolysis-targeting chimeras (PROTACs), molecular glues, and other modalities. The course will cover the design and optimization of protein degraders, exploring E3 ligase selection, target protein ligands, linker chemistry, and methods for assessing degrader compound properties. Advantages of TPD over conventional small molecule inhibitors will be discussed, along with case studies in various therapeutic areas. Practical aspects of TPD drug discovery, including screening methods and in vitro/in vivo evaluation, will also be addressed.

Additionally, the course will touch upon emerging TPD strategies and explore the current state of TPD in clinical development. Participants will gain a solid understanding of TPD's potential to revolutionize drug discovery and its implications for treating a wide range of diseases. This course is designed for researchers, drug discovery scientists, and graduate students interested in expanding their knowledge of targeted protein degradation and its applications in modern drug development.

Who Should Attend?

• Drug discovery scientists
• Graduate students
• Anyone interested in expanding their knowledge of targeted protein degradation and its applications in modern drug development

Course Benefits

• Acquire a solid understanding of TPD's potential to revolutionize drug discovery.
• Learn enhanced skills in the design and optimization of targeted protein degraders.
• Gain insights into the implications of TPD for treating a wide range of diseases.

Course Topics

The course will cover:

• key components of TPD, including the ubiquitin-proteasome system, proteolysis-targeting chimeras (PROTACs), molecular glues, and other modalities.
• E3 ligase selection, target protein ligands, linker chemistry, and various methods for developing effective degrader compounds.
• practical aspects of TPD drug discovery, including screening methods and in vitro/in vivo evaluation.
• emerging TPD strategies and the current state of TPD in clinical development.

Instructors

A full instructor list will be posted soon.