En

April 23-26, 2023Oegstgeest, The Netherlands

Course Outline:

In the last ten years there have been significant developments in the field of designing small molecule protein degraders both as chemical tools and clinical candidates. These degraders can offer major advantages over small molecule inhibitors as a therapeutic strategy by achieving more complete target inhibition and by expanding the potentially druggable proteome. This course aims to provide opportunities for in depth discussions on the key aspects of PROTAC design and development for medicinal chemists. The course will introduce small molecule protein degraders, including PROTACs and molecular glues, and give a detailed overview of the novel technologies used to characterise protein degradation biophysically and in living cells. The course will finish with a series of medicinal chemistry case studies, including the discovery of clinical small molecule protein degraders.

Confirmed Speakers:

The Ternary Complex E3-Degrader-Target: Biophysical Binding Assays and Structures

  • Dr Chun-wa Chung (GSK, United Kingdom)

Introduction to Small Molecule Degraders: PROTACS and Molecular Glues

  • Prof. Alessio Ciulli (University of Dundee, United Kingdom)
  • Dr Suzanne O'Connor (University of Dundee, United Kingdom)

Importance of Degradation Kinetics and Mechanisms for Development of Potent Therapeutic Degraders

  • Dr Danette Daniels (Foghorn Therapeutics, United States)

The Current & Future Clinical Landscape of Molecular Degraders of Disease-Causing Proteins

  • Dr Ingo Hartung

Medicinal Chemistry Optimisation of Small Molecule Degraders

  • Dr Andrea Testa


Course Organisers:

  • Prof. Alessio Ciulli (University of Dundee, United Kingdom)
  • Prof. Suzanne O'Connor (University of Dundee, United Kingdom)

Local Organiser:

  • Prof. Laura Heitman (Leiden University, The Netherlands)