The Future of Drug Discovery: A Symposium on PROTACs from Lead Optimization to Pharmacokinetics and Metabolite Identification
PROteolysis-Targeting Chimeras (PROTACs) represent a novel approach in drug design that offers significant advantages, including the ability to target proteins and prosecute therapeutic concepts previously considered beyond inhibitors. PROTACs are increasingly established within pharmaceutical development pipelines, advancing from early-stage discovery into clinical trials. Their unique structure introduces new mechanisms for targeted protein degradation, providing opportunities for more effective and sustained treatment options.
We are pleased to share this symposium as an educational opportunity to learn about structure, mechanism and analytical characteristics of PROTACs.
Take a look at the symposium lineup:
Keynote Presentation: PROTACs: From Hit ID to in vivo Efficacy
- Dr William Farnaby, Principal Investigator, Centre for Targeted Protein Degradation, University of Dundee, UK
This educational presentation will focus on leanings from a recent disclosure on the discovery of panKRAS PROTACs as part of a collaboration between the University of Dundee Centre for Targeted Protein Degradation and Boehringer-Ingelheim (Popow et al., Science 385, 1338–1347 (2024)). Dr Farnaby will use the case study to expand key elements of PROTAC discovery and optimization.
Optimization of an end-to-end workflow for bioanalytical quantification of PROTACs
- Nikunj Tanna: Principle Scientist, Waters Corporation, US
A Comparison of Pharmacokinetic Parameters of Gefitinib and Gefitinib based PROTACs- 3 by optimised LC-MS/MS
- Amy Bartlett: Principle Market Development Manager, Waters Corporation, UK
Solving the Challenge of Protein Degrader Metabolite ID: The Metabolic Fate of PROTACs based Gefitinib in the Rat
- Dr Rob Plumb: Consultant Scientist, Waters Corporation, US
Key Learning Points
- The latest in PROTACs design and optimization for therapeutic applications.
- Cutting-edge techniques for bioanalysis and pharmacokinetics.
- In-depth insights into metabolite profiling of PROTAC-based drugs.
Presenter: Dr William Farnaby (Principal Investigator, Centre for Targeted Protein Degradation, University of Dundee, UK)
Dr William Farnaby is a Principal Investigator within the University of Dundee Centre for Targeted Protein Degradation. He has recently been awarded EPSRC New Investigator and Wellcome Trust Early Career awards, supporting his long-term vision for using induced proximity chemistry to address and understand diseases of the central nervous system. Previously, Dr William Farnaby led a large Targeted Protein Degradation drug discovery team, as part of a collaboration between the University of Dundee and Boehringer-Ingelheim. He has been a key contributor to major, highly cited advances in the field of targeted protein degradation and in particular in the area of structure based PROTAC design. Prior to this, he co-invented multiple clinical candidates for CNS diseases as a medicinal chemist at Takeda, including the CH24Hi drug for Dravet syndrome, Soticlestat.
Presenter: Nikunj Tanna (Principle Scientist, Waters Corporation, US)
Nikunj Tanna is a Principal Scientist at Waters corporation. His role at Waters focuses on complete workflow solutions for quantitation of small and large molecules. He has a particular emphasis on sample preparation and automation for bioanalysis, ADME and DMPK applications. In his previous role as General supervisor and Bioanalytical scientist at Berg LLC, he led a clinical diagnostics team focused on providing PK support for the company’s small molecule drug candidates.
Presenter: Amy Bartlett (Principle Market Development Manager, Waters Corporation, UK)
Amy has long established expertise in quantitative LC-MS/MS analysis and throughout her 18 years at Waters, has led teams of experienced applications scientists providing application and scientific support to Waters' customers across a broad range of markets, applications, and technologies. Prior to this, Amy worked for several years in the pharmaceutical industry in Analytical Development and Discovery DMPK roles.
Presenter: Dr Rob Plumb (Consultant Scientist, Waters Corporation, US)
Dr Plumb has published over 160 papers on the subject of HPLC/MS and NMR for bioanalysis, metabolomics and metabolite identification. After obtaining Ph. D in Analytical Chemistry in 1999, he worked at Glaxo Research and Development Drug Metabolism Department. During his time at Glaxo and later GlaxoWellcome, he continued his research in liquid chromatography combined with NMR and mass spectrometry for metabolite identification. In 2001, he moved to Waters Corporation in Milford, MA, USA where he has worked in R&D, pharmaceutical marketing, metabolic phenotyping and discovery omics. He is currently a scientific advisor for the Research, Discovery and Analytical Testing function.
