Proteomics in Drug Discovery: Webinar 2 - Proteomics Driving New Therapeutic Approaches

Proteomics in Drug Discovery: Expanding the Druggable Proteome

Over 90% of approved drugs target proteins – yet many disease-relevant proteins remain inaccessible. Advances in both high-throughput and mass-spectrometry based proteomic methods enable both whole proteome coverage and deep characterisation of specific proteins.

Despite progress, proteins pose unique challenges – ranging from their complexity and post-translational modifications to analytical and computational limitations. Many promising proteins remain “undruggable” due to structural or functional barriers.

This begs the question: How can we best leverage the proteomic techniques we have available to further support our understanding of diseases and support drug discovery?

In this webinar series, you will:

• Discover how drug hunters are translating proteomics into novel therapeutics
• Explore how different proteomics methods illuminate disease biology and guide target identification
• See real-world case studies using chemoproteomics, structural proteomics and AI

Webinar 2: Proteomics Driving New Therapeutic Approaches

Wednesday 30th of April, at 3pm BST, 4pm CEST, 10am EST

This webinar will focus on how advances in proteomics are accelerating drug target identification, supporting the design of drugs, giving rise to new modalities, and providing key insights into whether these drugs will be effective.

Talk 1: POLYPHARM-AI: Harnessing Molecular Drivers of Comorbidity for Precision Drug Discovery

• Explore how AI can decode the molecular drivers of complex, non-Mendelian diseases – predicting mechanisms of action, therapeutic targets, side effects and efficacy
• Get greater coverage of protein targets, covering the human proteome – includes all major gene families, including receptors, enzymes and most membrane proteins.

Jeffrey Skolnick, Regents’ Progressor, Georgia Institute of Technology

Talk 2: Chemical Proteomics to Develop Drugs with Novel Mechanisms of Action

• Most drugs bind to similar types of proteins and share similar mechanisms of action, which limits our ability to develop safe and effective therapeutics
• Chemical proteomics is a powerful technique to discover novel binding sites and guide the optimization of drugs with unique mechanisms of action
• This presentation will outline how we applied chemical proteomics to develop an allosteric inhibitor of JAK1, an important drug target in chronic inflammatory and autoimmune diseases.

Madeline Kavanagh, Assistant Professor of Chemical Biology, Leiden University

Talk 3: Impact of MS-based proteomics on the journey to discover KRAS degraders

• Relevance of MS-based proteomics for PROTACs development
• Application of global proteomics, phosphoproteomics and targeted proteomics to assess degrader selectivity and downstream signalling effect
• Using MS-based proteomics for characterizing KRAS degraders

Ilaria Puoti, Cellular and Proteomic Scientist, University of Dundee

Previous webinars in the series:

Webinar 1: Unlocking The Power of Proteomics for Drug Discovery

Now available on-demand

This webinar will explore how cutting-edge proteomics technologies are shaping the future of drug development. Topics include mass spectrometry, covalent chemoproteomics, and thermal proteomic profiling.

Talk 1: Druggable Proteome Through Covalent Chemoproteomics

• The application of covalent fragment screening in cells by chemoproteomics offers potential for expansion of the liganded proteome.
• In collaboration with the Francis Crick Institute, we have developed a protocol to enable rapid and robust profiling of fragment-proteins interactions in cells to expand the druggable proteome and unlock therapeutic opportunities.

Jacob Bush, Director, Chemical Biology, GSK

Talk 2: Thermal Proteomic Profiling for Drug Discovery Applications

• Thermal Proteomic Profiling (TPP) is emerging as a powerful tool for identifying drug-protein interactions in both eukaryotic and bacterial systems, offering insight into efficacy and mechanism of action.
• This talk will describe the principle of cellular thermal shift assay (CETSA) and thermal proteome profiling (TPP)
• Different TPP formats and how they can be used
• Applications of TPP for target identification (eukaryotic and bacteria)

Andre Mateus, Assistant Professor, Umeå universitet

Talk 3: Investigating the Cell-Membrane Proteome of Cancer and Brain TME Cells for Advancing the Drug Target Discovery Process

• The role of proteomics in profiling the cell-membrane and secretome landscape of cancer and TME cells
• Intercellular crosstalk supportive of aberrant and metastatic proliferation
• Changes in downstream signaling pathways upon targeting cell-membrane receptors
• Exploring the cell-membrane PPIs for promoting novel therapeutic avenues

Iulia Lazar, Professor, Biological Sciences, Virginia Tech