DAY TWO I MARCH 27, 2025

8:00 am Check In & Morning Refreshments

8:50 am Chair’s Opening Remarks

Discovering Biophysical Frontiers: The Emerging Techniques & Technologies to Enhance Drug Discovery

9:00 am Computationally Guided Design & Testing of De Novo Miniproteins

Synopsis

  • Using generative AI we design 45-60 amino acid miniproteins to bind to desired targets
  • We developed a high throughput production platform to express, purify and characterize thousands of unique miniprotein sequences
  • Data we generate is used to further optimize the computational tools and improve affinity and developability of hits

9:30 am Tailored Biophysical Methods For Soluble Enzymes & Transmembrane Receptor Targets

  • Arne Rufer Expert Scientist & Science & Technology Lead, Lead Discovery, Roche

Synopsis

  • Introduction to the enzymes and transmembrane receptor targets being studies by Roche
  • Complementary structural, direct binding and enzyme kinetics data for elucidation of small molecule mode of action
  • Chemical probe approaches facilitating characterization of GPCR-ligand interactions 

10:00 am Morning Break & Networking

10:45 am Membrane Proteins & the Development of Assimilation Proximity Assays

Synopsis

  • Cutting-edge technique for identifying and characterizing drug targets within the complex membrane environment
  • Innovating strategies to address the unique challenges associated with studying membrane proteins
  • Exploring how assimilation proximity assays can streamline the drug discovery process by enabling the rapid identification of potent and selective drug candidates

11:15 am Using Single Molecule Tracking For In-Cell Interactions & a Closer Look At Particle Dynamics for Detailed Understanding of Biological Processes

  • Laura Caccianini Postdoctoral Researcher, Massachusetts Institute of Technology

Synopsis

  • Implementing direct visualization of molecular interactions in real-time for the quantification of binding kinetics and affinities and identification of conformational changes induced by drug binding for improved efficacy
  • Exploring the many uses of probing protein dynamics, e,g, to measure diffusion coefficients and anomalous diffusion, characterization of protein-protein interactions for better understanding and discovery
  • Understanding drug transport and cellular uptake by tracking the movement of drug molecules within cells, visualization of drug delivery mechanisms and cellular uptake pathways and assessment of drug distribution and localization in tissues

11:45 am Lunch

Analysing Case Studies in Biophysical Approaches to Target Selection, Hit Identification, Mechanism Exploration and Hit-To-Lead Studies To Improve Knowledge & Aid Future Drug Discovery

12:45 pm Fragment-Based Discovery of Reveals Unprecedented Ligandability and Enables Direct Targeting of a Cancer-Relevant Transcription Factor

Synopsis

  • Transcription factors remain of high interest in oncology and other disease areas
  • Direct targeting of certain classes or domains of transcription factors is unexplored, and they are considered undruggable
  • Fragment screening and optimization, driven by multiple orthogonal biophysical techniques coupled with structure-based design, enabled the discovery of ligands targeting such a transcription factor

1:15 pm Looking Into Hit Selection & The Biophysical Methods Being Utilised to Enhance The Expertise in The Industry for More Efficient Drug Discovery

Synopsis

  • Explaining the background of the research, including the target and disease for the biological context of the mechanism being investigated
  • Understanding the methods, techniques and technologies used to identify an appropriate mechanism for drug interaction
  • Revealing the results obtained from the study and the future directions being taken for better understanding of the area

1:45 pm Afternoon Break & Networking

2:15 pm Small Molecule Drug Discovery Involving Conformational Dynamics & a New Technique for Hit-Validation

Synopsis

  • Assessing the recent advancements in the field, and how biophysics can aid identification of hits and the optimisation of drug properties
  • Exploring the techniques and strategies most commonly used to characterise small molecules for better efficiency in development
  • Hearing the specifics on the hit-validation process

2:45 pm Biophysical Insights for Deubiquitinases Chemical Matter

  • Ben Levin Principal Scientist, Stablix Inc.

Synopsis

  • Introduction to Stablix and Targeted Protein Stabilization (TPS) and hit ID chemical matter
  • Characterization of DUB chemical matter
  • Expanding horizons for biophysical characterization

3:15 pm Panel Discussion: Considering the Future Directions of Biophysics in Drug Discovery

Synopsis

  • Highlighting cutting-edge, biophysical techniques that are revolutionizing our understanding of biological systems to accelerate drug discovery
  • Exploring the future requirements in techniques for advancing current approaches
  • Investigating the current challenges and methods for solving them for improved discovery

4:15 pm Chair’s Closing Remarks

4:30 pm End of Conference Day 2

Conference Day One
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