CONFERENCE DAY ONE

Wednesday, December 11, 2024

8:00 am Check-In & Light Breakfast

8:50 am Chair’s Opening Remarks

Streamlining Hit Generation with High-Throughput & Unbiased Covalent Screens to Define Innovative Warheads for Hard-to-Drug Targets

9:00 am Covalency Offers Unique Opportunities for Difficult Targets

Synopsis

  • Covalency provides opportunities for difficult drug targets
  • Screening identifies a starting point for a TF target
  • Proteomics is an essential tool for covalency focused efforts 

9:30 am Mass Spectrometry Screening & Hit Optimization Strategies for Efficient Covalent Drug Discovery

Synopsis

  • Maximizing throughput for MS-based covalent screens
  • Integrating data generated from MS screens to identify potent and selective hit compounds
  • Triaging hits to identify the most tractable compounds

10:00 am Panel Discussion: Debating Systematic & Scalable Screening Methods to Rationally Discover & Develop Covalent Handles with Optimized Reactivity & Selectivity

  • Maurizio Pellecchia Professor of Biomedical Sciences, Director Center for Molecular & Translational Medicine, University of California Riverside & Armida Labs
  • Brett Babin Principal Scientist, Genentech
  • Iván Cornella Chief Scientific Officer, Covant Therapeutics
  • David Weinstein Vice President & Head of Chemistry, Vividion Therapeutics
  • Monica Schenone Senior Director & Head of Chemical Biology & Proteomics, Pfizer

Synopsis

  • Debating the pros and cons of target-agnostic and target-focused screening to identify the best use cases
  • What are the best methods for finding tractable hits?
  • Discussing how to balance reactivity with sensitivity within screening cascades
  • Streamlining hit to lead by sifting through hits and appropriately triaging

11:00 am Morning Break & Speed Networking

Synopsis

Our speed networking session is the ideal opportunity to get face-to-face time with many of the brightest minds working to discover and develop covalent modalities. Introduce yourself to the attendees that you would like to have more in-depth conversations with, benchmark against industry leaders, and establish meaningful business relationships that you can pursue for the rest of the conference and beyond

Accelerating the Development of Unbiased & Scalable Platforms to Access & De-Risk Novel Chemistry Amenable for Covalency & Propel Discovery Pipelines

12:00 pm Practical Approaches to Accelerate Covalent Drug Discovery

  • Brent Martin Vice President, Chemical Biology, Scorpion Therapeutics

Synopsis

  • Exploring early profiling and selection of actionable targets
  • Assessing hits to predict target traceability
  • Enabling biochemical and chemoproteomics assays to build programs

12:30 pm Mechanistic Study of Reversible & Irreversible Covalent Inhibitors

  • Xiang Yi Principal scientist, Amgen Inc.

Synopsis

  • The emergence of reversible covalency addresses off-target safety concerns, countering challenges posed by irreversible covalent inhibitors. Yet, characterization of this novel mechanism is hindered by limited assays and tools
  • Establishing enzyme kinetic assays, incorporating slow binding Ki Kinact measurement and jump dilution to enable the determination and differentiation of reversible from irreversible covalency mechanism

1:00 pm Session Reserved for WuXi AppTec

1:30 pm Lunch Break & Networking

Spearheading the Specific Covalent Targeting of More Abundant Residues Beyond Cysteine to Access Novel Binding Pockets & Expand the Druggable Proteome

2:30 pm Specific Covalent Targeting of Histidine, Tyrosine & Lysine to Expand the Druggable Proteome

  • Andrea Zuhl Vice President, Chemical Biology & Proteomics, HYKU Biosciences

Synopsis

  • Development of novel warheads for covalent screening of histidine, tyrosine and lysine residues
  • Enhancing the capture and mass spectrometry detection of sensitive peptide-ligand pairs
  • Integration of structural information to prioritize novel binding pockets for further development of covalent or non-covalent compounds

3:00 pm Targeting of Histidine Residues to Increase the Pool of Potential Targets Amendable for Covalent Drug Discovery

  • Maurizio Pellecchia Professor of Biomedical Sciences, Director Center for Molecular & Translational Medicine, University of California Riverside & Armida Labs

Synopsis

  • Showcasing how to identify and map histidine residues across a wide range of proteins to determine their potential as covalent drug targets
  • How to marry the right electrophiles with histidine moieties
  • Ligand-first versus electrophile-first approaches to target Histidine residues 

3:30 pm Afternoon Networking Break

Advancing Chemoproteomic Platforms & Probes to Better Interrogate Novel Biology & Amplify the Druggable Proteome Outside Oncology

4:00 pm Towards a Chemical Biology Platform for the Systematic Discovery & Evaluation of Novel Covalent Chemistry

Synopsis

  • Exploring insights into flexible library setup to synthesis novel covalent warhead libraries
  • Showcasing MS and proteomics-based discovery and profiling assays for novel covalent warhead motifs
  • Examining setups to screen and profile novel covalent libraries

4:30 pm Roundtable Discussion: Fueling the Covalency Renaissance by Strategizing the Chemistry Toolbox to Target Residues Beyond Cysteine with Orthogonal Reactivity

Synopsis

  • Which amino acids are seen as the next frontier in covalent drug discovery?
  • What is the mass spectrometry or alternative screening toolbox for other amino acids?
  • How can we build drug-like warheads that hit other sidechains? Should we be screening these more promiscuous warheads?
  • What are the different methods to validate non-cysteine covalency in simplified systems?

5:00 pm Covalent Fragment-Based Ligand Discovery to Drug Refractory Targets

  • Rhamy Zeid Vice President, Head of Biology, Nexo Therapeutics

Synopsis

  • How can covalent fragment-based ligand discovery be leveraged to tackle so-called undruggable targets?
  • What are the advantages of a target-centric approach to covalent fragment-based ligand discovery?
  • What approaches (biochemical and cell-based) can be deployed to progress covalent fragment starting points to mature lead molecules within a drug discovery campaign? 

5:30 pm Chairs Closing Remarks

5:35 pm End of Conference Day One

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