Conference Day One

8:00 am Registration & Coffee

8:45 am Chairman’s Opening Remarks

Discovery Day: Building Cutting Edge Tools, Uncovering New Targets & Assessing the Feasibility of Candidates to Build the Next Generation of Kinase Drugs

Assay Development, Kinome Exploration & Kinase-Focussed Drug Discovery Principles

9:00 am Presentation From Our Lead Partner, Reaction Biology

Synopsis

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9:30 am Understanding the Global Atlas of Motifs for the Human Protein Kinome

Synopsis

  • Experimental profiling of kinases
  • Computational application and evaluation of performance
  • Illumination of MS phosphoproteomics data

10:00 am Morning Refreshments & Speed Networking

11:00 am Presentation From Our Expertise Partner, Promega

  • Matthew Robers Senior Research Scientist & Group Leader, Promega Corporation

Synopsis

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11:30 am Characterizing the Structural & Functional Aspects of the Phosphatase Enzymes for Drug Development

Synopsis

  • Describing the disease relevance of members of the phosphatase family to inform indication-specific target selection
  • Providing a historical view of approaches towards targeted modulation of phosphatases to foster learnings going into future R&D
  • Grasping modern approaches towards phosphatase modulators using non-orthosteric mechanisms-of-action

12:00 pm Utilizing AI/ML Strategies to Optimize Drug Discovery

  • Rafael Depetris Director of Protein Biochemistry & Structural Biology, Volastra Therapeutics

Synopsis

  • Explaining the data requirements for AI/ML to be applicable to a situation
  • Using computational modeling to predict mutations
  • Identifying ideal binding domains and optimizing them to your needs with structural biology principles
  • Using this understanding to map out the molecular mechanisms behind resistance to inform drug design
  • Exploring issues when translating computational data to an in vivo setting to plan ahead

12:30 pm Lunch Break

1:30 pm Presentation From Our Expertise Partner, Assay Quant

  • Erik Schaefer Co-Founder, President, Chief Executive Officer & Chief Scientific Officer, AssayQuant Technologies Inc.

Synopsis

Sox Technology Sensors

Inhibitor or PROTAC – Overcoming Tumor Resistance & Improving Durability

2:00 pm Degradation Is Not Always Superior to Enzymatic Inhibition: Lessons Learned from EGFR Heterobifunctional Degraders

Synopsis

  • Targeted degradation of EGFR failed to suppress resistance common to EGFR targeted therapies
  • Degradation resulted in decreased efficacy relative to non-degrader controls
  • Comparing degrader vs non-degrader controls highlighted an unexpected role for ER stress contributing to the efficacy of canonical EGFR targeted therapies

2:30 pm Afternoon Break & Poster Session

3:00 pm Expert Panel Discussion: To Degrade or Not to Degrade – Rationale Behind Selecting Inhibitory or Degradation Modality

Synopsis

  • Highlighting the advantages of using a degrader vs. catalytic site inhibitors and optimizing PKPD
  • Optimizing the linker, linage and E3 ligand for maximal binding and optimizing residency time
  • Discussing the issues of translating degradation efficiency to the clinic with different kinase inhibitors

3:30 pm Full Audience Activity – Roundtable Discussion

  • Sandra Wiley Director of Translational Science, MEI Pharma

Synopsis

At your table discuss the following questions:

  • What are the 3 most important factors to consider when selecting your modality of choice?
  • In your mind, what are the central pros of a PROTAC degrader vs a traditional inhibitor?
  • What feature would you prioritize as your ‘dealbreaker’ when making a final decision regarding modality?

4:00 pm Chairman’s Closing Remarks

4:15 pm End of Conference Day 1