Conference Day 1

8:20 am Chair’s Opening Remarks

Showcasing Safety & Toxicology Profiles of Drugs Leveraging E3 Ligases

8:45 am Considering Toxicology & the Safety Profile before Entry Into the Clinic

Synopsis

  • Harnessing the very best preclinical models to evaluate the safety of E3 ligase, ligands, and degraders
  • Identifying safety signals for the new wave of E3 ligases, like the teratogenic cereblon

Examining the Current Perspective of the E3 Ligase Field/Landscape

9:00 am PANEL DISCUSSION: Lay of the Ligase Land – Where Are We Now & What Does the Next 5 Years of Ligase Discovery Look Like?

Synopsis

  • How do we publicize ‘novel’ ligases to make them available for the community more broadly?
  • How do you generate an intellectual property that will protect your drug?
  • How big a role will tissue specificity play in the future success of E3 ligase discovery and drug development?

Identify & Discover

New Approaches to Identifying New E3 Ligases & E3 Ligands

9:45 am Exploring Success Found in Targeting a Novel E3 Ligase With a Small Molecule

Synopsis

  • Reviewing the structural biology of the novel ligase
  • Elucidating the novel ligase mode of action
  • Outlining opportunities for translation to the clinic

10:15 am Morning Break & Speed Networking

11:15 am Utilizing a Novel Whole Proteome Approach to Characterize Weak Target Ligase Interactions

Synopsis

  • Unveiling a novel platform for efficient E3 ligase screening
  • Utilizing platform for degrader discovery
  • Unlocking previously undruggable targets using this platform

11:45 am Examining E3 Ligase Binder Identification by Function First Approach

Synopsis

  • Examining selection strategy of the right E3 ligase following to identification of its binders depending on POI
  • Spotlighting a highly productive degrader discovery system based on the synthesis and evaluation of more than 1,500 degraders/week
  • Overcoming challenges for drug-like property by prediction based on in silico properties and AI technology

Showcasing Innovative Technologies to Discover Novel E3 Ligases

12:15 pm Leveraging the Discovery of Novel E3 Ligands for Targeted Protein Degradation

Synopsis

  • Unveiling how the discovery of ligands to novel E3 ligases represents a significant opportunity and the major challenge for targeted protein degradation
  • Examining targeted protein degradation using Cullgen’s novel E3 ligand platform

12:45 pm Networking Lunch Break

1:45 pm Discovery & Development of Novel E3 Ligases for Targeted Protein Degradation

Synopsis

  • Developing a platform for discovering molecular glues targeting novel E3 ligases
  • Examining approaches to identifying novel ligands to E3 ligases
  • Characterizing of novel E3 ligases for use in promoting targeted protein

Highlighting Throughput, Systematic Screening for Ligase Ligands/Binders

2:15 pm Championing a High Throughput Approach to Uncovering a Novel E3 Ligase to Streamline Your Ligase Discovery Pipeline

  • Jo Hyunsun Founder & Chief Executive Officer, Pin Therapeutics

Synopsis

  • Accessing a comprehensive library of novel, and lesser-known E3 ligases to kickstart your drug development with your chosen ligand
  • Elucidating the novel ligase mode of action to inform potential utility in disease
  • Utilizing ternary complex imaging data to optimize your candidate

2:45 pm Profiling a Lesser-Known Ligase for Targeted Drug Discovery

Synopsis

  • Characterizing the ligase mode of action and weighing its suitability for drug
  • Mapping out the ligase tissue expression using proteomic, transcriptomic, and genomic analyses
  • Detailing the physiology of the ligase and its endogenous ligand

3:15 pm Afternoon Break & Networking

3:45 pm Progressing from Discovery to Development Efficiently by Selecting Your Degrader Early

Synopsis

  • Considering the biology of your E3 ligase from a structural and physiological perspective first to inform small molecule degrader selection
  • Maximizing efficiency in translation with an effective molecular glue versus chimeric degraders
  • Selecting a novel ligase with downstream application in mind, to avoid wasted time and effort

4:15 pm Avoiding Toxicity in Ligase Inhibition

Synopsis

  • Considering off-target effects using purified proteins-based assays to understand how many ligases you are inhibiting
  • Unveiling the mode of action for a novel inhibitor for a specific ligase in the context of strong variability

4:45 pm Translating Identification of Your Ligase Into a Druggable Target

  • Ian Churcher Chief Scientific Officer, Amphista Therapeutics

Synopsis

  • Combining your binder for a ligase with a tool that enables meaningful modulation
  • Promoting degradation of a ligase with a novel degrader

5:15 pm End of Day One

All times in EDT