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
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
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