8:00 am Morning Refreshments
8:55 am Chair’s Opening Remarks
OPTIMIZING PROTEIN DEGRADER PHYSICOCHEMICAL PROPERTIES TO IMPROVE DELIVERY ACROSS THE BLOOD BRAIN BARRIER
9:00 am Explaining Blood−Brain Barrier Permeability of Small Molecules by Integrated Analysis of Different Transport Mechanisms
Synopsis
- Constructing a model to determine small molecule feasibility to cross the BBB via different transport mechanisms
- Breaking down small molecule ability to cross the BBB via diffusion, influx and efflux mechanisms
- Predicting impacts on adding chemical moieties on small molecule BBB penetration
DISCOVERING TARGET PROTEINS & MAXIMIZING SCREENING STRATEGIES TO ENSURE PROTEIN DEGRADER SPECIFICITY TO CNS INDICATIONS
9:30 am Roundtable Discussion: Starting From Scratch: Investigating CNS Targets Without Binding Inhibition Knowledge to Identify Brain & Pathology-Specific Target Proteins
Synopsis
- Tackling difficult to drug targets across CNS disease pathologies
- What are the clinically effective targets for CNS protein degraders?
- Outlining best practices to screen and develop ligands specifically targeting toxic CNS aggregates
10:15 am Exploring High-Throughput Target Screens to CNS-Specific Protein Degraders
Synopsis
- Adapting Plexium’s high-throughput screening for degraders of CNS-relevant diseases
- Setting expectations for optimal library size when screening for CNS protein degraders
- Exploring high-throughput screening in iPSC-derived neuronal cells to search for protein degradation characteristics
10:45 am Morning Break & Networking
11:15 am Identifying & Advancing Hits from CNS Protein Degrader Library Screens
Synopsis
- Investigating the promise of phenotypic screens to identify protein degraders
- Detailing a strategy for rapidly translating from degrader hits to in vivo efficacy
- Outlining leading indications for degraders targeting autophagy in CNS disorders
OVERCOMING THE BARRIERS TO TRANSLATON TO UNLOCK CLINICAL SUCCESS IN CNS PROTEIN DEGRADATION
11:45 am Panel Discussion: Breaking Down the Pitfalls in Protein Degrader Assays & Brainstorming CNS-Specific Considerations
Synopsis
- Streamlining PROTAC sample handling to foster standardized degrader assay development and analysis
- Evaluating PROTAC behavior as small molecules to understand mechanism of action
- Spotlighting additional PK and in vitro cost and time burdens in non-optimized assay conditions
12:15 pm Lunch & Networking
1:15 pm Re-Evaluating Pharmacokinetic Profiles, Brain Penetration & Off-Target Effects of PROTAC-Like Compounds Targeting Tau
Synopsis
- Exploring pharmacokinetic profiles of CNS protein degraders
- Evaluating small molecule measurements of brain penetration against previously reported data
- Analyzing understanding of off target-effects misleading target engagement
1:45 pm Fireside Chat: Navigating the Future Development of Protein Degraders for CNS & Making the Most of Early Industry Collaboration
Synopsis
- To what extent are gaps in biological understanding hampering development of CNS protein degraders?
- What are the short to medium term barriers to overcome to accelerate CNS degrader development on par with oncology?
- How can the drug development community collaborate and mutually benefit in exploring TPD applications to CNS?
2:15 pm Chair’s Closing Remarks
2:30 pm End of Conference
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