7:00am Morning Coffee & Registration
7:55 am Chairs Opening Remarks
Advancing Target Identification Strategies to Prioritize High-Value Targets & Expand the Therapeutic Window for Safer, More Effective Proximity-Based Drugs
8:00 am Beyond Screens: AI & Active Learning for Smarter Target Identification in Proximity Drug Discovery
Synopsis
- How to use AI-driven modeling to uncover and validate novel drug targets, including historically undruggable proteins like transcription factors?
- How to apply active learning to prioritize the most promising targets by continuously refining biological insights through iterative prototype-test cycles, to accelerate the discovery of clinically viable drug targets?
- How to integrate multimodal machine learning to identify high-value targets by analyzing structural, sequence, and functional data simultaneously?
- How to enhance target identification by embedding real-world biological constraints, ensuring AI-generated targets are clinically relevant and actionable?
9:00 am Cryo-EM Driven Design Of Precision Proximity Inducing Drugs
Synopsis
- Identifying novel molecular glue targets by combining AI-driven interface prediction with cryo-EMÂ
- Leveraging high resolution cryo-EM to enable design of molecular glues for challenging targetsÂ
- Improving safety profiles with cryo-EM analysis of off-target interactionsÂ
- Platform ability to generate pipeline assets across multiple indications
9:30 am Target-First vs. Modality-First: Identifying Disease-Driven Targets to Maximize Proximity-Based Therapeutic Impact
Synopsis
- Why should drug developers take a ‘target-first’ approach rather than retrofitting induced proximity strategies to unsuitable targets to improve translational success and avoid costly late-stage failures?
- How can chemical biology strategies be leveraged to fine-tune target-ligand interactions, ensuring induced proximity drugs achieve optimal selectivity, potency, and drug-like properties?
- Which disease areas offer the highest potential for induced proximity applications, and how to determine the best induced proximity strategy for a given target to maximize therapeutic impact and patient benefit?
10:00am Morning Break & Speed Networking
Engineering Assays & Screening Strategies to Strengthen Target Engagement & Drive Successful Validation of Novel Proximity-Based Modalities
11:00 am Optimizing Induced Proximity Labeling Techniques to Accurately Measure Induced Proximity Interactions In-Cell for Improved Translational Outcomes
Synopsis
- How to optimize in-cell assays to assess permeability, intracellular stability and functional engagement for ensuring efficacy in complex biological environments?
- How to improve assay scalability in routine use for more cost-effective, high-throughput alternatives to de-risk early-stage development and improve translation?
- How can advanced proximity-labeling methods (e.g., TurboID, MicroMap) improve resolution in mapping real-time protein interactomes to refine MoA validation for selecting the most clinically viable therapeutic candidates?
11:30 am Roundtable Discussion: Phenotypic vs. Target-Based Screening: Identifying the Right Effector for the Right Target to Maximize Therapeutic Efficacy
Synopsis
- How to leverage agnostic phenotypic screening in discovering novel IP mechanisms beyond traditional target-based approaches to unlock new target-effector pairings?
- How to harness emerging multi-modal screening platforms that integrate phenotypic and biochemical assays, to create a more efficient IP drug discovery workflow?
12:00 pm Leveraging Neo-Native E3 Ligases for Screening to Expand Induced Proximity Drug Discovery
Synopsis
- How to develop E3 ligase-agnostic screening strategies, like covalent ligand discovery and electrophilic fragment libraries, to uncover novel ligase-substrate pairs and expand the scope of induced proximity drug discovery?
- How to leverage functional proteomics, RNA-seq, and single-cell profiling to map tissuespecific E3 ligase expression patterns and design next-gen proximity inducers with improved selectivity?
- How to harness insights from chemical proteomics and AI driven modeling to accelerate discovery of non-degradative E3 ligases that modulate protein function via PTMs beyond degradation?
12:30pm Lunch Break & Networking
Expanding the Frontier of Induced Proximity-Based Drugs to Unlock Novel Modalities, Validate Hypotheses & Achieve Proof of Concept Across All Disease Indications
1:30 pm Harnessing tPRIME (Targeted PRoximity Induced Modulator of Expression) with Transcription Factors to Enable Fine-Tuned Gene Expression Control & Unlock New Therapeutic Modalities
Synopsis
- How can tPRIME be leveraged to enhance transcriptional regulation, ensuring more precise and sustained target activation for therapeutic benefit?
- What structural and molecular determinants drive the success of tPRIME in selectively stabilizing transcription factors without off-target effects?
- How can tPRIME be applied across different disease models to expand druggable space and overcome limitations in targeting transcription factors with traditional small molecules?
2:00 pm DUBTACs: Recruiting Deubiquitinating Enzymes to Rescue & Stabilize Disease-Driving Proteins to Expand Therapeutic Applications Beyond Traditional Degradation
Synopsis
- How can DUBTACs be leveraged to selectively stabilize and restore function to diseaseassociated proteins, expanding the scope of induced proximity beyond degradation?
- How to improve substrate specificity for DUBTACs to increase safety, efficacy and minimise unintended protein stabilization?
- How can structure-guided drug design and proximity-labelling methods identify previously undruggable targets to improve the discovery of novel DUBTAC-compatible targets?
2:30 pm RIPTAC™ Therapeutics: A Modality to Take Hold of Human Diseases – Pushing the Frontiers of Induced Proximity Drugs
Synopsis
- How to harness RIPTACâ„¢ therapeutics as a novel drug modality that employs a hold and kill mechanism to selectively target tumors and induce cancer cell death
- How to optimize the design of bifunctional small molecules to drive the formation of protein-protein interactions for enhanced therapeutic efficacy
- How to expand beyond traditional precision oncology by leveraging RIPTACâ„¢ therapeutics to overcome resistance mechanisms and extend treatment options for cancer patients
3:00pm Afternoon Break & Poster Session
4:00 pm RIBOTACS: A New Frontier for Selective Gene & RNA Modulation to Expand Therapeutic Possibilities for Undruggable Targets
Synopsis
- How can DNATACs be leveraged to modulate gene expression via targeted epigenetic regulation or DNA cleavage, without permanent genomic modifications for broadening patient application?
- How do RNATACs open new possibilities for targeting RNA stability, localization, and splicing, expanding therapeutic opportunities beyond RNA degradation?
- How to avoid off target gene modulation with structural biology, AI and chemical design for ensuring precise targeting?
4:30 pm Unlocking the Potential of Novel Non-Degrading Molecular Glues to Overcome Target Specificity for Enabling Rational Discovery & Design
Synopsis
- How to leverage a target-centric approach to guide the discovery of non-degrading molecular glues to match the right modality with each target, expanding beyond ubiquitin-based mechanisms?
- What role do stabilization and sequestration-based molecular glues play in modulating undruggable targets compared to traditional bifunctional approaches?
- How to optimize screening and linker strategies to improve drug-like properties (e.g. bioavailability) of non-degrading glue for increased clinical viability?