8:00 am Morning Coffee
8:50 am Chair’s Opening Remarks
Exploring the Versatility of Induced Proximity Drugs in Post Translational Modifications Offering Novel Opportunities for Therapeutic Intervention
9:00 am PHICS: Pioneering Precision in Protein Phosphorylation Modulation
Synopsis
- PHICS technology overview
- Rewiring kinases towards neo- and native- substrates
- Case study: targeting mutant KRAS
9:30 am Developing Induced Proximity Drugs with ADCs to Demonstrate Improved Potency & Selectivity Profiles
Synopsis
- What motivates the integration of ADCs with induced proximity drugs?
- How do ADCs enhance the therapeutic approach compared to standalone strategies?
- How are antibodies designed and optimized for ADCs targeting epigenetic regulators in the context of induced proximity?
10:00 am Application of Technology Platforms for Mechanism of Action Discovery
Synopsis
- Discovery of bioactive agents by phenotypic screening requires mechanism of action deconvolution
- Molecular glue mediated induced proximity can be used as a dimerization tool
- Velcrin-induced PDE3A-SLFN12 complex formation activates the SLFN12 RNase
10:30 am Morning Networking Break & Scientific Poster Session
Expanding Targeted Protein Degradation Beyond PROTACs with Unique Mechanisms of Action to Unlock Novel Druggable Targets
11:30 am Showcasing the EpiTAC Platform to Optimizing the Clearance of Membrane & Extracellular Targets
Synopsis
- What are the molecular mechanisms underlying degradation of extracellular proteins and how can these be modulated by bispecific antibodies for optimal protein clearance?
- How to define a suitable target for induced degradation?
- What are the key design principles for effective EpiTAC bispecific antibodies?
- How is the degradation activity of EpiTACs monitored? How to minimize off-target effects?
12:00 pm Leveraging Cryo-EM & AI for Discovery of Molecular Glues
Synopsis
- Harnessing artificial intelligence and cryo-EM to discover novel druggable protein interfaces
- Develop proximity-inducing glues that stabilize important druggable protein-protein interfaces
- Exploring the mechanistic insights, preclinical development,and current status of our pipeline programs
12:30 pm Reviewing the Induced Proximity Landscape to Spark Novel & Continued Opportunities for Therapeutic Intervention
Synopsis
- Showcasing an overview of the heterobifunctional space, including protein degraders & protein stabilizers
- Delving into novel induced proximity modalities
- Reviewing the induced proximity deals & companies landscape
1:00 pm Round Table: Overcoming Challenges in Structural profiling to Reveal Ternary Complexes & Elucidate the Mechanisms of Action of Novel Induced Proximity Modalities
Synopsis
- How to capture and utilize dynamic conformational changes in ternary complexes?
- How to overcome limitations in applying cryo-EM to the study of induced proximity mechanisms?
- How are structural studies adapted to reflect intracellular environments?
1:30 pm Networking Lunch Break
Examining Pre-Clinical & Translational Cases to Inform the Strategy for Progressing Emerging Induced Proximity Compunds into the Clinic
2:30 pm Unlocking GPCRs & Ion Channels to Antibody Pharmacology via Chemically Induced Proximity
Synopsis
- Showcasing the development of Solu Therapeutics CyTACs (Cytotoxicity Targeting Chimeras) Platform
- Exploring the in vitro, ex vivo and in vivo characterization of CyTACs targeting GPCRs and ion channels
- Reviewing PK/PD and in vivo efficacy in mice and non-human primates
3:00 pm Fireside Chat: Interrogating Delivery & Formulation Strategies to Improve the Development of Orally Bioavailable Compounds with Optimal Dosing & Administration Regimes
Synopsis
- What assays to employ to improve oral bioavailability through design cycles?
- How does the oral bioavailability of induced proximity drugs correlate with the administered dose? What dose optimization strategies can be employed?
- How to improve the solubility of heterobifunctionals through strategic formulation?
3:30 pm Advancing Small Molecules Targeting Autophagy Receptors into Preclinical Development to Address Unmet Patient Need in CNS Diseases
Synopsis
- How to identify biomarkers to monitor target engagement and the pharmacodynamic effects of AUTOTACs in preclinical models?
- How to efficiently identify, and successfully address, challenges that arise in the pre-clinic?
- What regulatory pathways are being considered for advancing AUTOTACs into clinical trials?