8:00 am Check-In, Coffee & Light Breakfast
8:45 am Chair’s Opening Remarks
Navigating In Vitro Hurdles to Streamline Translational Inhibitors Beyond Oncology
9:00 am Pioneering Novel Kinase Inhibitors: Facilitating CNS Penetration to Combat Neurodegenerative Diseases
Synopsis
- Understanding the unique characteristics of BTK inhibitors and degraders to enable translatability
- Maintaining neuroprotective functions of compounds to limit pleiotropic off-target effects common to BTK inhibitors and degraders
- Prioritizing efficacy over specific targets as a benchmark for optimizing compounds within in vitro models to successfully induce neuroprotection
9:30 am CNS-Penetrant TYK Inhibitors: Addressing Translational Challenges in Neuroinflammation
Synopsis
- Delving into genetic and pharmacologic rationale for TYK2 inhibition in multiple sclerosis
- Highlighting key neuroinflammatory and neurodegeneration-associated cell types and signaling pathways modulated by TYK inhibitors
- Conducting in vivo confirmation of CNS penetration and activity in CNS disease models
10:00 am Morning Refreshments & Networking
10:45 am Novel Brain-Penetrant Kinase Inhibitors: Triggering Harmonious Mechanisms to Treat Neurodegeneration
Synopsis
- Unraveling the impact of multi-kinase targets to reverse multifactorial neurodegenerative mechanisms
- Facilitating harmonious pathways that simultaneously induce autophagy and reduce vascular fibrosis and neuroinflammation
- Orchestrating peripheral-central immune communication via mast cell-microglia regulation
11:15 am Roundtable Discussion: Essential Data, Tools & Collaboration: Expediting Discovery of Kinase-Targeting Drugs
Synopsis
Despite recent advancements in kinase-targeted drug discovery, it is evident that there is a long-standing gap in translation for kinase inhibitors. Not only is there a big discrepancy between what is understood in vitro vs in vivo, but the growing
need for transparency in data and knowledge calls for experts working in discovery and development to strive for consistent collaboration.
Engage in our dynamic 45-minute roundtable discussion to address shared, modality-agnostic challenges with various stakeholders in the kinase space:
- Dissecting the types of data required to generate comprehensive evidence for effectively introducing in vitro findings into in vivo models
- Demonstrating kinase activity via robust assays to open avenues for biomarkers that can guide preclinical work towards diagnostics
- Creating an accessible platform that can encourage collaboration across experts to narrow the gap in knowledge across discovery and development
Identifying Degraders to Establish Alternative Strategies & Innovate Drug Development
12:00 pm Innovating PROTACs to Surpass Limitations of Traditional Kinase Inhibitors for Elevated Tumor Targeting
Synopsis
- Demonstrating unique mechanisms employed by PROTACs to promote targeted degradation of kinases
- Testing various combinations of chemical motifs and linker chemistries to produce effective PROTACs
- Streamlining the design of potent and selective PROTACs through anchor-linkerwarhead combinations for maximized degradation efficiency
12:30 pm Lunch & Networking
1:30 pm Leveraging Basal Protein-Protein Interactions for Targeted Degradation or Inhibition of Kinases
Synopsis
- Identifying sub-micromolar, protein-protein interactions between kinases and ligases or chaperones
- Structurally characterizing these interactions using site-directed mutagenesis to prioritize those most suitable for small molecule “glue-ability”
- Translating structural insights into small molecule strategies that promote kinase degradation or inhibition
Highlighting Novel Targets to Unlock Approaches to Next-Generation Kinase Therapeutics
2:00 pm Validating a Hit-Finding Strategy Around the Scaffolding Function of Aurora Kinase A
Synopsis
- Leveraging an indirect method to target N-Myc through disruption of protein-protein interactions (PPIs)
- Assessing the landscape to date and the potential for druggable allosteric pockets along the PPI interface
- Enabling a comprehensive hit discovery campaign to find PPI disruptors which maintain kinase activity