8:00 am Check-In & Light Refreshments
8:50 am Chair’s Opening Remarks
Drugging the Undruggable: Exploring the Potential of RNA Binders, Degraders & Molecular Glues for Hard-to-Drug Targets
9:00 am Demystifying Molecular Glues Through the Identification & Targeting of E3 Ligase Interactions
Synopsis
- Developing a method to discover novel molecular glues through systematic processes aims to replace discovery by serendipity with a structured approach to hit identification
- Evaluating DEL screening for hit identification for molecular glues
- Understanding which assays to run in parallel to evaluate the validity of your hits & understand the degradation pathway being targeted
9:30 am Methods for the Discovery, Evaluation & Characterization of New Ligands for Targeted Protein Degradation
Synopsis
- Identifying new E3 ligase interactions that can be harnessed against undruggable targets
- Generating actionable insights that can be used for further hit ID cascades
- Presenting methods for proximity labeling of a target of interest for identifying complex members and transient interactions
- Developing HTS methods to identify new molecules for targeted protein degradation
- Optimizing data analysis tools for protein degrader molecular properties
- Guiding protac SAR using quantitative measurement of biochemical properties and degradation activities
10:00 am Morning Break & Poster Session Continued
Synopsis
This is an informal session to help you connect with your peers in a relaxed atmosphere and forge new and beneficial relationships. With an audience of experts in medicinal chemistry & hit identification eager to discuss shared challenges, you will have the opportunity to display a poster presenting your own work. Additionally, you will have the chance to review others’ posters. To submit a poster, please contact info@hansonwade.com
11:00 am Double the Fun: Chemical Proteomics to Identify Novel Targets on Both Ends of a Novel E2-Based Bifunctional Degrader Platform
Synopsis
- Characterizing E2s and degradation machinery recruited by a novel E2-specific scaffold through chemical proteomics technologies
- Profiling of broad chemical matter to identify novel targets for TPD
- Characterizing the selectivity of degrader molecules throughout multiple cycles of compound optimization
11:30 am Luck Meets Design: Serendipitous Molecule Discovery for Targeted Protein Degradation
Synopsis
- Developing a drug screening assays to identify novel brain tumor therapies
- Developing a novel natural compound for targeted protein degradation
- Application of novel PROTAC for breast and brain cancer
12:00 pm Lunch & Networking
The Renaissance of Phenotypic Screening – Evaluating the Outcomes of Phenotypic & Target Based Screens
1:00 pm An Integrative Process to Discover Ligands of Nuclear Receptors with Different Modes of Action & Cellular Functions
Synopsis
- Discovering inhibitors of xenobiotic receptor PXR by automated phenotypic and target-based HTS
- Optimizing binding affinity by medicinal chemistry
- Revealing modes of action (agonists, inverse agonists and antagonists) by structural and pharmacology
1:30 pm Panel Discussion – Comparing & Contrasting the Abilities of Phenotypic VS Target Based Screening
Synopsis
- Comparing phenotypic and target-based screening to reveal phenotypic approaches’ broad discovery potential versus the specificity of target-based methods
- Contrasting these methods to highlight phenotypic screening’s ability to uncover novel mechanisms of action, while target-based screening focuses on predefined molecular targets
- Discussing both approaches to underscore phenotypic screening’s relevance in identifying hits through functional therapeutic effects, compared to target-based screening offering faster target validation
2:15 pm Emerging Strategies for Hit Identification of Covalent Compounds for High Accuracy Leads
Synopsis
- Talk details to be confirmed
Introducing Lab Automation to Increase the Efficiency & Consistency of Hit Identification Whilst Reducing Human Error
2:45 pm Automation in the 4th Generation Labspace: Freeing the Humans in the Loop so they can Dream Bigger, Reach Further & Push the Boundaries of Discovery Faster than Ever Before
Synopsis
- Leveraging advances in automation and robotics technologies to address major factors limiting the scope of high-throughput screening investigations
- Maximizing output through miniaturization; using advanced robotics to achieve more for less
- Building for the future; hit ID in the autonomous labspace