Conference Day One | Wednesday, May 21
8:00 am Morning Registration & Coffee
8:55 am Chair’s Opening Remarks
Identifying, Selecting & Validating GPCR-Targets with Downstream Characterization to Develop Drugs for a Wider Range of Diseases
9:00 am Application of Structure-Based Drug Discovery to Accelerate GPCR Drug Discovery
Synopsis
- Evolution of GPCR drug discovery approach
- Outline of a productive integrated structure based drug design strategy
- Structure to clinic case study
9:30 am Harnessing a Highly-Selective Designer Protein Platform to Identify Agonists, Antagonists & Inverse Agonists for GPCR Targets
Synopsis
- Engineering of a ‘hyper-stable,’ non-cross reactive human protein with hypervariable binding loops to selectively bind GPCRs
- Development of a robust platform to screen libraries of ligands for GLP-1R and cannabinoid receptor CB2R
- Functional characterization of agonists, antagonists, and inverse agonists for therapeutic development
10:00 am Morning Break & Speed Networking
Synopsis
This networking session is your opportunity to get face-to-face with many of the brightest minds working in the GPCR field and establish meaningful business relationships to pursue for the rest of the conference.
Overcoming Structural Biology Limitations of GPCRs to Develop More Effective Screening Strategies to Identify Agonists & Antagonists
11:00 am Unlocking GPCR Drug Discovery: A Seamless Platform for High-Quality Protein Production, Structural Insights, and Advanced Signaling Analysis
Synopsis
- G protein-coupled receptors (GPCRs) remain a cornerstone of drug discovery, yet their complexity presents significant challenges. Our platform provides a seamless, end-to-end solution to accelerate GPCR-targeted drug discovery by integrating high-quality GPCR protein production, structural biology, and advanced signaling analysis
- We specialize in the production of functional GPCRs and GPCR complexes to support hit identification, profiling, and structure-based drug design using cutting-edge cryo-electron microscopy (cryo-EM)
- Additionally, our in-depth characterization capabilities leverage a portfolio of over 200 proprietary cell lines and 400 diverse assay formats, enabling precise and comprehensive analysis of GPCR
11:30 am Decoding GPCR Dynamics: Structural Insights and Pharmacological Implications through Cryo-EM
Synopsis
- Structural characterization of GPCRs in different conformational states are key to understand mechanism of activation and downstream pharmacology
- Challenges in the Discovery of GPCR-targeted biologic drugs and how Tectonic GEODe™ platform overcomes these
- Impact of stabilization of active and inactive conformations on the discovery of biologics targeting GPCRs
12:00 pm Networking Lunch
Harnessing Novel Modalities to Target GPCRs with Reduced Toxicity & Enhanced Specificity
Afternoon Chair:
1:00 pm Empowering Drug Discovery With Real-Time Signaling
Synopsis
- Real-time measurement of signaling kinetics reveals different properties of ligands after washout or antagonist treatment
- Receptor expression level can affect signaling modality and kinetics
- Continuous signaling reporting simplifies screening for agonists, antagonists and allosteric modulators
1:30 pm Roundtable Discussion: Examining the Future Possibilities of Modalities for GPCRTargeted Drugs to Become More Effective & Feasible
Synopsis
- How can we begin to develop orally available peptides?
- How do you turn a peptide starting point into a small molecule drug?
- What are the other modalities that can be employed to target GPCRs? Do some modalities lend themselves better to specific indications/GPCRs?
2:00 pm Afternoon Break & Poster Session
Synopsis
Contribute to the conversation and share your cutting-edge research with like-minded GPCR experts. To present a poster, register your place and submit an abstract highlighting your breakthrough discovery. *Please visit the website for T&Cs for presenting a poster
3:00 pm Next-Generation ADCs for GPCR-Expressing Tumors: Unlocking New Therapeutic Opportunities
Synopsis
- GPCRs as Emerging Targets: Understanding the role of GPCRs in oncogenic signaling and tumor progression
- Tumor-Specific GPCR Targeting: Designing ADCs with enhanced selectivity for tumorassociated GPCR isoforms
- Combination Strategies: Exploring synergistic effects of SKM-104 ADC with checkpoint inhibitors, chemotherapy, or radiotherapy
3:30 pm A Curious Journey in OX2R Drug Discovery
Synopsis
- Identification of an agonist series using a new screening assay based on ConfoBodies®
- Elaboration of the chemical series gave a puzzling structure activity relationship
- Determination of the active state structure with a series representative revealed the cause of these unexpected activity cliffs