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 Harnessing Structural Biology & AI for GPCR Targets Across Metabolic & Immune Diseases
Synopsis
- How to identify the right target out of 800 GPCRs to pursue
- Exploring biophysical and biochemical characterization of potential GPCRs to understand what makes a good target
- Understanding the dynamics of GPCRs and how these can be related to small molecules, antibodies, peptides and more
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 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
10:30 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
11:30 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
12:00 pm Supercharging Analysis of GPCRs to Help Design Drugs
Synopsis
- Combining structural biology, computational chemistry, medicinal chemistry, and pharmacology to develop effective drugs for GPCRs
- Understanding the structural diversity of GPCRs to design drugs that are selective and effective across GPCR subtypes
- Understanding molecular insights into GPCRs and mechanism of action of small molecules to increase efficacy
12:30 pm 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
1:00 pm Networking Lunch
Achieving Success with the Development & Manufacturing of Therapeutics for Metabolic Diseases Targeting GLP-1 & Beyond
2:00 pm Design & Development of Novel GPCR Targeting Small Molecule Agonists with the Application of Quenched Molecular Dynamic (QMD) Simulations
Synopsis
- Generation of physiologicaly relevant conformers, binding mode, design of peptidomimetics by constraining peptide backbone, we develop orally available peptide or small molecules
- Further profiling against several GPCR family member target proteins for selectivity and stability for targeted treatment
- Generate natural peptide sequence to a stable conformer, search for amide back-bone, alpha-C, acid and amine mimetic functional groups to turn in to peptidomimitics
- Then, covert constrained peptidomimitic scaffolds region which serve as peptoid or smnall molecue for oral delivery
- Biolexis MolecuLern technology, ML training models employed on targeting several GPCR class proteins for the design of peptidomimetics, stable peptides, allosteric modulators, inverse agonists & small molecule agonists
2:30 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
3:00 pm Roundtable Discussion: Solid dose manufacturing using GPCR small molecules and beyond: Myths vs Facts
Synopsis
- What is better, Tablets or Capsules?
- Which is more difficult to manufacture into a solid dose product, a high dose drug or low dose drug?
- Which one gets you to the clinic faster – smaller and more flexible drug product CDMO or a large global CDMO?
3:30 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
4:00 pm Fireside Chat: Examining the Future Possibilities of Modalities for GPCRTargeted Drugs to Become More Effective & Feasible
Synopsis
- Can we develop orally available peptides?
- How do you make a peptidic starting point into a small molecule?
- What are the different modalities that can be employed to target different GPCRs?
Harnessing Novel Modalities to Target GPCRs with Reduced Toxicity & Enhanced Specificity
4:30 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
5:00 pm Exploring Dynamics & Physiological Relevance in Small Molecule & Biotherapeutic Development
Synopsis
- How to get from structure of a target GPCR to design of the small molecule
- Understanding the dynamics of GPCRs and how these can be related to small molecules, antibodies, peptides and more
- How to ensure that the membrane protein is in the physiologically relevant state for analysis