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 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
12:00 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
12:30 pm Networking Lunch
Decoding GPCR Pharmacology Through Mechanisms of Action to Enhance Drug Design & Targeting
1:30 pm Structural & Functional Basis of Ligand Multispecificity at Human Chemokine Receptors
Synopsis
- How to define and relate structure and pharmacology
- How to elucidate the mechanisms of action by which endogenous ligands can differentially recognize and activate the same receptor
- How can these findings potentially guide discovery of targeted therapeutics
2:00 pm Turbocharging the Pharmacology of GPCRs to Determine What is Physiologically Relevant
Synopsis
- Uncovering GPCR mutations in mouse models that match the human phenotype
- Reviewing how pathway-specific targeting has led to distinct drug properties highlights the ability to fine-tune drug effects
- Determining what is physiologically relevant by assessing the functional context of signaling pathways to ensure that drug effects align with natural biological processes
2:30 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
Harnessing Novel Modalities to Target GPCRs with Reduced Toxicity & Enhanced Specificity
3:30 pm Roundtable Discussion: Examining the Future Possibilities of Modalities for GPCR-Targeted 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?
4:30 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