Explore the Agenda
8:00 am Check In & Registration
8:45 am Chair’s Opening Remarks
Harnessing GPCR Signaling Complexity with Targeted Bias & Endosomal Dynamics to Optimize Drug Response & Clinical Outcomes
9:00 am GPCR Signaling Models for Mechanism-Driven Drug Discovery
- Disentangling intrinsic, system, and kinetic bias using time-resolved signaling assays combined with mechanistic mathematical modeling to provide a clearer, more reproducible and more predictive view of GPCR signaling
- Linking extended signaling parameters, beyond traditional potency and efficacy, to downstream functional effects to identify the optimal signaling profile for therapeutic efficacy and tolerability
- Enabling more efficient small-molecule design and optimization by connecting mechanistic signaling insights directly to chemistry and SAR
9:30 am Roundtable Discussion: Assessing the Pharmacological Impact of GPCR Biased Signaling, Endosomal Pathways & Oligomerization
- What are the current best practices for measuring GPCR signaling bias in vitro, and what limitations do they have for in vivo and clinical translation?
- What are the pros and cons of therapeutic targeting of oligomeric GPCRs? Are there targets that you think are especially promising for successful clinical translation?
- Are there current pharmacological tools for targeting endosomal GPCRs that may have broad translational potential? If not, why not?
10:15 am Morning Break & Speed Networking
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11:15 am Unlocking G-Protein Subtype Bias at D1 Receptors to Drive Enhanced Pharmacological Effects
- Creating BRET-based assays that distinguish true Gs versus Golf engagement, enabling accurate measurement of receptor–G-protein coupling without downstream signaling noise
- Linking Golf-biased D1 activation to enhanced striatal electrophysiology and improved motor performance, demonstrating how molecular bias translates into region-specific physiological effects
- Delving into the mechanistic differences between Gs and Golf activation and their pharmacological consequences, which may lead to translatable strategies for targeting desired neurological effects
11:45 am Presentation Details to be Revealed
12:15 pm Panel Discussion: Assessing the Pharmacological Impact of Biased Signaling, Endosomal Pathways & Oligomerization to Demystify GPCR Complexity
- What are the innovative methodologies to study biased, endosomal, and oligomeric GPCR signaling?
- How can we establish best practices for interpreting complex signaling data and distinguishing true pharmacological effects?
- How to translate mechanistic insights into improved GPCRs-targeted drug discovery and development
12:45 pm Lunch Break & Networking
Optimizing Allosteric GPCR Modulators with Integrated Screening & Computational Tools to Improve Functional Selectivity
1:45 pm Beyond Incretins – Smarter Drug Design for Non-Incretin GPCRs: Innovative Screening & Computational Strategies for Next-Gen Allosteric Modulators
- Discovering high-throughput and functional screening methods for identifying allosteric modulators
- How can we quantify efficacy, cooperativity, and pathway-specific modulation and use AI/ML to predict allosteric sites and optimize ligand properties?
- Case studies of allosteric GPCR modulators progressing to the clinic and how they’ve overcome side-effect profiles, exploited subtype selectivity and modulated complex signaling
2:15 pm Presentation Details to be Revealed
2:45 pm Targeting the Intracellular GPCR Core: A New Paradigm for Rationally Designing Biased Neuropeptide Ligands
- Identifying a conserved intracellular allosteric pocket on GPCRs, to design small molecules that directly modulate G-protein engagement, enabling unusually strong and clean pathway-selective signaling bias
- Selectively restricting or promoting access of specific transducers at the GPCR core, to allow rational tuning of signaling outputs, achieving desired therapeutic pathways while minimizing on-target side effects
- Leveraging a pocket that is conserved yet structurally variable across the GPCR superfamily, to provide a scalable framework for tailoring receptor-specific biased ligands and discovering new activities guided by ternary-complex insight
3:15 pm Afternoon Break & Poster Presentation Session
Take this opportunity to showcase your latest research and innovations with your peers and
understand the strategies of your fellow GPCR experts. Visit the website for the full T&Cs of
submitting a poster
Decoding GPCR Structural Plasticity with Cryo-EM & Time-Resolved Modeling to Expose Hidden Ligand Interactions, Activation Pathways & Mechanistic Design Rules
4:15 pm Activation of the RXFP1 Relaxin Receptor By Diverse Agonists
- RXFP1 is a GPCR involved in cardiovascular and renal adaptation to pregnancy
- Using Cryo-EM, we determined the structure of this receptor bound to native relaxin hormone as well as the small molecule drug candidate AZD5462
- The two ligands bind different surfaces on the receptor and induce divergent signaling outputs
4:45 pm Capturing Dynamic Structural Changes to Reveal Mechanistic Insights in GPCR Function & Ligand Binding
- Integrating time-resolved data with molecular simulations to capture transient conformational states and predict functional outcomes
- Linking structure to functional mechanism by demonstrating how G protein activation correlates with allosteric structural rearrangements in the receptor and the ligand binding pocket, providing actionable insights for drug discovery
- Observing how ligand binding sites evolve during receptor activation, moving beyond static snapshots to understand dynamic GPCR behaviour