Explore the Agenda
Conference Day Two
8:00 am Check-In & Light Breakfast
9:00 am Chair’s Opening Remarks
From Unknowns to Actionable Targets: Strategies to De-Orphanize GPCRs With Greater Precision & Confidence
9:15 am From Discovery to First-in-Class: Pioneering an Orphan GPCR for Unmet Medical Needs
- Leveraging advanced computational methods to discover and verify a high-potential orphan GPCR linked to our disease of interest
- Pursuing the project against investor and industry skepticism, supported by strong clinical evidence and a differentiated indication strategy
- Presenting early clinical results from Phase I trial
9:45 am Roundtable Discussion: Building in High Binding Affinity & Selectivity into GPCR Ligands Using Structure-Guided & Biophysical Approaches
- What are the main challenges in overcoming GPCR ligand promiscuity, and how can we ensure selectivity when overlapping signalling pathways risk off-target effects and reduced therapeutic precision?
- How can allosteric modulators that bind to alternative receptor sites be leveraged to achieve more refined control of receptor activity and significantly improve specificity?
- In what ways can high-resolution structural data inform the rational design of GPCR ligands, helping to optimise binding interactions and accelerate the development of highly selective therapeutic agents?
- Can we optimise binding kinetics so that ligands have a long residence time in the receptor to achieve higher efficacy?
10:30 am Morning Break & Networking
Advancing Functional Assays & Biomarker Strategies for GPCRs to Accelerate Hit-to-Lead Discovery & Enhance Druggability Assessment
11:00 am Translating GPCR Insights into Successful Medicines by Overcoming Target Engagement & Biomarker Challenges
- Developing predictive biomarkers to identify oncology patients most likely to respond to GPCR-targeted ADCs or radio-conjugates, enabling precision therapy selection
- Leveraging human-derived tumour models (patient-derived xenografts, resistant models) to translate GPCR biology into clinically relevant drug responses
- Implementing advanced target engagement assays to confirm ADC binding, internalisation, and payload release within the tumour microenvironment
11:30 am Advancing Functional Assays for GPCRs to Accelerate Hit-to-Lead Discovery & Improve Druggability Assessment
- Strategies to design and implement new approaches for quantifying GPCR signalling, enabling ligand comparison across diverse signalling pathways
- Application of reverse-design principles to functionalize known ligands with fluorophores and tracers for real-time visualization and measurement of receptor– ligand interactions
- Learnings from deeply characterized cannabinoid ligands, with examples of kinetic, biosensor, and target engagement assays
12:00 pm Roundtable Discussion: How Can We Advance GPCR Drug Discovery Through Cell-Based Screening & Structural Biology?
- How can we best balance studying GPCRs in their native cellular environment versus using isolated or recombinant proteins?
- Which protein sourcing and experimental system approaches optimise GPCR stability, activity, and translational relevance?
- What structural biology strategies, including cryo-EM and NMR, are most effective for guiding rational GPCR drug design?
12:45 pm Lunch Break & Networking
Advancing GPCR Therapies Into Emerging Disease Areas to Address Unmet Patient Needs
1:45 pm Identification & Validation of GPCR1 as a Novel Pancancer ADC Target
- GPCR1 is enriched in multiple types of cancers including solid and heme indications
- SKM104 is a specific anti-GPCR1 antibody with optimal properties for ADC modality
- SKM104-MA-L2 is an anti-GPCR1, exatecan-based ADC showing robust anti-tumour activity in multiple cancer models
2:15 pm Novel Agonist Anti-GPCR Antibody to Trigger Resolution of Inflammation
- First-in-class antibody targeting GPCR with agonistic activity
- Anti-GPCR antibody to trigger resolution of inflammation and treat chronic inflammatory diseases
- Agonist Antibodies inhibit inflammatory immune cell recruitment and activation