Explore the Agenda
Conference Day One
8:00 am Check-In & Light Breakfast
9:00 am Chair’s Opening Remarks
Charting New Territory in GPCR Drug Development: Tools & Strategies to Unlock Complex & Emerging Targets to Expand Therapeutic Potential
9:15 am Potent Modulators of GPR126 Promote Schwann Cell-Mediated Myelination of Peripheral Nerve Axons
- Discovering potent GPR126 modulators, including picomolar peptide agonists and low-molecular-weight agonists/PAMs, and using cryo-EM to reveal a novel allosteric binding site
- Demonstrating that agonist and PAM modulation of GPR126 increases axon myelination in a Schwann cell in vitro model via activation of myelination pathways
- Presenting aGPCRs as tractable drug targets, with GPR126 modulation offering a promising route for developing therapeutics for peripheral neuropathies
9:45 am Accelerating Therapeutic Success by Connecting GPCR Targets to Actionable Biology: Allosteric Regulators of Free Fatty Acid Receptor 2
- Structural insights into multiple binding pockets for allosteric regulators of FFA2
- Defining the molecular basis for PAM versus NAM activity of ligands that bind to overlapping sites
- Assessment of tissue-selective function of such modulators
10:15 am Morning Break & Speed Networking
Join our speed networking session tailored for GPCR professionals, like yourselves, to connect with fellow industry peers to facilitate rapid yet meaningful exchanges of insights and expertise. Elevate your networking experience during this session designed for impactful connections within the space.
Advancing GPCR Structural Biology Through Experimental & Computational Innovation to Improve Predictive Modelling & Drug Design
11:15 am Predicting GPCR Complexes: Integrating Structural Biology & AI for Smarter Drug Design
- Explore cutting-edge strategies to predict GPCR-GPCR and GPCR-peptide complexes using AI-enhanced structural modelling
- Demonstrate how dynamic modelling and conformational flexibility inform rational drug design for GPCR targets
- Share computational insights of GPCR dynamics integrating experimental data and machine learning
11:45 am Enabling Structure-Based Drug Discovery for G Protein-coupled Receptor GPR55
- Enablement of GPR55 for structural studies
- Structure determination of GPR55 in complex with diverse ligands
- Structure-guided drug discovery
12:15 pm Unleashing GPCR Drug Discovery: From Static Structures to Dynamic Insights
- Harnessing cryo-EM and X-ray crystallography to reveal receptor structures and guide simulation-ready models
- Animating GPCRs through molecular dynamics in lipid bilayers to decode ligand binding, activation, and biased signalling
- Accelerating drug discovery via structure-based virtual screening to identify novel therapeutics and mutation-specific strategies
12:45 pm Lunch Break & Networking
1:45 pm Fireside Chat: How Can We Balance Innovation & Proven Methods in GPCR Structure-Based Discovery?
- Uncovering elusive allosteric binding sites by applying machine learning and predictive modelling, while addressing the experimental challenges of validating these computationally identified targets
- Translating computational workflows into tangible outcomes by moving beyond theoretical models to real-world applications, including the successful development of viable drug candidates and clinical strategies
- Integrating traditional structural biology with modern AI-driven methods by combining techniques like cryo-EM and crystallography with simulations and generative models, to create more dynamic and effective pharmaceutical pipelines
Harnessing Next-Generation Modalities to Expand the Therapeutic Reach of GPCR Drug Discovery
2:45 pm DT-7012: A Highly Differentiated Anti-CCR8 Depleting Antibody for Clinical Success
- Identifying key differentiating features during drug discovery to overcome the competitive landscape of CCR8-targeted antibodies
- Validating a novel CCR8 antibody candidate with the potential for superior clinical efficacy through strategic design and translational focus
- Highlighting a real-time case study of our CCR8 program, from target validation to first-in-human dosing, illustrating the power of rational antibody design for GPCR therapeutics
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.
4:15 pm Capturing Native GPCR Structures to Accelerate Drug Discovery
- Incorporating wild-type GPCRs into nanomembrane particles to facilitate the discovery of small molecules, antibodies, and peptides
- Enabling the study of GPCR oligomerisation, comparing results from recombinant versus endogenously expressed receptors
- Discovering how combining structural biology with antibody discovery in a CXCR4- focused study led to the identification of promising therapeutic candidates
4:45 pm Engineering Antibody Agonists to Transform GPCR Targeting With Durable Biologics
- Stabilising GPCRs in active conformations to enable the generation of functional antibody agonists, a key hurdle in expanding biologic modalities for these targets
- Recognising the limitations of current GPCR antibodies which are predominantly antagonists or binders, and investing in technologies that support agonist development
- Leveraging the advantages of antibody agonists such as improved pharmacokinetics, longer half-life, and scalable manufacturing to create more durable and patient friendly therapies