Conference Day One | Wednesday 27th November, 2024
8:00 am Check-In & Light Breakfast
8:50 am Chair’s Opening Remarks
Leveraging Structural Biology & Predictive Modelling to Improve Hit-to-Lead Optimisation for Difficult-to-Drug GPCRs
9:00 am Enabling drug discovery for GPCRs & Membrane Proteins
Synopsis
- GPCR reagent toolbox
- Supporting Structure based drug design
- Affinity screening
9:30 am Developing Ligands to Image & Target the Medium Chain Fatty Acid Receptor GPR84
Synopsis
- Can biased ligands or allosteric ligands that bind at distinct locations fine-tune receptor function to allow tissue-selective beneficial outcomes
- Can we intuitively design ligands with varying bias or will this remain a process of serendipity
10:00 am Targeting GPCRs with Agonistic Antibodies: A New Frontier in Obesity Treatment
Synopsis
- Discovery of novel agonistic VHH using ConfoGen Technology
- Structure of agonistic VHH in complex with GPCR
- In Vivo efficacy and selectivity with highly potent agonistic VHH
10:30 am Morning Break & Speed Networking
Successfully Identifying & Validating Genetic Variants of GPCRs to Unlock Previously Undrugged Targets
11:30 am MC4R Pharmacochaperone as a Novel Therapeutic Strategy for Genetic Forms of Early-Onset Obesity
Synopsis
- MC4R mutations resulting in receptor trafficking default as the cause of early onset obesity
- Therapeutic use of small molecule pharmacochaperones to rescue plasma membrane trafficking of MC4R
- Presentation of an unique toolbox made of in vitro and genetic in vivo models, and of in vivo proof-of-concept data
12:00 pm Discovery of Antagonists of GPR35, a Genetically Validated Target in Gastrointestinal Diseases
Synopsis
- GPR35 is a genetically validated target in gastrointestinal diseases
- A drug discovery program led to the identification of small molecules with strong pharmacological validation
- A preclinical candidate has been nominated for clinical development
12:30 pm Lunch Break & Networking
Utilising the GPCR Toolbox & Navigating GPCRs Signalling Pathways to Develop Targeted GPCR Drug with Disease Relevance
1:30 pm Fireside Chat: The Evolving Toolbox to Investigate & Successfully Drug GPCRs: New Innovations & Opportunities to Come
Synopsis
- What tools do we need to better investigate and drug GPCRs to enable access to previously undrugged targets with relevant therapeutic values
- Where and how can innovation expand the toolbox to supercharge GPCRs targeting drug discovery strategies
- Where in workflow investment, guidelines and expertise are needed to open up the therapeutic opportunities across broader range of diseases for patients in need
2:30 pm Subcellular Organisation of Signalling of the Glucagon Receptor Family
Synopsis
- Intracellular receptor signalling nanodomains
- Lipid regulation of plasma membrane signal microarchitecture
- Cell-type specific signalling regulation
3:00 pm Trends in GPCR Drug Discovery
Synopsis
- New drug approvals and agents in clinical trials
- Shifts in disease indications and yet untapped targets
- Drug repurposing and re-targeting
- Company partnering landscape
3:30 pm Afternoon Break & Poster Session
Synopsis
Share your ground-breaking data and innovative drug discovery strategies with your fellow GPCR experts. This is your opportunity to showcase your contribution to GPCR drug discovery to a wide array of experts.
Better Informing Structure-Based Drug Design & Mapping Novel Disease Targets with Robust Screening, Computational & AI Tools
4:30 pm Confo Therapeutics’ Technology as a Superior Platform for Fragment-Based Drug Discovery on Difficult to Drug GPCRs
Synopsis
- What is the most optimum workflow for performing fragment-based drug discovery to identify selective and ligand efficient small molecules?
- Is there utility in the ultra-large scale screening of drug-like compounds or should we be more selective?
5:00 pm Customising CADD for SBDD Targeting the Elusive Ligand & Water Induced GPCR Pocketome
Synopsis
- Successful application of CADD to GPCR SBDD requires consideration of ligand-induced fit and water networks for PCR-ligand structure and potency/affinity prediction
- Meaningful use of AI/ML/ cheminformatics approaches for virtual ligand screening and design approaches requires combination with best practice and state of the art computational chemistry/CADD methods and protocols customised to the GPCR pocket and ligand chemistry of interest
- The applicability domain of CADD/cheminformatics/AI methods for GPCR SBDD depends on the integration with expanding GPCR Structural Biology, Biophysics/Biochemical/Pharmacological screening data and technologies