Conference Day Two | Thursday 28th November, 2024
7:30 am Check-In & Light Breakfast
8:20 am Chair’s Opening Remarks
Pursuing Emerging Modalities & Novel Targets to Expand the Druggable Paradigm of GPCRs for Patients in Need
8:30 am Targeting Class B GPCRs to Advance the Next-Generation of Metabolic Therapeutics
Synopsis
- Leveraging a novel drug modality and proprietary discovery platform to unlock Class B GPCRs
- Advancing a pipeline of differentiated therapeutics for obesity and metabolic disorders
- Capturing the untapped potential of Class B GPCRs with novel monotherapy and combination approaches
9:00 am PAR2 in Immuno-oncology: From Target Identification to the Selection of a Candidate with a Superior Mode of Action
Synopsis
- Target identification through public and proprietary clinical data
- Target validation with relevant in vivo models
- Understanding of receptor biology and thorough benchmark to determine the optimal mechanism of action
9:30 am GPCR Perspectives & Challenges in the Development of Radioligand Therapies – RLT for Nuclear Oncology
Synopsis
- The therapeutic roles of GPCRs in the innovation of RLT for nuclear oncology
- What are the key focal points in novel RLT developments
- Why peptides are the most attractive ligands for RLT
10:00 am Morning Break & Speed Networking
Overcoming GPCRs System Bias with Novel & Accurate Assays to Robustly & Accurately Accelerate Hit Finding
11:00 am Chemical Probes & Biosensors for Kinetic Measurements of GPCR Ligand Binding & Signal Transduction
Synopsis
- Development and characterization of chemical probes for the CB2R cannabinoid receptor
- Real-time kinetic measurements of ligand binding and receptor activation in cells
- Kinetic GPCR assays for profiling of ligands
11:30 am Using a Human iPSC-Based HCI Assays for Target Identification & Compound Screening
Synopsis
- A human iPSC-derived neuronal assay development
- The use of high content imaging for tau aggregation assay
- Genetic perturbations and compounds screening
12:00 pm Roundtable Discussion: Biosensor Assays for Measuring the Kinetics of GPCR Targeting & Multiplexed Bioactivity & Selectivity Screening for Streamlined Hit Identification
Synopsis
- Join this session for an interactive discussion on how to leverage kinetic based, biosensor assays and multiplexing to better understand context-dependent GPCR activity to empower novel drug discovery
1:00 pm Lunch Break & Networking
Navigating On Target Effect, Biomarker Identification & Patient Selection Challenges to Successfully Translate Disease Relevant GPCR Targeting Candidates into Clinic
2:00 pm Panel discussion: Decipher the Biology & Achieve Therapeutic Potential of Human GPCRs from Discovery to Clinical Development
Synopsis
- How to overcome translational challenges such as animal model selection, off target effects, biomarker identification and patient selection to develop a robust pipeline of safe, effective and disease relevant GPCRs targeting drugs • How can previous clinical data of GPCRs candidate relate to new findings and novel strategies
- How do we efficiently identify, and successfully address challenges that arise in the clinic for previously inaccessible
- GPCRs drug targets by leveraging computational tools, human genetic data available and lessons learnt
3:00 pm Integrating Medicinal Chemistry & Chemical Biology for a Translational GPCR Drug Discovery Strategy
Synopsis
- Labelled chemical probes are instrumental in target localization, mechanistic studies, assay development, and establishing biomarkers for target engagement.
- Integrating medicinal chemistry with chemical biology in a comprehensive, translational end-to-end drug discovery strategy can expedite the development of novel GPCR therapeutics.
- Productive partnerships between industry and academia can significantly accelerate drug discovery activities.
3:30 pm GPR65 Inhibition as a Strategy to Overcome Chronic Acidosis-Mediated Immune Suppression in Solid Tumours & Identification of PTT-4256 as a Clinical Development Candidate
Synopsis
- Genetic validation of GPR65 as an immuno-oncology target
- PoC studies with tool GR65 inhibitor molecules demonstrating efficacy in pre-clinical tumour models
- Identification of PTT-4256 as a first in class inhibitor of GPR65 and path to the clinic
4:00 pm Optimising Binding Kinetics Yields Insurmountable MC2 Receptor Antagonists for the Treatment of Diseases of ACTH Excess
Synopsis
- Diseases such as Cushing’s and Congenital Adrenal Hyperplasia are characterised by supraphysiological levels of the hormone ACTH. MC2R antagonists should inhibit this effect, but are at risk of being out-competed by high ACTH levels, resulting in very high doses being required for efficacy
- This talk will describe the discovery and characterisation of MC2R antagonists with slow dissociation kinetics that display insurmountable antagonism
- These compounds show significantly enhanced efficacy at low doses in in vivo models of ACTH excess, and promise to be more effective in a wider patient population where ACTH levels can vary significantly