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

  • Arne Rufer Expert Scientist, Science, Technology & Discovery Lead, Roche

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

  • Arne Rufer Expert Scientist, Science, Technology & Discovery Lead, Roche

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

4:30 pm End of GPCR-Targeted Drug Discovery Summit Europe 2024