8:00 am Registration Opens

8:50 am Chair’s Opening Remarks

Current State of Play: The GPCR Drug Discovery & Development Landscape

9:00 am Panel Discussion: What Does the Next 5 Years of GPCR Drug Discovery & Development Look Like?

  • Alan Kopin Co-Founder & Chief Scientific Officer, On Target Therapeutics
  • Jeff Finer Chief Executive Officer, Septerna

Synopsis

  • Exploring the current lay of the land; which GPCRs show most promise now and where does the future lie?
  • What technologies are the most exciting right now and will propel the field forward?
  • How do we increase the number of antibody therapeutics in the GPCR market

Spotlighting the Tools Enhancing our Understanding of GPCR Structural & Changing Conformational Biology & Validation in Drug Discovery

9:45 am Early-Stage Development of BRET-Based Assays to Characterize the Activation of the Human Adhesion GPCR ADGRE5

Synopsis

  • Applying mechano-stimulation to study human ADGRE5 activation revealed by BRET-based biosensors
  • Demonstrating the mechanistic aspects of ADGRE5 receptor activation and impact on actin remodeling, exposing a possible mechanism by which hADGRE5 may promote tumor metastasis
  • Showcasing the future for the application of different technologies to study adhesion GPCR biology and develop screening assays to identify novel therapeutics targeting them in a pathophysiological setting

10:15 am Progressing Beyond Static Structural GPCR Understanding

Synopsis

  • Strategies to engineer, express, and purify (orphan) GPCRs
  • Using cryo-EM to solve small molecule-bound GPCR structures in multiple complexes to progress structure-based drug discovery
  • Achieving strong molecular dynamic understanding using experimental structures in tandem with computational modelling techniques

10:45 am

Morning Break & Speed Networking

11:15 am Using Cryo-EM Techniques to Empower our Attempts at Drug Docking

Synopsis

  • Improving the hit-rate through bioinformatics to predict high resolution homology models
  • Pinpointing how drug docking will accelerate drug discovery through more effective translation in vitro
  • Unveiling the role highly accurate alpha fold modelling will play in identifying allosteric and unknown pockets

11:45 am Sane in the Membrane – Salipro Platform for GPCRs

Synopsis

  • Salipro platform allows direct reconstitution of membrane proteins incl GPCRs, ion channels from cells
  • Salipro platform presents new opportunities for de novo development and characterisation of biologics and small molecules
  • Case studies on Salipro-CXCR4 and Salipro-CXCR4-CXCL12 complex

12:15 pm Unlocking Difficult-to-Drug GPCRs with GPCR Native Complexes

Synopsis

  • Rapid structure determination to fuel structure-based drug design
  • Expanding chemical space with new hit identification technologies
  • Revealing novel molecular insights of GPCR modulation

12:45 pm

Lunch

Pinpointing the Modalities Showing Most Promise in Targeting GPCRs

1:45 pm Showcasing Discovery and Validation of a Known GPCR Target Using an Antibody [case study]

Synopsis

  • Highlighting the existing challenges with antibody modulated GPCR targeting
  • Relaying a novel approach used to target with a large molecule
  • Spearheading early clinical development

2:15 pm Structural Insights into Antibody-Based Targeting of a Family A GPCR

Synopsis

  • Cryo-EM structure of a family A GPCR in complex with an extracellular antibody
  • Structural insights into a GPCR of therapeutic interest
  • Insights into antibodies as a GPCR structural chaperone and targeting modality

2:45 pm A Lipidated Protease-Resistant Chemerin Peptide Offers a Novel Therapeutic for Dry Eyes

  • Alan Kopin Co-Founder & Chief Scientific Officer, On Target Therapeutics
  • Gary Jacob Chief Executive Officer, OKYO Pharma

Synopsis

  • A systematic approach to developing lipidated peptide ligands
  • In vitro and in vivo testing of lipidated stable chemerin
  • Moving from preclinical studies into the clinic

3:15 pm

Afternoon Break & Networking

3:45 pm Multiplexed Validation of Anti-GPCR Antibodies to Define the GPCR-RAMP Interactome

  • Thomas Sakmar Professor, Senior Physician, The Rockefellar University

Synopsis

  • Creating a multiplexed suspension bead array system to validate hundreds of anti- GPCR antibodies
  • Validating an expression library of >200 dual-epitope-tagged GPCRs
  • Demonstrating sensitive multiplexed detection of GPCR-RAMP complexes from cell extracts

4:15 pm Using a Novel Platform to Build Small Molecule Correctors of a Misfolded GPCR

Synopsis

  • Synthetic biology to develop custom cellular trafficking assays
  • High throughput nanoscale chemistry to build potent and pharmaceutically tractable small molecules
  • Scaled multiplexed assays to optimize the ‘mutational generality’ of hit series

4:45 pm Panel Discussion: Which Modality to Choose? Debating the Implementation of Biologics vs Small Molecules

Synopsis

  • With only 3 FDA approved antibodies and roughly 20 in development, what are the hurdles to showing efficacy in antibody drug development for GPCRs
  • Will antibodies replace small molecules in the GPCR space?
  • Are there indications where an antibody may fair better or equal to small molecules (oncology space?)

5:30 pm End of Day One