Day Two

Thursday, March 24 2022 | 8.30 AM - 3.00 PM

8:30 am Morning Networking Coffee

8:50 am Chair’s Opening Remarks

Exploring Emerging GPCR-Targeting Modalities for Drug Discovery

9:00 am Panel Discussion: The Future of Biologics to Develop Next Generation GPCR-Targeted Therapeutics


Biologics offer great potential in developing therapeutics targeting GPCRs due to their high affinity, selectivity, and long half-life. While many antibodies to GPCRs are in clinical trials and two antibodies have been FDA approved, further effort is needed to promote the rate of advancement of biologics targeting GPCRs. We will discuss the current challenges and solutions to enable rapid identification, precision engineering and selection of highly specific antibodies to transform GPCR drug discovery

  • How to develop of highly selective and specific biologics that recognize conformational determinants leading to novel GPCR therapeutics?
  • How to increase hits with consideration for receptor cross reactivity?
  • How to improve immunogenicity and enhanced efficacy and safety of novel antibodies?

10:00 am Salipro DirectMX™ Enables Discovery of Novel Therapeutics Against GPCRs


  • Introduction to the Salipro DirectMX™ technology
  • How to use the Salipro technology in antibody discovery, structure biology and for development of small molecular compounds
  • The chemokine receptor CXCR4 is a validated oncology target, and the development of new compounds has been hampered by difficulties purifying the native receptor
  • Showcasing Salipro DirectMX™ for CXCR4, its characterization, and the Cryo-EM structure determination of the native human wildtype CXCR4

10:30 am Morning Networking Break

Expanding GPCR-Targeting Modalities Beyond Traditional Small Molecules

11:30 am Strategies & Successes to Discover Antibodies as the Next Potential Modality Towards Drugging GPCRs


  • Expanding modality selection for greater receptor immunogenicity and functionality
  • Developing novel tools for high-throughput sampling and miniaturization of assays to effectively screen for functional antibodies

12:00 pm The Discovery of Therapeutic Antibodies Targeting Specific Conformations of GPCRs


  • Use of ConfoBody to generate immunogen towards antibody discovery on GPCR
  • Successful development of agonist VHH to GPCRs
  • New modality towards undruggable GPCR

12:30 pm Orion Biotechnology: Unlocking the Therapeutic Potential of Complex GPCRs Using a Novel Modality


  • Unlocking the therapeutic potential of GPCRs with a novel drug modality and purpose-built discovery platform
  • Addresses previously undruggable GPCR targets by precision engineering ligands of peptide and protein GPCRs to develop analogs with superior binding affinity, potency, and pharmacological control, offering significant advantages over small molecule and antibody approaches
  • Advancing a diversified pipeline of potential first-in-class/best-in-class therapeutics against high value GPCR targets in oncology and other serious diseases

1:00 pm Networking Lunch

Elevating the Biological Relevance & Therapeutic Value of GPCRs for Various Disease Indications

2:00 pm Pioneering a Novel Macrophage Conditioning Approach Through GPR65 to Advance Cancer Survival


  • Introduction to the pH sensing GPCR, GPR65, as a genetically validated IO target
  • In vivo model selection based on biological rationale, gene expression profiling and characterization of the TME
  • Assessment of the effects of a GPR65 antagonist on tumor growth

2:30 pm 4D Pharmacology – Multidimensional Therapeutic Design for AgingRelated Disease

  • Stuart Maudsley Odysseus Professor of Receptor Pharmacology & Vice Chair & Co-Founder, University of Antwerp & heptOME


  • GPCRs can act as key regulators of the aging process
  • GPCRs function in multiple dimensions
  • Age-related pathobiology underpins a diverse range of disease processes

3:00 pm Chair’s Closing Remarks & End of GPCR Pathway & Function Focus Day