GPCR-Based Drug Discovery


G-protein coupled receptors (GPCRs) play roles in many physiological processes and have therefore been the target of medical therapeutics for decades. Their complexities in signaling though are still being unraveled and starting to be exploited for more targeted therapies. For example, therapeutics with fewer side effects are being sought by finding biased ligands of specific GPCRs that will activate or block the pathway of medical interest while not initiating less desirable signaling cascades that the GPCR also controls. Progress in biophysical techniques and cryo-electron microscopy have also aided targeted drug discovery against GPCRs by enabling biosensor-based screens or by helping elucidate structural features of GPCRs that guide structure-based drug design. At CHI’s well established GPCR-Based Drug Discovery conference, join colleagues and experts in the GPCR field who hail from both, academics and industry, to review advances in the field and discuss cutting edge topics impacting drug development against this very medically relevant class of drug targets.

Preliminary Agenda


Bias and Beyond:  Challenges and Opportunities in GPCR Drug Development
Ian James, PhD, Associate Director, Clinical Operations, Trevena Inc.

De novo Design of Gα Mimetics: Generalizable Tools for Allosteric Control of G Protein-Coupled Receptors
Christopher D. Bahl, PhD, Head of Protein Design, Institute for Protein Innovation

Structural Insights into Binding Specificity, Efficacy and Bias of Salmeterol, a β2 Adrenergic Receptor Partial Agonist
Matthieu Masureel, PhD, Postdoctoral Research Fellow, Kobilka Lab, Department of Molecular and Cellular Physiology, Stanford University 

Biophysical Approaches for GPCRs and Medicinal Chemistry Case Studies

Lessons Learned from Various GPCR Lead Optimization Projects
Chi Sum, PhD, Senior Research Investigator, Lead Discovery and Optimization, Bristol Myers Squibb & Co.

First Orally Bioavailable Antagonist of the Neuropeptide Y Receptor 2 (NPY2R)
Pierre Wasnaire, PhD, Senior Scientist, Pharmaceuticals R&D, Bayer AG

Nanodiscs for GPCRs
Daniel Oprian, PhD, Professor, Biochemistry, Brandeis University

Non-Classical Signaling

Understanding the Consequences of GPCR Dimerization
Terry Hébert, PhD, Professor, Department of Pharmacology and Therapeutics, McGill University

Non-Traditional Aspects of Gαs: Interaction with Ubiquitin and Regulation of GPCR Endosomal Sorting
Christine Lavoie, PhD, Professor, Department of Pharmacology and Physiology, University of Sherbrooke

GPCRs in Disease

GPR84: Can Context-Dependent Signaling Inform Therapeutic Direction?
Carleton Sage, PhD, Vice President, Computational Sciences, Beacon Discovery

CollaborativeDrugDiscovery_horizontalGPCR-Based Drug Discovery Using Smart Drug Discovery Software to Enhance Collaboration and Manage Disperse Assay Data
Robert Thorn, PhD, Customer Engagement Scientist, Collaborative Drug Discovery, Inc.

* The program is subject to change without notice, due to unforeseen reason.

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