GPCR-Based Drug Discovery - Part 2 Header


G protein-coupled receptors (GPCRs) have steadily remained an important target class for drug discovery because of the myriad of biological processes they initiate as transducers of extracellular signals to inside the cell. However, they have always been and still remain a complex target class. Their multi-membrane spanning structure makes them difficult to isolate. Their ability to couple to various intracellular messengers (G proteins and other proteins) complicates interpretation and measurement of downstream signaling.

This two-part meeting enables discovery biologists and chemists to share progress, advances and new strategies in discovering, designing and optimizing GPCR-targeted compounds as well as hear about new work from academia that sheds light on the pharmacological complexities of this receptor class. Updates and challenges of GPCR-targeted compounds advancing in the drug development pipeline will also be a part of the agenda. 

Part Two: 

The second meeting in the set, Part 2: Signaling and Pharmacological Complexities, explores the unique aspects of GPCR signaling which makes the receptors such challenging yet fruitful targets. With the difficulties of targeting GPCRs also come multiple avenues for their pharmacological modulation. Insights on receptor trafficking, modifications, desensitization and selective/biased coupling and how that impacts design of GPCR-targeted compounds will be discussed. Case studies of GPCR-targeted compounds advancing in preclinical or clinical development, including biased ligands and allosteric modulators, will also be featured.   

Preliminary Agenda


GPCR Complexities: Allosterism, Biased Signaling and More

Directing Opioid Receptor Signaling to Improve Analgesic Therapies

Laura M. Bohn, Ph.D., Professor, Departments of Molecular Therapeutics & Neuroscience, The Scripps Research Institute

Discovery of Non-Desensitizing, Selective CB2 Agonists

David J. Unett, Ph.D., Vice President, Receptor Pharmacology, Arena Pharmaceuticals

Positive Allosteric Modulators of mGlu4 for the Treatment of Parkinson’s Disease: From HTS to Pre-Clinical Leads

Corey R. Hopkins, Ph.D., Research Assistant Professor, Vanderbilt Center for Neuroscience Drug Discovery

NK1 Biased Signaling (Gs v.Gq v. Arrestin)

Thomas M. Frimurer, Ph.D., Associate Professor, The Novo Nordisk Foundation Centre for Basic Metabolic Research, University of Copenhagen

Extended cAMP GPCR-Generated Signaling

Thomas J. Gardella, Ph.D., Associate Professor, Medicine, Massachusetts General Hospital, Harvard


GPCRs in Disease

GPCRs in Cancer: an Untapped Opportunity

Paul Insel, M.D., Distinguished Professor, Pharmacology and Medicine, University of California San Diego

Drug Discovery with an Orphan GPCR

Alexander Gragerov, Ph.D., Senior Director of Research, Discovery, Omeros Corp.

Desensitization of Cardiac Adrenergic Receptor Signaling  Through Receptor Cross-Talk

Kevin Xiang, Ph.D., Professor, Pharmacology, University of California Davis


GPCR-Interacting Proteins

GPCR-Mediated G Protein Activation

Heidi Hamm, Ph.D., Professor, Department of Pharmacology, Vanderbilt University Medical Center

Biasing Beta2-Adrenergic Receptor Signaling

Jeffrey L. Benovic, Ph.D., Professor and Chair, Department of Biochemistry & Molecular Biology, Thomas Jefferson University




For questions or suggestions about the meeting, please contact:
Anjani Shah, Ph.D.
Conference Director
Cambridge Healthtech Institute
T: (+1) 781—247-6252
E: ashah@healthtech.com

For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Jon Stroup
Senior Manager, Business Development
Cambridge Healthtech Institute
T: (+1) 781-972-5483
E: jstroup@healthtech.com