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.
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.
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 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-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.
Cambridge Healthtech Institute
T: (+1) 781—247-6252
For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Senior Manager, Business Development
Cambridge Healthtech Institute
T: (+1) 781-972-5483