Though many compounds that bind or prevent binding to G protein-coupled receptors (GPCRs) have successfully been developed into therapeutic agents, often details on how the drug achieves its effect are not clear. Not only do GPCRs control multiple signaling pathways, but GPCRs have their own complicated kinetic, cellular location and signaling life cycle, which varies from one receptor type to another and its cellular environment. Part 2 of our back-to-back GPCR meetings focuses on recently tractable pharmacologic complexities in the field, receptor-associated proteins that are emerging as drug targets and case-studies of lead compounds, especially allosteric modulators, that are progressing in development. 

Preliminary Agenda

Pharmacological Complexities

The Activated Conformation of GPCRs and the Mechanism of Activation of G Proteins

Roger K. Sunahara, Ph.D., Professor of Pharmacology, Department of Pharmacology, University of Michigan Medical School

GPCR Trafficking and Endosomal Signaling

Adriano Marchese, Ph.D., Associate Professor, Pharmacology, Stritch School of Medicine, Loyola University Chicago

Opioid Receptor Trafficking, Signaling and Physiology

Manoj Puthenveedu, Ph.D., Assistant Professor, Biological Sciences and The Center for the Neural Basis of Cognition, Carnegie Mellon University

Receptor Binding Kinetics in GPCR Drug Discovery: The Good, the Bad, and the Confusing

Brian J. Murphy, Ph.D., Senior Principal Scientist, Fibrosis Drug Discovery, Bristol-Myers Squibb

Allosteric Modulation

Identification of Orthosteric and Allosteric Residues Important for FFAR1 Binding and Function

Gayathri Swaminath, Ph.D., Principal Scientist, Metabolic Disorders, Amgen

Allosteric Ligands of Metabotropic Glutamate Receptor 5 Have Biased Agonism and Cooperativity

Karen Gregory, Ph.D., Postdoctoral Fellow, Laboratory of Arthur Christopolous, Department of Drug Discovery Biology, Monash University, Australia

Identifying Bias in CCR1 Antagonists

Annette Gilchrist, Ph.D., Assistant Professor, Pharmaceutical Sciences, Midwestern University

GPCR Modifications and Associated Proteins: New Discovery Targets?

Exploring Protease-activated Receptor Biased Signaling Inside and Outside of the Cell

JoAnn Trejo, Ph.D., Professor, Pharmacology, University of California San Diego

Heterologous Desensitization of GPCR-RTK Transactivation

Michael Beazely, Ph.D., Assistant Professor, School of Pharmacy, University of Waterloo, Canada

Crystal Structures of Peptide-Bound RAMP-GPCR Complexes

Augen A. Pioszak, Ph.D., Assistant Professor, Department of Biochemistry and Molecular Biology, University of Oklahoma Health Sciences Center

For questions or suggestions about the meeting, please contact:
Anjani Shah, Ph.D.
Conference Director
Cambridge Healthtech Institute
T: (+1) 781-972-5400 headquarters; 914-723-0255 (direct)

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

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Molecular Sensing 

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The exhibit hall was sold out in 2014, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2015, contact:

Jon Stroup
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