Despite their fruitful history in the drug development industry, discovering or designing new therapeutic agents that modulate a GPCR in a specific way is still a challenge, and in fact is undergoing a renewal because of explosion of new knowledge about their structure and ways to more precisely control their signaling via which G protein or other receptor-associated protein they couple to (biased signaling). Part 1 of CHI’s back-to-back GPCR meetings will focus on structural aspects of GPCRs and new assays, technologies and approaches for discovering and designing GPCR-targeted compounds.

Preliminary Agenda

GPCR Conformation and Biased Signaling Advances

KEYNOTE: New Structural and Biological Insights to Functional Selectivity 

Bryan Roth, M.D., Ph.D., Professor, Department of Pharmacology, University of North Carolina Medical School

GPCR Ligand Kinetics and Conformational Dynamics

Thomas P. Sakmar, M.D., Professor, Chemical Biology and Signal Transduction, The Rockefeller University

Biased Signaling as a Common Theme in Receptor Signaling

Brian J. Arey, Ph.D., Senior Principle Scientist, Cardiovascular Drug Discovery, Bristol-Myers Squibb Co.

Biosensors for Probing GPCR Conformation

Wei Liu, Ph.D., Assistant Professor, Department of Chemistry and Biochemistry, Arizona State University

Real-time, SPR Monitoring of Small Molecule Binding Events on a Nanodisc-Reconstituted GPCR

Nicolas Bocquet, Ph.D., Scientist, Pharma Research and Early Development (pRED), Roche Innovation Center Basel, F. Hoffmann-La Roche

GPCR Structure-Based Design and Computational Chemistry

Computational Methods to Identify Allosteric Binding Sites for Design of Biased Ligands for GPCRs

Nagarajan Vaidehi, Ph.D., Professor, Immunology, City of Hope, Beckman Research Institute

Exploring Structural Aspects of Biased Signaling

Mark G. Bures, Ph.D., Research Advisor, Chemistry, Eli Lilly & Co.

New Approaches for GPCR-Targeted Drug Discovery

New, Rapid GPCR-Screening Methods for Drug DiscoverySamantha J. Allen, Ph.D., Associate Principal Scientist, Screening and Protein Sciences, Merck  

Fragment-Based Lead Generation on a Proteinase-Activated GPCR

Niek Dekker, Ph.D., Principal Scientist, Discovery Sciences, AstraZeneca

The Power of Multi-Faceted Live-Cell Molecular Pharmacology Profiling

Kevin Pfleger, Ph.D., Associate Professor, Molecular Endocrinology & Pharmacology, Harry Perkins Institute of Medical Research, University of Western Australia

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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2014 Discovery on Target Brochure  




Molecular Sensing 

Rosa Drug Development Advisors




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
Sr. Business Development Manager

Westin Boston Waterfront


Westin Boston Waterfront
425 Summer Street
Boston, MA 02210