GPCR-Based Drug Discovery - Part 1 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 One:

The first meeting in the set, Part 1: Screening and Structure-based Approaches, will include presentations and discussions related to discovering and designing compounds that act on GPCRs. Recent advances in biophysical approaches to studying GPCRs have enabled progress in both, structure-based design of ligands for GPCRs, and new screening methods, which though not as high throughput as traditional cell-based assays, allow receptors to be studied in more relevant cellular contexts.

Preliminary Agenda


Biophysical Approaches for Studying GPCRs

KEYNOTE PRESENTATION: NMR and Allosteric Signal Transduction Networks in the β1-Adrenergic Receptor

Gebhard F.X. Schertler, Ph.D., Professor, Head of Biology and Chemistry, Paul Scherrer Institut

GPCR Dynamics as Revealed by NMR

Matthew Eddy, Ph.D., Postdoctoral Fellow, Ray Stevens Laboratory, The Bridge Institute, University of Southern California

Combining Biophysical Techniques to Identify and Optimize New Chemical Entities in Targeted GPCR Drug Discovery

Daniel Mattle, Ph.D., Roche Postdoctoral Research Fellow, Roche Pharma Research and Early Development (pRED), Roche Innovation Center Basel

A2AR Ligand Binding Kinetics using Fluorescence Anisotropy: Determining Binding Rates in the Ligand Depletion Regime

Anne Robinson, Ph.D., Professor and Chair, Chemical & Biomolecular Engineering, Tulane University


GPCR Structural Insights for Ligand Design

Revealing the Structural Basis for GPCR Drug Action through Atomic-Level Simulation

Ron Dror, Ph.D., Associate Professor of Computer Science and, by courtesy, Molecular and Cellular Physiology, Stanford University

Changing Landscape in GPCR-Targeted Drugs

Andrew Tebben, Ph.D., Senior Principal Scientist, Molecular Structure and Design, Bristol Myers Squibb Co.

Molecular and Structural Mechanisms of Opioid Receptor Function

Aashish Manglik, M.D., Ph.D., Stanford Distinguished Fellow, Department of Molecular and Cellular Physiology, Stanford University

Probing the Functional and Therapeutic Significance of GPCR Oligomerization at the Nano-Scale via Super-Resolution Imaging

Aylin Hanyaloglu, Ph.D., Senior Lecturer, Institute of Reproductive and Developmental Biology, Imperial College London

GPCR Drug Discovery at the Single Molecule Level

Tim Kaminski, Ph.D., Postdoctoral Fellow, Biophysics/Discovery Sciences, AstraZeneca




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