Web Desc
G Protein-Coupled Receptors: Molecular Mechanisms and Novel Functional Insights
Organizer(s): Arthur Christopoulos and Michel Bouvier
Date: February 17 - 22, 2012
Location: Fairmont Banff Springs, Banff, AB, Canada
Sponsored by Bayer USA Foundation, Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Merck & Co., Inc. and Vertex Pharmaceuticals Incorporated
Summary of Meeting:
The seven transmembrane-spanning G protein-coupled receptors (GPCRs) are the largest superfamily of receptors in the human genome, are involved in virtually all physiological processes and represent the targets for at least 30% of all current medicines. Recent years have witnessed the coalescing of a number of important paradigms, including ligand-biased signaling, allosteric modulation and receptor dimerization, with substantial advances in structural determination, chemical biology and in vivo approaches to studying GPCR function. These developments will undoubtedly have a profound impact on future approaches to GPCR-based drug discovery. This meeting will focus on the interplay between these developments, and how they can be exploited to advance the translational application of cutting-edge GPCR-based research.
Scholarship Deadline: October 17 2011
Discounted Abstract Deadline: October 17 2011
Abstract Deadline: November 18 2011
Discounted Registration Deadline: December 19 2011
Keystone Symposia thanks our Sponsor(s) for generously supporting this meeting:
Bayer USA FoundationJohnson & Johnson Pharmaceutical Research & Development, L.L.C.Merck & Co., Inc.Vertex Pharmaceuticals Incorporated
We gratefully acknowledge additional in-kind support for this conference from those foregoing speaker expense reimbursements:

AstraZeneca

Eli Lilly and Company

Heptares Therapeutics Ltd


Masataka Harada
We gratefully acknowledge the generous grant for this conference provided by:

National Institute on Drug Abuse (NIDA)
Grant No. 1R13DA032154-01
The views expressed in written conference materials or publications and by speakers and moderators do not necessarily reflect the official policies of the Department of Health and Human Services; nor does mention of trade names, commercial practices, or organizations imply endorsement by the U.S. Government.
We appreciate the organizations that provide Keystone Symposia with additional support, such as marketing and advertising:

Click here to view more of these organizations
Special thanks to the following for their support of Keystone Symposia initiatives to increase participation at this meeting by scientists from underrepresented backgrounds:

Click here to view more of these organizations

Program

Friday, February 17 | 3:00PM - 7:30PM
Registration
Room: Van Horne Foyer


Friday, February 17 | 6:15PM - 7:15PM
Refreshments
Room: Van Horne Foyer


Friday, February 17 | 7:15PM - 8:30PM
Welcome and Keynote Address
Room: Van Horne Ballroom C

Speaker 1 of 2
* Arthur Christopoulos, Monash University, Australia

Friday, February 17 | 7:15PM - 8:30PM
Welcome and Keynote Address
Room: Van Horne Ballroom C

Speaker 2 of 2
Marc G. Caron, Duke University Medical Center, USA
Integrated Approaches to Understanding Drug Action at GPCRs

Saturday, February 18 | 7:00AM - 8:00AM
Breakfast
Room: Van Horne Ballroom A-B


Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 1 of 7
* Stephen J. Hill, University of Nottingham, UK

Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 2 of 7
Jennifer L. Whistler, University of California, San Francisco, USA
Opioid Receptor Trafficking in Physiology and Disease

Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 3 of 7
Paul A. Insel, University of California, San Diego, USA
Identification of New GPCR Targets for Cardiac Fibrosis

Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 4 of 7
Evi Kostenis, University of Bonn, Germany
Label Free Technology Platforms to Studying Pleiotropic 7TM Receptor Signaling

Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 5 of 7
Hugh Rosen, ActivX Biosciences, USA
Chemical and Biological Insights from Alternate Binding Mode Agonists of SIP1 Receptor

Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 6 of 7
Jonathan D. Violin, Trevena Inc., USA
Short Talk: A G Protein-Biased mu-opioid Receptor Ligand Elicits Potent Analgesia but Reduced Constipation and Respiratory Depression Compared to Morphine in Rodents

Saturday, February 18 | 8:00AM - 11:15AM
GPCR Signaling I
Room: Van Horne Ballroom C

Speaker 7 of 7
Senthikumar Rajagopal, Virginia Commonwealth University, USA
Short Talk: Activation of G Protein-Coupled Bile Acid Receptor, TGR5 Induces Muscle Relaxation via PKA- and Epac-Mediated Inhibition of RhoA/Rho Kinase Pathway

Saturday, February 18 | 9:20AM - 9:40AM
Coffee Break
Room: Van Horne Foyer


Saturday, February 18 | 11:15AM - 11:15AM
On Own for Lunch and Recreation


Saturday, February 18 | 11:15AM - 1:00PM
Poster Setup
Room: Van Horne Ballroom A-B


Saturday, February 18 | 1:00PM - 10:00PM
Poster Viewing
Room: Van Horne Ballroom A-B


Saturday, February 18 | 4:30PM - 5:00PM
Coffee Available
Room: Van Horne Foyer


Saturday, February 18 | 5:00PM - 7:00PM
GPCR Physiology I
Room: Van Horne Ballroom C

Speaker 1 of 5
* Laura M. Bohn, The Scripps Research Institute, USA

Saturday, February 18 | 5:00PM - 7:00PM
GPCR Physiology I
Room: Van Horne Ballroom C

Speaker 2 of 5
Michel Bouvier, University of Montreal, Canada
Targeting G Protein-Coupled Receptor Folding and Their Export from Endoplasmic Reticulum for Drug Discovery

Saturday, February 18 | 5:00PM - 7:00PM
GPCR Physiology I
Room: Van Horne Ballroom C

Speaker 3 of 5
Brigitte L. Kieffer, Douglas Institute, Canada
Delta Opioid Receptor Imaging in vivo: Anatomy, Dynamics and Physiology

Saturday, February 18 | 5:00PM - 7:00PM
GPCR Physiology I
Room: Van Horne Ballroom C

Speaker 4 of 5
Stefano Marullo, Institut Cochin, France
The beta2 Adrenergic Receptor as a Bacterial Entry Receptor

Saturday, February 18 | 5:00PM - 7:00PM
GPCR Physiology I
Room: Van Horne Ballroom C

Speaker 5 of 5
David Maussang-Detaille, Leiden/Amsterdam Center for Drug Research, VU University Amsterdam, Netherlands
Short Talk: Therapeutic Inhibition of Chemokine Receptors Using Nanobodies (VHH-Based Single Variable Domains)

Saturday, February 18 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Van Horne Ballroom B-C


Saturday, February 18 | 7:30PM - 10:00PM
Poster Session 1
Room: Van Horne Ballroom A-B


Sunday, February 19 | 7:00AM - 8:00AM
Breakfast
Room: Van Horne Ballroom A-B


Sunday, February 19 | 7:30AM - 8:00AM
Poster Setup
Room: Van Horne BallroomA-B


Sunday, February 19 | 8:00AM - 5:00PM
Poster Viewing
Room: Van Horne Ballroom A-B


Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 1 of 7
* Patrick M. Sexton, Monash University, Australia

Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 2 of 7
Arthur Christopoulos, Monash University, Australia
Allosteric Modulation of GPCRs: From Function to Structure

Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 3 of 7
Jean-Philippe Pin, Montpellier University, France
Structural Dynamics of Metabotropic Glutamate Receptors

Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 4 of 7
Craig W. Lindsley, Vanderbilt University, USA
Discovery of Small Molecule Modulators of Family A and C GPCRs

Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 5 of 7
Christian C. Felder, Karuna Pharmaceuticals, USA
Challenges and Opportunities in Translating Allosteric Modulator-Based Drug Discovery

Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 6 of 7
Kenneth E. Carlson, Ironwood Pharmaceuticals, USA
Short Talk: Direct Interaction between an Allosteric Agonist Pepducin and the Chemokine Receptor CXCR4

Sunday, February 19 | 8:00AM - 11:15AM
Allosteric Modulation of GPCRs
Room: Van Horne Ballroom C

Speaker 7 of 7
Amy Grunbeck, Rockefeller University, USA
Short Talk: Identification of a Small Molecule-Ligand-Binding Pocket in a G Protein-Coupled Receptor Using Genetically-Encoded Photocrosslinkers

Sunday, February 19 | 9:20AM - 9:40AM
Coffee Break
Room: Van Horne Foyer


Sunday, February 19 | 11:15AM - 12:00PM
Lunch


Sunday, February 19 | 12:00PM - 2:30PM
Poster Session 2
Room: Van Horne Ballroom A-B


Sunday, February 19 | 4:30PM - 5:00PM
Coffee Available
Room: Van Horne Foyer


Sunday, February 19 | 5:00PM - 7:00PM
GPCR Signaling II
Room: Van Horne Ballroom C

Speaker 1 of 5
* Michel Bouvier, University of Montreal, Canada

Sunday, February 19 | 5:00PM - 7:00PM
GPCR Signaling II
Room: Van Horne Ballroom C

Speaker 2 of 5
Stephane A. Laporte, McGill University, Canada
Biased Modulation of the Prostaglandin FP Receptor

Sunday, February 19 | 5:00PM - 7:00PM
GPCR Signaling II
Room: Van Horne Ballroom C

Speaker 3 of 5
Roger K. Sunahara, University of California, San Diego, USA
Crystal Structure of the beta2-Adrenergic Receptor in Complex with Gs: Elucidation of the Mechanism for Receptor-Mediated Nucleotide Exchange on Heterotrimeric G Proteins

Sunday, February 19 | 5:00PM - 7:00PM
GPCR Signaling II
Room: Van Horne Ballroom C

Speaker 4 of 5
JoAnn Trejo, University of California, San Diego, USA
Regulation of GPCR Signaling by Ubiquitination

Sunday, February 19 | 5:00PM - 7:00PM
GPCR Signaling II
Room: Van Horne Ballroom C

Speaker 5 of 5
Martin Beaulieu, Universite Laval, Canada
Short Talk: Quantitative Characterization of RTK-GPCR Transactivation Using Spatial Intensity Distribution Analysis (SpIDA)

Sunday, February 19 | 7:00PM - 7:00PM
On Own for Dinner


Monday, February 20 | 7:00AM - 8:00AM
Breakfast
Room: Van Horne Ballroom A-B


Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 1 of 7
* Brigitte L. Kieffer, Douglas Institute, Canada

Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 2 of 7
Laura M. Bohn, The Scripps Research Institute, USA
Animal Model Correlates of GPCR Functional Selectivity: Studies of the Serotonin 2A Receptor

Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 3 of 7
Ilpo Huhtaniemi, Imperial College London, UK
In vivo Demonstration of the Role of Dimerization for LH Receptor

Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 4 of 7
Bernhard Bettler, University of Basel, Switzerland
Beyond GABA-B Receptor Heteromers: Insights into the Role of Auxiliary Subunits

Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 5 of 7
Andrew B. Tobin, University of Glasgow, UK
Dissecting the in vivo Roles of GPCR Phosphorylation

Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 6 of 7
Greg Polites, Sanofi-Aventis, USA
Short Talk: The CreLuc Reporter Mouse Model: A Transgenic Bioimaging Mouse Model that can Assay Ligand Activation of GPCRs

Monday, February 20 | 8:00AM - 11:15AM
GPCR Physiology II
Room: Van Horne Ballroom C

Speaker 7 of 7
Ralf Jockers, Institute Cochin, France
Short Talk: Rare MTNR1B Variants Impairing Melatonin MT2 Receptor Function Strongly Contribute to Type 2 Diabetes

Monday, February 20 | 9:20AM - 9:40AM
Coffee Break
Room: Van Horne Foyer


Monday, February 20 | 11:15AM - 11:15AM
On Own for Lunch and Recreation
Room: Van Horne A-B


Monday, February 20 | 11:15AM - 1:00PM
Poster Setup
Room: Van Horne Ballroom A-B


Monday, February 20 | 1:00PM - 10:00PM
Poster Viewing
Room: Van Horne Ballroom A-B


Monday, February 20 | 4:30PM - 5:00PM
Coffee Available
Room: Van Horne Foyer


Monday, February 20 | 5:00PM - 7:00PM
Structural and Computational Studies of GPCRs
Room: Van Horne Ballroom C

Speaker 1 of 5
* Fiona H. Marshall, Heptares Therapeutics Ltd., UK

Monday, February 20 | 5:00PM - 7:00PM
Structural and Computational Studies of GPCRs
Room: Van Horne Ballroom C

Speaker 2 of 5
Brian K. Kobilka, Stanford University School of Medicine, USA
Structural Insights into the Dynamic Process of G Protein Coupled Receptor Activation


Monday, February 20 | 5:00PM - 7:00PM
Structural and Computational Studies of GPCRs
Room: Van Horne Ballroom C

Speaker 3 of 5
Patrick M. Sexton, Monash University, Australia
Polar Residues of the Transmembrane Domain of the Glucagon-like Peptide 1 Receptor Control Ligand-Directed Biased Signaling

Monday, February 20 | 5:00PM - 7:00PM
Structural and Computational Studies of GPCRs
Room: Van Horne Ballroom C

Speaker 4 of 5
Tara Mirzadegan, Janssen R&D Pharmaceutical Companies of Johnson & Johnson, USA
Bioinformatic Studies of GPCRs: From Sequence to Structure

Monday, February 20 | 5:00PM - 7:00PM
Structural and Computational Studies of GPCRs
Room: Van Horne Ballroom C

Speaker 5 of 5
Nevin A. Lambert, Medical College of Georgia, USA
Short Talk: Transient Self-Association of beta2 Adrenergic and CXCR4 Receptors

Monday, February 20 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Van Horne Ballroom A-B


Monday, February 20 | 7:30PM - 10:00PM
Poster Session 3
Room: Van Horne Ballroom A-B


Tuesday, February 21 | 7:00AM - 8:00AM
Breakfast
Room: Van Horne Ballroom A-B


Tuesday, February 21 | 8:00AM - 11:00AM
Changing Paradigms for GPCR Drug Discovery
Room: Van Horne Ballroom C

Speaker 1 of 6
* Christian C. Felder, Karuna Pharmaceuticals, USA

Tuesday, February 21 | 8:00AM - 11:00AM
Changing Paradigms for GPCR Drug Discovery
Room: Van Horne Ballroom C

Speaker 2 of 6
Marcel Hibert, University of Strasbourg, France
Novel FRET-Based Approaches to GPCR Drug Screening and more

Tuesday, February 21 | 8:00AM - 11:00AM
Changing Paradigms for GPCR Drug Discovery
Room: Van Horne Ballroom C

Speaker 3 of 6
Stephen Rees, AstraZeneca, UK
Drug Discovery Challenges for Orphan GPCRs

Tuesday, February 21 | 8:00AM - 11:00AM
Changing Paradigms for GPCR Drug Discovery
Room: Van Horne Ballroom C

Speaker 4 of 6
Fiona H. Marshall, Heptares Therapeutics Ltd., UK
Structure Based Drug Discovery for GPCRs

Tuesday, February 21 | 8:00AM - 11:00AM
Changing Paradigms for GPCR Drug Discovery
Room: Van Horne Ballroom C

Speaker 5 of 6
Stephen J. Hill, University of Nottingham, UK
New Insights into GPCR Pharmacology Using Fluorescent Ligands

Tuesday, February 21 | 8:00AM - 11:00AM
Changing Paradigms for GPCR Drug Discovery
Room: Van Horne Ballroom C

Speaker 6 of 6
Ron O. Dror, Stanford University, USA
Short Talk: Revealing the Atomic-Level Mechanisms of GPCR Activation and Drug Binding through Long-Timescale Simulation

Tuesday, February 21 | 9:20AM - 9:40AM
Coffee Break
Room: Van Horne Foyer


Tuesday, February 21 | 11:00AM - 11:00AM
On Own for Lunch and Recreation


Tuesday, February 21 | 4:30PM - 5:00PM
Coffee Available
Room: Van Horne Foyer


Tuesday, February 21 | 5:00PM - 7:00PM
New Topics in GPCR Structure and Function
Room: Van Horne Ballroom C

Speaker 1 of 5
* Andrew B. Tobin, University of Glasgow, UK

Tuesday, February 21 | 5:00PM - 7:00PM
New Topics in GPCR Structure and Function
Room: Van Horne Ballroom C

Speaker 2 of 5
Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany
Single Molecule Studies of GPCRs

Tuesday, February 21 | 5:00PM - 7:00PM
New Topics in GPCR Structure and Function
Room: Van Horne Ballroom C

Speaker 3 of 5
Ruben Abagyan, University of California, San Diego, USA
From a Few X-Ray Structures of GPCRs to Predictive Models of Many in Different States: Opportunities and Limitations

Tuesday, February 21 | 5:00PM - 7:00PM
New Topics in GPCR Structure and Function
Room: Van Horne Ballroom C

Speaker 4 of 5
J. Silvio Gutkind, University of California, San Diego, USA
Novel GPCR-Regulated Oncogenic and Pro-Metastatic Signaling Circuitries

Tuesday, February 21 | 5:00PM - 7:00PM
New Topics in GPCR Structure and Function
Room: Van Horne Ballroom C

Speaker 5 of 5
Sophie Roizard, Ecole Polytechnique Fédérale de Lausanne, Switzerland
Short Talk: Single Molecule Studies of Adenosine Receptors Compartmentation in Supported-Native Membranes by Correlated Electron and Fluorescence Microscopies

Tuesday, February 21 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Cascade


Tuesday, February 21 | 8:00PM - 11:00PM
Entertainment
Room: Cascade


Tuesday, February 21 | 8:00PM - 11:00PM
Cash Bar
Room: Cascade


Wednesday, February 22 | 10:25AM - 10:25AM
Departure


*Session Chair.