Past Meeting | Keystone Symposia

This meeting took place in the past. Here is a list of meetings that are related:
GPCR Structure and Function: Taking GPCR Drug Development and Discovery to the Next Level (2018B8)
G Protein-Coupled Receptors: Structure, Signaling and Drug Discovery (2016B3)
G Protein-Coupled Receptors: Structural Dynamics and Functional Implications (2014Z1)

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: 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

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:

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.