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This meeting took place in 2012
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G Protein-Coupled Receptors: Molecular Mechanisms and Novel Functional Insights (B4)
Organizer(s) Arthur Christopoulos and Michel Bouvier
February 17—22, 2012
Fairmont Banff Springs • Banff, AB Canada
Abstract Deadline: Oct 17, 2011
Late Abstract Deadline: Nov 18, 2011
Scholarship Deadline: Oct 17, 2011
Early Registration Deadline: Dec 19, 2011
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.
View Scholarships/Awards
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.
View Scholarships/Awards
No registration fees are used to fund entertainment or alcohol at this conference
FRIDAY, FEBRUARY 17
SATURDAY, FEBRUARY 18
SUNDAY, FEBRUARY 19
MONDAY, FEBRUARY 20
TUESDAY, FEBRUARY 21
WEDNESDAY, FEBRUARY 22
Conference Program Print | View meeting in 12 hr (am/pm) time
FRIDAY, FEBRUARY 17
19:15—20:30
Welcome and Keynote Address
Marc G. Caron,
Duke University Medical Center, USA
Integrated Approaches to Understanding Drug Action at GPCRs
Integrated Approaches to Understanding Drug Action at GPCRs
08:00—11:15
GPCR Signaling I
*
Stephen J. Hill,
University of Nottingham, UK
Jennifer L. Whistler,
University of California, San Francisco, USA
Opioid Receptor Trafficking in Physiology and Disease
Opioid Receptor Trafficking in Physiology and Disease
Paul A. Insel,
University of California, San Diego, USA
Identification of New GPCR Targets for Cardiac Fibrosis
Identification of New GPCR Targets for Cardiac Fibrosis
Hugh Rosen,
ActivX Biosciences, USA
Chemical and Biological Insights from Alternate Binding Mode Agonists of SIP1 Receptor
Chemical and Biological Insights from Alternate Binding Mode Agonists of SIP1 Receptor
Evi Kostenis,
University of Bonn, Germany
Label Free Technology Platforms to Studying Pleiotropic 7TM Receptor Signaling
Label Free Technology Platforms to Studying Pleiotropic 7TM Receptor Signaling
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
Short Talk: A G Protein-Biased mu-opioid Receptor Ligand Elicits Potent Analgesia but Reduced Constipation and Respiratory Depression Compared to Morphine in Rodents
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
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
17:00—19:00
GPCR Physiology I
*
Laura M. Bohn,
The Scripps Research Institute, USA
Michel Bouvier,
University of Montreal, Canada
Targeting G Protein-Coupled Receptor Folding and Their Export from Endoplasmic Reticulum for Drug Discovery
Targeting G Protein-Coupled Receptor Folding and Their Export from Endoplasmic Reticulum for Drug Discovery
Brigitte L. Kieffer,
Douglas Institute, Canada
Delta Opioid Receptor Imaging in vivo: Anatomy, Dynamics and Physiology
Delta Opioid Receptor Imaging in vivo: Anatomy, Dynamics and Physiology
Stefano Marullo,
Institut Cochin, France
The beta2 Adrenergic Receptor as a Bacterial Entry Receptor
The beta2 Adrenergic Receptor as a Bacterial Entry Receptor
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)
Short Talk: Therapeutic Inhibition of Chemokine Receptors Using Nanobodies (VHH-Based Single Variable Domains)
08:00—11:15
Allosteric Modulation of GPCRs
*
Patrick M. Sexton,
Monash University, Australia
Arthur Christopoulos,
Monash University, Australia
Allosteric Modulation of GPCRs: From Function to Structure
Allosteric Modulation of GPCRs: From Function to Structure
Jean-Philippe Pin,
Montpellier University, France
Structural Dynamics of Metabotropic Glutamate Receptors
Structural Dynamics of Metabotropic Glutamate Receptors
Craig W. Lindsley,
Vanderbilt University, USA
Discovery of Small Molecule Modulators of Family A and C GPCRs
Discovery of Small Molecule Modulators of Family A and C GPCRs
Christian C. Felder,
Karuna Pharmaceuticals, USA
Challenges and Opportunities in Translating Allosteric Modulator-Based Drug Discovery
Challenges and Opportunities in Translating Allosteric Modulator-Based Drug Discovery
Kenneth E. Carlson,
Ironwood Pharmaceuticals, USA
Short Talk: Direct Interaction between an Allosteric Agonist Pepducin and the Chemokine Receptor CXCR4
Short Talk: Direct Interaction between an Allosteric Agonist Pepducin and the Chemokine Receptor CXCR4
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
Short Talk: Identification of a Small Molecule-Ligand-Binding Pocket in a G Protein-Coupled Receptor Using Genetically-Encoded Photocrosslinkers
17:00—19:00
GPCR Signaling II
*
Michel Bouvier,
University of Montreal, Canada
Stephane A. Laporte,
McGill University, Canada
Biased Modulation of the Prostaglandin FP Receptor
Biased Modulation of the Prostaglandin FP Receptor
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
Crystal Structure of the beta2-Adrenergic Receptor in Complex with Gs: Elucidation of the Mechanism for Receptor-Mediated Nucleotide Exchange on Heterotrimeric G Proteins
JoAnn Trejo,
University of California, San Diego, USA
Regulation of GPCR Signaling by Ubiquitination
Regulation of GPCR Signaling by Ubiquitination
Martin Beaulieu,
Universite Laval, Canada
Short Talk: Quantitative Characterization of RTK-GPCR Transactivation Using Spatial Intensity Distribution Analysis (SpIDA)
Short Talk: Quantitative Characterization of RTK-GPCR Transactivation Using Spatial Intensity Distribution Analysis (SpIDA)
08:00—11:15
GPCR Physiology II
*
Brigitte L. Kieffer,
Douglas Institute, Canada
Laura M. Bohn,
The Scripps Research Institute, USA
Animal Model Correlates of GPCR Functional Selectivity: Studies of the Serotonin 2A Receptor
Animal Model Correlates of GPCR Functional Selectivity: Studies of the Serotonin 2A Receptor
Ilpo Huhtaniemi,
Imperial College London, UK
In vivo Demonstration of the Role of Dimerization for LH Receptor
In vivo Demonstration of the Role of Dimerization for LH Receptor
Bernhard Bettler,
University of Basel, Switzerland
Beyond GABA-B Receptor Heteromers: Insights into the Role of Auxiliary Subunits
Beyond GABA-B Receptor Heteromers: Insights into the Role of Auxiliary Subunits
Andrew B. Tobin,
University of Glasgow, Scotland
Dissecting the in vivo Roles of GPCR Phosphorylation
Dissecting the in vivo Roles of GPCR Phosphorylation
Greg Polites,
Sanofi-Aventis, USA
Short Talk: The CreLuc Reporter Mouse Model: A Transgenic Bioimaging Mouse Model that can Assay Ligand Activation of GPCRs
Short Talk: The CreLuc Reporter Mouse Model: A Transgenic Bioimaging Mouse Model that can Assay Ligand Activation of GPCRs
Ralf Jockers,
Institute Cochin, France
Short Talk: Rare MTNR1B Variants Impairing Melatonin MT2 Receptor Function Strongly Contribute to Type 2 Diabetes
Short Talk: Rare MTNR1B Variants Impairing Melatonin MT2 Receptor Function Strongly Contribute to Type 2 Diabetes
17:00—19:00
Structural and Computational Studies of GPCRs
Brian K. Kobilka,
Stanford University School of Medicine, USA
Structural Insights into the Dynamic Process of G Protein Coupled Receptor Activation
Structural Insights into the Dynamic Process of G Protein Coupled Receptor Activation
Patrick M. Sexton,
Monash University, Australia
Polar Residues of the Transmembrane Domain of the Glucagon-like Peptide 1 Receptor Control Ligand-Directed Biased Signaling
Polar Residues of the Transmembrane Domain of the Glucagon-like Peptide 1 Receptor Control Ligand-Directed Biased Signaling
Tara Mirzadegan,
Janssen R&D Pharmaceutical Companies of Johnson & Johnson, USA
Bioinformatic Studies of GPCRs: From Sequence to Structure
Bioinformatic Studies of GPCRs: From Sequence to Structure
Nevin A. Lambert,
Medical College of Georgia, USA
Short Talk: Transient Self-Association of beta2 Adrenergic and CXCR4 Receptors
Short Talk: Transient Self-Association of beta2 Adrenergic and CXCR4 Receptors
08:00—11:00
Changing Paradigms for GPCR Drug Discovery
*
Christian C. Felder,
Karuna Pharmaceuticals, USA
Marcel Hibert,
University of Strasbourg, France
Novel FRET-Based Approaches to GPCR Drug Screening and more
Novel FRET-Based Approaches to GPCR Drug Screening and more
Stephen Rees,
AstraZeneca, UK
Drug Discovery Challenges for Orphan GPCRs
Drug Discovery Challenges for Orphan GPCRs
Stephen J. Hill,
University of Nottingham, UK
New Insights into GPCR Pharmacology Using Fluorescent Ligands
New Insights into GPCR Pharmacology Using Fluorescent Ligands
Ron O. Dror,
Stanford University, USA
Short Talk: Revealing the Atomic-Level Mechanisms of GPCR Activation and Drug Binding through Long-Timescale Simulation
Short Talk: Revealing the Atomic-Level Mechanisms of GPCR Activation and Drug Binding through Long-Timescale Simulation
17:00—19:00
New Topics in GPCR Structure and Function
*
Andrew B. Tobin,
University of Glasgow, Scotland
Martin J. Lohse,
Max Delbrück Center for Molecular Medicine, Germany
Single Molecule Studies of GPCRs
Single Molecule Studies of GPCRs
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
From a Few X-Ray Structures of GPCRs to Predictive Models of Many in Different States: Opportunities and Limitations
J. Silvio Gutkind,
University of California, San Diego, USA
Novel GPCR-Regulated Oncogenic and Pro-Metastatic Signaling Circuitries
Novel GPCR-Regulated Oncogenic and Pro-Metastatic Signaling Circuitries
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
Short Talk: Single Molecule Studies of Adenosine Receptors Compartmentation in Supported-Native Membranes by Correlated Electron and Fluorescence Microscopies
*Session Chair †Invited, not yet responded.
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