Web Desc
G Protein-Coupled Receptors
Organizer(s): Brian K. Kobilka, Martin J. Lohse and Thue W. Schwartz
Date: April 07 - 12, 2010
Location: Beaver Run Resort, Breckenridge, CO, USA
Supported by The Directors' Fund
For important information on the coronavirus, please click here
Summary of Meeting:
The large family of GPCRs includes many potential therapeutic targets, yet successful development of new drugs for GPCRs has been disappointing in spite of having access to all GPCR sequences in the genome, as well as physiologic insights from gene modification technology, larger more diverse compound libraries, and advances in high-throughput screening technologies. The goal of this meeting is to examine the challenges facing GPCR drug discovery, and to explore the application of structural biology, genomics and proteomics to GPCR target selection, and to lead identification and optimization.
Scholarship Deadline: December 7 2009
Discounted Abstract Deadline: December 7 2009
Abstract Deadline: January 5 2010
Discounted Registration Deadline: February 5 2010
We gratefully acknowledge additional support for this conference from:

Bristol-Myers Squibb Company

National Institute of General Medical Sciences (NIGMS)
Novus Biologicals, Inc.Transposagen Biopharmaceuticals, Inc.
We gratefully acknowledge additional in-kind support for this conference from those foregoing speaker expense reimbursements:

Sanofi-Aventis Pharma Deutschland GmbH

Vertex Pharmaceuticals Incorporated
We gratefully acknowledge the generous grant for this conference provided by:

National Institute of General Medical Sciences (NIGMS)
Grant No. 1R13GM093551-01
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

Wednesday, April 07 | 3:00PM - 7:30PM
Registration
Room: Foyer


Wednesday, April 07 | 6:30PM - 7:30PM
Refreshments
Room: Foyer


Wednesday, April 07 | 7:30PM - 8:30PM
Keynote Address
Room: Peaks 4-5

Speaker 1 of 2
* Brian K. Kobilka, Stanford University School of Medicine, USA

Wednesday, April 07 | 7:30PM - 8:30PM
Keynote Address
Room: Peaks 4-5

Speaker 2 of 2
Shaun R. Coughlin, University of California, San Francisco, USA
The Long Road from GPCR Cloning to a Drug: Lessons from Protease-Activated Receptor-1

Thursday, April 08 | 7:00AM - 8:00AM
Breakfast
Room: Summit Gallery


Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 1 of 7
* Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany

Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 2 of 7
Terry P. Kenakin, University of North Carolina at Chapel Hill, USA
Importance of Efficacy in GPCR Drug Discovery

Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 3 of 7
Robert J. Lefkowitz, HHMI/Duke University Medical Center, USA
Arrestin Signaling and Arrestin Biased Ligands for GPCRs

Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 4 of 7
George S. Ballie, University of Glasgow, UK
Targeting cAMP Degradation

Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 5 of 7
Jan Deussing, Max Planck Institute of Psychiatry, Germany
From Large Scale Mutagenesis Strategies to In-Depth Genetical Dissection
of CRHR1 Function in the Mouse


Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 6 of 7
Holly M. Dressler, Genzyme - Sanofi, USA
Short Talk: The CreLuc Reporter Mouse Model: A Transgenic Bioimaging Mouse Model that can Assay Ligand Activation of GPCRs

Thursday, April 08 | 8:00AM - 11:15AM
Ligand Efficacy and Compartmentalized Signaling
Room: Peaks 4-5

Speaker 7 of 7
Jonathan D. Violin, Trevena Inc., USA
Short Talk: A Beta-Arrestin Biased Ligand of the Angiotensin II Type 1 Receptor Stimulates Cardiac Performance and Reduces Blood Pressure

Thursday, April 08 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Thursday, April 08 | 11:15AM - 11:15AM
On Own for Lunch and Recreation


Thursday, April 08 | 11:15AM - 1:00PM
Poster Setup
Room: Peaks 1-3


Thursday, April 08 | 1:00PM - 10:00PM
Poster Viewing
Room: Peaks 1-3


Thursday, April 08 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Thursday, April 08 | 5:00PM - 7:00PM
GPCR Structure and Activation I
Room: Peaks 4-5

Speaker 1 of 5
* Heidi E. Hamm, USA

Thursday, April 08 | 5:00PM - 7:00PM
GPCR Structure and Activation I
Room: Peaks 4-5

Speaker 2 of 5
Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany
Real-Time Monitoring of GPCR Signaling in Living Cells

Thursday, April 08 | 5:00PM - 7:00PM
GPCR Structure and Activation I
Room: Peaks 4-5

Speaker 3 of 5
Jonathan A. Javitch, Columbia University, USA
Pick Your Partner Carefully: Communication between Protomers of GPCR Dimers Modulates Activation

Thursday, April 08 | 5:00PM - 7:00PM
GPCR Structure and Activation I
Room: Peaks 4-5

Speaker 4 of 5
Michael F. Brown, University of Arizona, USA
The Role of Lipids in GPCR Structure and Function

Thursday, April 08 | 5:00PM - 7:00PM
GPCR Structure and Activation I
Room: Peaks 4-5

Speaker 5 of 5
Martin Cottet, Institut de Génomique Fonctionnelle, France
Short Talk: Fluorescent Ligands and TR-FRET for the Labeling and Detection of GPCR Dimers in Native Tissues

Thursday, April 08 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Foyer/Peaks 1-3


Thursday, April 08 | 7:30PM - 10:00PM
Poster Session 1
Room: Peaks 1-3


Friday, April 09 | 7:00AM - 8:00AM
Breakfast
Room: Summit Gallery


Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 1 of 7
* Leonardo Pardo, Universitad Autonoma Barcelona, Spain

Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 2 of 7
Oliver P. Ernst, University of Toronto, Canada
Inactive and Active Conformations of Rhodopsin: Insights from Spectroscopic and Structural Studies


Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 3 of 7
H. Eric Xu, Van Andel Institute, USA
Ligand Recognition by Family B GPCRs

Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 4 of 7
Gebhard F. X. Schertler, Paul Scherrer Institut, Switzerland
Structure of a Constitutively Active Rhodopsin: Implications for Ligand Binding and Activation of GPCRs.

Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 5 of 7
Brian K. Kobilka, Stanford University School of Medicine, USA
Structural Insights into Ligand Efficacy

Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 6 of 7
Jesús Giraldo, Universitat Autònoma de Barcelona, Spain
Short Talk: Mathematical Modeling of Symmetrically/ Asymmetrically Activated GPCR Dimers Provides New Clues on Receptor Signaling

Friday, April 09 | 8:00AM - 11:15AM
GPCR Structure and Activation II
Room: Peaks 4-5

Speaker 7 of 7
Irina Kufareva, University of California, San Diego, USA
Short Talk: Rational Design of Point Mutations Improving GPCR Stability and Conformational Homogeneity

Friday, April 09 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Friday, April 09 | 11:15AM - 11:15AM
On Own for Lunch and Recreation


Friday, April 09 | 11:15AM - 1:00PM
Poster Setup
Room: Peaks 1-3


Friday, April 09 | 1:00PM - 10:00PM
Poster Viewing
Room: Peaks 1-3


Friday, April 09 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Friday, April 09 | 5:00PM - 7:00PM
Structure-Based Drug Discovery as Applied to Soluble Protein
s

Room: Peaks 4-5

Speaker 1 of 5
* Brian K. Shoichet, University of California, San Francisco, USA

Friday, April 09 | 5:00PM - 7:00PM
Structure-Based Drug Discovery as Applied to Soluble Protein
s

Room: Peaks 4-5

Speaker 2 of 5
Tom L. Blundell, University of Cambridge, UK
Structural Biology, Drug Discovery and Fragment-based Screening

Friday, April 09 | 5:00PM - 7:00PM
Structure-Based Drug Discovery as Applied to Soluble Protein
s

Room: Peaks 4-5

Speaker 3 of 5
Philip J. Hajduk, Abbott Laboratories, USA
Fragment-Based Approaches to Soluble and Membrane Proteins

Friday, April 09 | 5:00PM - 7:00PM
Structure-Based Drug Discovery as Applied to Soluble Protein
s

Room: Peaks 4-5

Speaker 4 of 5
Jonathan M. Moore, Vertex Pharmaceuticals Incorporated, USA
Crystal Structure of the Ectodomain Complex of the CGRP Receptor, a Class-B GPCR, Reveals the Site of Drug Antagonism

Friday, April 09 | 5:00PM - 7:00PM
Structure-Based Drug Discovery as Applied to Soluble Protein
s

Room: Peaks 4-5

Speaker 5 of 5
Liquan Yang, University of Rochester, USA
Short Talk: GPR56 Inhibits VEGF Secretion and Suppresses Melanoma Angiogenesis

Friday, April 09 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Foyer/Peaks 1-3


Friday, April 09 | 7:30PM - 10:00PM
Poster Session 2
Room: Peaks 1-3


Saturday, April 10 | 7:00AM - 8:00AM
Breakfast
Room: Summit Gallery


Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 1 of 8
* Jonathan A. Javitch, Columbia University, USA

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 2 of 8
Heidi E. Hamm, USA
New Insights into R*-G High Affinity Complex from Structural, Biophysical and Modeling Studies

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 3 of 8
Vsevolod V. Gurevich, Vanderbilt University, USA
Structural Basis of Arrestin Function: Redesigning a Marvel of Evolutionary Engineering

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 4 of 8
Gang Pei, TongJi University, China
Arrestin Signaling and Diseases

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 5 of 8
Jürgen Wess, National Institutes of Health, USA
Mapping the Receptor-G Protein Interface: Cross-Linking Analysis of a GPCR/G Protein Complex

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 6 of 8
Kristoffer Sahlholm, Karolinska Institutet, Sweden
Short Talk: Agonist-Specific Voltage-Sensitivity at the Dopamine D2S Receptor; Effects of Binding Site Mutations

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 7 of 8
George Essien Umanah, University of Tennessee, USA
Short Talk: Residue-to-Residue Contacts between G alpha and its GPCR in the Ligand Bound and Unbound State

Saturday, April 10 | 8:00AM - 11:30AM
G Proteins, Arrestins and Other Signaling Molecules Activate
d by GPCRs

Room: Peaks 4-5

Speaker 8 of 8
Xavier Deupi, Universitat Autonoma de Barcelona. School of Medicine, Spain
Short Talk: Integration of GPCR Structure, Dynamics and Function

Saturday, April 10 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Saturday, April 10 | 11:00AM - 1:00PM
Poster Setup
Room: Peaks 1-3


Saturday, April 10 | 1:00PM - 10:00PM
Poster Viewing
Room: Peaks 1-3


Saturday, April 10 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Saturday, April 10 | 5:00PM - 7:00PM
GPCR Structure and Activation III
Room: Peaks 4-5

Speaker 1 of 5
* Gebhard F. X. Schertler, Paul Scherrer Institut, Switzerland

Saturday, April 10 | 5:00PM - 7:00PM
GPCR Structure and Activation III
Room: Peaks 4-5

Speaker 2 of 5
Steven O. Smith, Stony Brook University, USA
Structural Insights into the Mechanism of Light-Activation of the Visual Pigment Rhodopsin

Saturday, April 10 | 5:00PM - 7:00PM
GPCR Structure and Activation III
Room: Peaks 4-5

Speaker 3 of 5
Carsten Hoffmann, University of Jena, Germany
Receptor Activation Studied by Site Specific Fluorescence Labeling of GCPRs in Living Cells

Saturday, April 10 | 5:00PM - 7:00PM
GPCR Structure and Activation III
Room: Peaks 4-5

Speaker 4 of 5
Nigel J.M. Birdsall, National Institute for Medical Research, UK
Single Molecule Imaging of GPCR Monomers and Dimers in Living Cells

Saturday, April 10 | 5:00PM - 7:00PM
GPCR Structure and Activation III
Room: Peaks 4-5

Speaker 5 of 5
Michael J. Overduin, University of Alberta, Canada
Short Talk: Amphipathic Polymer-based Nanoparticles for Purifying and Characterizing Stable and Active GPCRs without Detergents

Saturday, April 10 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Peaks 1-3


Saturday, April 10 | 7:30PM - 10:00PM
Poster Session 3
Room: Peaks 1-3


Sunday, April 11 | 7:00AM - 8:00AM
Breakfast
Room: Summit Gallery


Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 1 of 7
* Brian K. Kobilka, Stanford University School of Medicine, USA

Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 2 of 7
Leonardo Pardo, Universitad Autonoma Barcelona, Spain
Deciphering Mechanisms of G Protein-Coupled Receptor Activation

Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 3 of 7
Thue W. Schwartz, University of Copenhagen, Denmark
From Ligands to Efficiancy in 7 TM Receptors

Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 4 of 7
Brian K. Shoichet, University of California, San Francisco, USA
Exploiting GPCR Structures for Ligand Discovery

Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 5 of 7
Robert D. Harvey, University of Nevada, Reno, USA
Compartmentation of cAMP Signaling in Cardiac Myocytes: A Computational Study

Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 6 of 7
Marta Filizola, Icahn School of Medicine at Mount Sinai, USA
Short Talk: Exploring G Protein-Coupled Receptor Processes at the Molecular Level Using Enhanced Molecular Dynamics Methods

Sunday, April 11 | 8:00AM - 11:15AM
Computational Approaches to GPCR Structure and Signaling
Room: Peaks 4-5

Speaker 7 of 7
Vsevolod Katritch, University of Southern California, USA
Short Talk: Ligand-Guided Receptor Optimization for GPCR Drug Discovery

Sunday, April 11 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Sunday, April 11 | 11:15AM - 11:15AM
On Own for Lunch and Recreation


Sunday, April 11 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Sunday, April 11 | 5:00PM - 7:00PM
New Topics in GPCR Drug Development
Room: Peaks 4-5

Speaker 1 of 6
* Thue W. Schwartz, University of Copenhagen, Denmark

Sunday, April 11 | 5:00PM - 7:00PM
New Topics in GPCR Drug Development
Room: Peaks 4-5

Speaker 2 of 6
Annette G. Beck-Sickinger, Leipzig University, Germany
Peptides as GPCR Drugs in Therapy and Diagnosis

Sunday, April 11 | 5:00PM - 7:00PM
New Topics in GPCR Drug Development
Room: Peaks 4-5

Speaker 3 of 6
Thomas Klabunde, Sanofi-Aventis Pharma Deutschland GmbH, Germany
Chemogenomics-Approaches to GPCR Lead Finding –Sequence-Derived 3D-Pharmacophore Models

Sunday, April 11 | 5:00PM - 7:00PM
New Topics in GPCR Drug Development
Room: Peaks 4-5

Speaker 4 of 6
Lakshmi A. Devi, Mount Sinai School of Medicine, USA
G Protien Coupled Receptor Hetero Dimerization in Drug Discovery

Sunday, April 11 | 5:00PM - 7:00PM
New Topics in GPCR Drug Development
Room: Peaks 4-5

Speaker 5 of 6
Wayne Stallaert, Max Planck Institute for Molecular Physiology, Germany
Short Talk: Monitoring the Multiple Signaling Pathways of beta-Adrenergic Receptors Using a Label-Free Impedance-Based Detection Method

Sunday, April 11 | 5:00PM - 7:00PM
New Topics in GPCR Drug Development
Room: Peaks 4-5

Speaker 6 of 6
Kenneth E. Carlson, Ironwood Pharmaceuticals, USA
Short Talk: Identification of a Pepducin Agonist of the CXCR4 Receptor

Sunday, April 11 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Breckenridge Ballroom


Sunday, April 11 | 8:00PM - 11:00PM
Entertainment
Room: Breckenridge Ballroom


Sunday, April 11 | 8:00PM - 11:00PM
Cash Bar
Room: Breckenridge Ballroom


Monday, April 12 | 10:22AM - 10:22AM
Departure


*Session Chair
†Invited, not yet responded.