Beaver Run Resort Floorplan

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This meeting took place in 2010


Here are the related meetings in 2018:
GPCR Structure and Function: Taking GPCR Drug Development and Discovery to the Next Level (B8)

For a complete list of the meetings for the upcoming/current season, see our meeting list, or search for a meeting.

G Protein-Coupled Receptors (C3)


Organizer(s) Brian K. Kobilka, Martin J. Lohse and Thue W. Schwartz
April 7—12, 2010
Beaver Run Resort • Breckenridge, Colorado USA
Abstract Deadline: Dec 7, 2009
Late Abstract Deadline: Jan 5, 2010
Scholarship Deadline: Dec 7, 2009
Early Registration Deadline: Feb 5, 2010

Supported by The Directors' Fund

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.

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Conference Program    Print  |   View meeting in 12 hr (am/pm) time


WEDNESDAY, APRIL 7

15:00—19:30
Registration

Foyer
18:30—19:30
Refreshments

Foyer
19:30—20:30
Keynote Address
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Brian K. Kobilka, Stanford University School of Medicine, USA

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 8

07:00—08:00
Breakfast

Summit Gallery
08:00—11:15
Ligand Efficacy and Compartmentalized Signaling
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany

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

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

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

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

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

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

09:20—09:40
Coffee Break

Foyer
11:15
On Own for Lunch and Recreation

11:15—13:00
Poster Setup

Peaks 1-3
13:00—22:00
Poster Viewing

Peaks 1-3
16:30—17:00
Coffee Available

Foyer
17:00—19:00
GPCR Structure and Activation I
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Heidi E. Hamm, , USA

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

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

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

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

19:00—20:00
Social Hour with Lite Bites

Foyer/Peaks 1-3
19:30—22:00
Poster Session 1

Peaks 1-3

FRIDAY, APRIL 9

07:00—08:00
Breakfast

Summit Gallery
08:00—11:15
GPCR Structure and Activation II
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Leonardo Pardo, Universitad Autonoma Barcelona, Spain

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

H. Eric Xu, Van Andel Research Institute, USA
Ligand Recognition by Family B GPCRs

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

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

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

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

09:20—09:40
Coffee Break

Foyer
11:15
On Own for Lunch and Recreation

11:15—13:00
Poster Setup

Peaks 1-3
13:00—22:00
Poster Viewing

Peaks 1-3
16:30—17:00
Coffee Available

Foyer
17:00—19:00
Structure-Based Drug Discovery as Applied to Soluble Proteins
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Brian K. Shoichet, University of California, San Francisco, USA

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

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

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

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

19:00—20:00
Social Hour with Lite Bites

Foyer/Peaks 1-3
19:30—22:00
Poster Session 2

Peaks 1-3

SATURDAY, APRIL 10

07:00—08:00
Breakfast

Summit Gallery
08:00—11:30
G Proteins, Arrestins and Other Signaling Molecules Activated by GPCRs
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Jonathan A. Javitch, Columbia University, USA

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

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

Gang Pei, TongJi University, China
Arrestin Signaling and Diseases

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

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

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

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

09:20—09:40
Coffee Break

Foyer
11:00—13:00
Poster Setup

Peaks 1-3
13:00—22:00
Poster Viewing

Peaks 1-3
16:30—17:00
Coffee Available

Foyer
17:00—19:00
GPCR Structure and Activation III
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Gebhard F. X. Schertler, Paul Scherrer Institut, Switzerland

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

Carsten Hoffmann, University of Würzburg, Germany
Receptor Activation Studied by Site Specific Fluorescence Labeling of GCPRs in Living Cells

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

Michael J. Overdui, University of Birmingham, UK
Short Talk: Amphipathic Polymer-based Nanoparticles for Purifying and Characterizing Stable and Active GPCRs without Detergents

19:00—20:00
Social Hour with Lite Bites

Peaks 1-3
19:30—22:00
Poster Session 3

Peaks 1-3

SUNDAY, APRIL 11

07:00—08:00
Breakfast

Summit Gallery
08:00—11:15
Computational Approaches to GPCR Structure and Signaling
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Brian K. Kobilka, Stanford University School of Medicine, USA

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

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

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

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

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

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

09:20—09:40
Coffee Break

Foyer
11:15
On Own for Lunch and Recreation

16:30—17:00
Coffee Available

Foyer
17:00—19:00
New Topics in GPCR Drug Development
Meeting has ended...abstracts no longer viewable online.

Peaks 4-5
* Thue W. Schwartz, University of Copenhagen, Denmark

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

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

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

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

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

19:00—20:00
Social Hour with Lite Bites

Breckenridge Ballroom
20:00—23:00
Entertainment

Breckenridge Ballroom

MONDAY, APRIL 12

 
Departure


*Session Chair †Invited, not yet responded.



We gratefully acknowledge support for this conference from:


Directors' Fund


These generous unrestricted gifts allow our Directors to schedule meetings in a wide variety of important areas, many of which are in the early stages of research.

Click here to view all of the donors who support the Directors' Fund.



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


National Institutes of Health

Grant No. 1R13GM093551-01




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.

Bristol-Myers Squibb Company
 

We gratefully acknowledge additional in-kind support for this conference from those foregoing speaker expense reimbursements:



Sanofi-Aventis Pharma Deutschland GmbH


Vertex Pharmaceuticals Incorporated


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Special thanks to the following for their support of Keystone Symposia initiatives to increase participation at this meeting by scientists from underrepresented backgrounds:


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Phone:+1 970-262-2690

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