Keystone Symposia Conference | G Protein-Coupled Receptors

Meeting Program

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Wednesday, April 7
3:00 - 7:30 PM	Registration	Foyer
6:30 - 7:30 PM	Refreshments	Foyer
7:30 - 8:30 PM	Keynote Address Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	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
7:00 - 8:00 AM	Breakfast	Summit Gallery
8:00 - 11:15 AM	Ligand Efficacy and Compartmentalized Signaling Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Terry P. Kenakin, GlaxoSmithKline, USA Importance of Efficacy in GPCR Drug Discovery
	Robert J. Lefkowitz, Howard Hughes Medical Institute at Duke University Medical Center, USA Arrestin Signaling and Arrestin Biased Ligands for GPCRs
	Wolfgang Wurst, Helmholtz Zentrum München, Germany Various Mutagenesis Strategies used to Dissect CRHR1 Function in vivo
	George Ballie, University of Glasgow, UK Targeting cAMP Degradation
	Holly M. Dressler, Sanofi-Aventis Pharmaceuticals, USA Short Talk: The CreLuc Reporter Mouse Model: A Transgenic Bioimaging Mouse Model that can Assay Ligand Activation of GPCRs
	Jonathan D. Violin†, University of California, San Diego, USA Short Talk: Title to be Determined
9:20 - 9:40 AM	Coffee Break	Foyer
11:15 AM-	On Own for Lunch and Recreation
11:15 AM- 1:00 PM	Poster Setup	Peaks 1-3
1:00 - 10:00 PM	Poster Viewing	Peaks 1-3
4:30 - 5:00 PM	Coffee Available	Foyer
5:00 - 7:00 PM	GPCR Structure and Activation I Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Speaker to be Announced,
	Martin J. Lohse, Universität Würzburg, 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
	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
7:00 - 8:00 PM	Social Hour w/ Lite Bites	Summit Gallery
7:30 - 10:00 PM	Poster Session 1 Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 1-3
Friday, April 9
7:00 - 8:00 AM	Breakfast	Summit Gallery
8:00 - 11:15 AM	GPCR Structure and Activation II Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Oliver P. Ernst, Charité - Universitätsmedizin Berlin, Germany 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
	Michael F. Brown, University of Arizona, USA The Role of Lipids in GPCR Structure and Function
	Gebhard F. X. Schertler, Paul Scherrer Institut, Switzerland Structure of a Constitutively Active Rhodopsin: Implications for Ligand Binding and Activation of GPCRs.
	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
9:20 - 9:40 AM	Coffee Break	Foyer
11:15 AM-	On Own for Lunch and Recreation
11:15 AM- 1:00 PM	Poster Setup	Peaks 1-3
1:00 - 10:00 PM	Poster Viewing	Peaks 1-3
4:30 - 5:00 PM	Coffee Available	Foyer
5:00 - 7:00 PM	Structure-Based Drug Discovery as Applied to Soluble Proteins Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Jonathan M. Moore, Vertex Pharmaceuticals Incorporated, USA Talk Title to be Determined
	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
	Liquan Yang, University of Rochester, USA Short Talk: GPR56 Inhibits VEGF Secretion and Suppresses Melanoma Angiogenesis
7:00 - 8:00 PM	Social Hour w/ Lite Bites	Summit Gallery
7:30 - 10:00 PM	Poster Session 2 Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 1-3
Saturday, April 10
7:00 - 11:00 AM	Poster Setup	Peaks 1-3
7:00 - 8:00 AM	Breakfast	Summit Gallery
8:00 - 11:15 AM	G Proteins, Arrestins and Other Signaling Molecules Activated by GPCRs Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Heidi E. Hamm, Vanderbilt University School of Medicine, 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
	Jurgen 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
9:20 - 9:40 AM	Coffee Break	Foyer
11:30 AM- 12:30 PM	Lunch	Summit Gallery
12:30 - 2:30 PM	Poster Session 3 Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 1-3
4:30 - 5:00 PM	Coffee Available	Foyer
5:00 - 7:00 PM	GPCR Structure and Activation III Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	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 Investigating Ligand-Specific Conformational Changes of GPCRs 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. Overduin, University of Birmingham, UK Short Talk: Amphipathic Polymer-based Nanoparticles for Purifying and Characterizing Stable and Active GPCRs without Detergents
7:00 PM-	On Own for Dinner
Sunday, April 11
7:00 - 8:00 AM	Breakfast	Summit Gallery
8:00 - 11:15 AM	Computational Approaches to GPCR Structure and Signaling Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Leonardo Pardo, Universitad Autonoma Barcelona, Spain Deciphering Mechanisms of G Protein-Coupled Receptor Activation
	Thue W. Schwartz, University of Copenhagen, Denmark Evidence for a Concerted Action Allosteric Mechanism for GPCR Activation
	Brian K. Shoichet, University of California, San Francisco, USA Exploiting GPCR Structures for Ligand Discovery
	Robert Harvey, University of Nevada, Reno, USA Compartmentation of cAMP Signaling in Cardiac Myocytes: A Computational Study
	Marta Filizola, Mount Sinai School of Medicine, USA Short Talk: Exploring G Protein-Coupled Receptor Processes at the Molecular Level Using Enhanced Molecular Dynamics Methods
	Vsevolod Katritch, University of California San Diego, USA Short Talk: Ligand-Guided Receptor Optimization for GPCR Drug Discovery
9:20 - 9:40 AM	Coffee Break	Foyer
11:00 AM-	On Own for Lunch and Recreation
4:30 - 5:00 PM	Coffee Available	Foyer
5:00 - 7:00 PM	New Topics in GPCR Drug Development Registered attendees for this meeting can view Abstracts for this session starting on 03/07/2010	Peaks 4-5
	Annette G. Beck-Sickinger, University of Leipzig, 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 Impact of Heterodimerization of GPCRs in Drug Discovery
	Wayne M. Stallaert, Universite de Montreal, Institute for Research in Immunology and Cancer, Canada Short Talk: Monitoring the Multiple Signaling Pathways of â-Adrenergic Receptors Using a Label-Free Impedance-Based Detection Method
7:00 - 8:00 PM	Social Hour w/ Lite Bites	Breckenridge Ballroom
8:00 - 11:00 PM	Entertainment	Breckenridge Ballroom
Monday, April 12
	Departure
*=Session Chair †=Speaker invited, not yet responded.

We gratefully acknowledge support for this conference from:

	Bristol-Myers Squibb Company
Sanofi-Aventis Pharma Deutschland GmbH	Vertex Pharmaceuticals Incorporated

The 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 organizations that provide Keystone Symposia with additional support, such as marketing and advertising...

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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.

G Protein-Coupled Receptors (C3)