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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
Abstract Deadline: December 7, 2009
Late Abstract Deadline: January 5, 2010
Scholarship Deadline: December 7, 2009
Early Registration Deadline: February 5, 2010


Supported by The Directors' Fund



This meeting took place in the 2010 season.

Listed below are current meetings that are similar to this meeting in nature/content:

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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.

Wednesday, April 7
3:00 - 7:30 PM Registration Foyer
6:30 - 7:30 PM Refreshments Foyer
7:30 - 8:30 PM Keynote Address Peaks 4-5
* Brian K. Kobilka, Stanford University
Shaun R. Coughlin, University of California, San Francisco
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 Peaks 4-5
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 Peaks 4-5
* Heidi E. Hamm, Vanderbilt University School of Medicine
Martin J. Lohse, Universität Würzburg
Real-Time Monitoring of GPCR Signaling in Living Cells
Jonathan A. Javitch, Columbia University
Pick Your Partner Carefully: Communication between Protomers of GPCR Dimers Modulates Activation
Michael F. Brown, University of Arizona
The Role of Lipids in GPCR Structure and Function
Martin Cottet, Institut de Génomique Fonctionnelle
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 Foyer/Peaks 1-3
7:30 - 10:00 PM Poster Session 1 Peaks 1-3
Friday, April 9
7:00 - 8:00 AM Breakfast Summit Gallery
8:00 - 11:15 AM GPCR Structure and Activation II Peaks 4-5
* Leonardo Pardo, Universitad Autonoma Barcelona
Oliver P. Ernst, CharitéCenter, Universitätsmedizin Berlin
Inactive and Active Conformations of Rhodopsin: Insights from Spectroscopic and Structural Studies
H. Eric Xu, Van Andel Research Institute
Ligand Recognition by Family B GPCRs
Gebhard F. X. Schertler, Paul Scherrer Institut
Structure of a Constitutively Active Rhodopsin: Implications for Ligand Binding and Activation of GPCRs.
Brian K. Kobilka, Stanford University
Structural Insights into Ligand Efficacy
Jesús Giraldo, Universitat Autònoma de Barcelona
Short Talk: Mathematical Modeling of Symmetrically/ Asymmetrically Activated GPCR Dimers Provides New Clues on Receptor Signaling
Irina Kufareva, University of California, San Diego
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 Peaks 4-5
* Brian K. Shoichet, University of California, San Francisco
Tom L. Blundell, University of Cambridge
Structural Biology, Drug Discovery and Fragment-based Screening
Philip J. Hajduk, Abbott Laboratories
Fragment-Based Approaches to Soluble and Membrane Proteins
Jonathan M. Moore, Vertex Pharmaceuticals Incorporated
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
Short Talk: GPR56 Inhibits VEGF Secretion and Suppresses Melanoma Angiogenesis
7:00 - 8:00 PM Social Hour w/ Lite Bites Foyer/Peaks 1-3
7:30 - 10:00 PM Poster Session 2 Peaks 1-3
Saturday, April 10
7:00 - 8:00 AM Breakfast Summit Gallery
8:00 - 11:30 AM G Proteins, Arrestins and Other Signaling Molecules Activated by GPCRs Peaks 4-5
* Jonathan A. Javitch, Columbia University
Heidi E. Hamm, Vanderbilt University School of Medicine
New Insights into R*-G High Affinity Complex from Structural, Biophysical and Modeling Studies
Vsevolod V. Gurevich, Vanderbilt University
Structural Basis of Arrestin Function: Redesigning a Marvel of Evolutionary Engineering
Gang Pei, TongJi University
Arrestin Signaling and Diseases
Jürgen Wess, National Institutes of Health
Mapping the Receptor-G Protein Interface: Cross-Linking Analysis of a GPCR/G Protein Complex
Kristoffer Sahlholm, Karolinska Institutet
Short Talk: Agonist-Specific Voltage-Sensitivity at the Dopamine D2S Receptor; Effects of Binding Site Mutations
George Essien Umanah, University of Tennessee
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
Short Talk: Integration of GPCR Structure, Dynamics and Function
9:20 - 9:40 AM Coffee Break Foyer
11:00 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 III Peaks 4-5
* Gebhard F. X. Schertler, Paul Scherrer Institut
Steven O. Smith, Stony Brook University
Structural Insights into the Mechanism of Light-Activation of the Visual Pigment Rhodopsin
Carsten Hoffmann, University of Würzburg
Receptor Activation Studied by Site Specific Fluorescence Labeling of GCPRs in Living Cells
Nigel J.M. Birdsall, National Institute for Medical Research
Single Molecule Imaging of GPCR Monomers and Dimers in Living Cells
Michael J. Overduin, University of Birmingham
Short Talk: Amphipathic Polymer-based Nanoparticles for Purifying and Characterizing Stable and Active GPCRs without Detergents
7:00 - 8:00 PM Social Hour w/ Lite Bites Peaks 1-3
7:30 - 10:00 PM Poster Session 3 Peaks 1-3
Sunday, April 11
7:00 - 8:00 AM Breakfast Summit Gallery
8:00 - 11:15 AM Computational Approaches to GPCR Structure and Signaling Peaks 4-5
* Brian K. Kobilka, Stanford University
Leonardo Pardo, Universitad Autonoma Barcelona
Deciphering Mechanisms of G Protein-Coupled Receptor Activation
Thue W. Schwartz, University of Copenhagen
From Ligands to Efficiancy in 7 TM Receptors
Brian K. Shoichet, University of California, San Francisco
Exploiting GPCR Structures for Ligand Discovery
Robert D. Harvey, University of Nevada, Reno
Compartmentation of cAMP Signaling in Cardiac Myocytes: A Computational Study
Marta Filizola, Mount Sinai School of Medicine
Short Talk: Exploring G Protein-Coupled Receptor Processes at the Molecular Level Using Enhanced Molecular Dynamics Methods
Vsevolod Katritch, University of California San Diego
Short Talk: Ligand-Guided Receptor Optimization for GPCR Drug Discovery
9:20 - 9:40 AM Coffee Break Foyer
11:15 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 Peaks 4-5
* Thue W. Schwartz, University of Copenhagen
Annette G. Beck-Sickinger, Leipzig University
Peptides as GPCR Drugs in Therapy and Diagnosis
Thomas Klabunde, Sanofi-Aventis Pharma Deutschland GmbH
Chemogenomics-Approaches to GPCR Lead Finding –Sequence-Derived 3D-Pharmacophore Models
Lakshmi A. Devi, Mount Sinai School of Medicine
G Protien Coupled Receptor Hetero Dimerization in Drug Discovery
Wayne M. Stallaert, Université de Montréal
Short Talk: Monitoring the Multiple Signaling Pathways of beta-Adrenergic Receptors Using a Label-Free Impedance-Based Detection Method
Kenneth E. Carlson, Anchor Therapeutics
Short Talk: Identification of a Pepducin Agonist of the CXCR4 Receptor
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.



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