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G Protein-Coupled Receptors: New Insights in Functional Regulation and Clinical Application (E2)

Organizer(s): Heidi E. Hamm, P. Jeffrey Conn, Jean-Philippe Pin and Olivier Civelli
May 18 - 23, 2008
INEC-Ireland's National Events & Conference Centre  ·  Killarney, Co. Kerry, Ireland
Abstract Deadline: January 18, 2008
Late Abstract Deadline: February 19, 2008
Scholarship Deadline: January 18, 2008
Early Registration Deadline: March 31, 2008


In collaboration with Science Foundation Ireland; Part of the Translational Medicine Series, Sponsored by Pfizer Global Research & Development



This meeting took place in the 2008 season.

For a complete list of the meetings for the upcoming/current season,
see our meeting list, or search for a meeting.
Summary of Meeting
The G-protein-coupled-receptor (GPCR) family accounts for almost 3% of the human genome and encompasses the largest number of receptors identified to date. Further, GPCRs have proven to be one of the primary targets for therapeutic drug intervention. Work in the field is rapidly progressing through the identification of structural aspects of activation, dimerization and its functional significance, ligand-directed signaling, de-orphanization of GPCRs and their signaling pathways, allosteric modulators of GPCR activation, as well as novel interacting protein complexes and their correlate signaling cascades. This Keystone Symposia meeting will focus on these important aspects of GPCRs as well as how they regulate functional systems such as sleep, stress and feeding. Finally, the effect of genetic disease on GPCR activation and signaling will be discussed.

Sunday, May 18
3:00 - 7:30 PM Registration INEC Conference Centre Foyer
6:30 - 7:30 PM Refreshments INEC Conference Centre Foyer
7:30 - 8:30 PM Keynote Address INEC Main Auditorium
Brian K. Kobilka, Stanford University
Structure and Dynamics of the Human beta 2 Adrenergic Receptor
Monday, May 19
7:00 - 8:00 AM Breakfast INEC Conference Centre Foyer
8:00 - 11:15 AM GPCR Conformation INEC Main Auditorium
* Jean-Philippe Pin, Institute of Functional Genomics - CNRS/INSERM/Montpellier University 1&2
Krzysztof Palczewski, Case Western Reserve University
Structure of Rhodopsin
Gebhard F. X. Schertler, Paul Scherrer Institut
Structure of the Beta 1 Adrenergic Receptor: Progress in Obtaining Recombinant G Protein Coupled Receptor Structures
Martin Caffrey, University of Limerick
Membrane Protein Structure Determination Using Crystallography and Lipidic Mesophases
Jonathan A. Javitch, Columbia University
Dopamine D2 Receptors Form Higher Order Oligomers at Physiological Expression Levels
Jean-Louis Banères, Institut des Biomolécules Max Mousseron, UMR 5247 CNRS
Heterodimer Regulation of GPCR Activation
9:20 - 9:40 AM Coffee Break INEC Conference Centre Foyer
11:15 AM - 1:00 PM Poster Setup INEC Conference Centre Foyer
11:15 AM - On Own for Lunch
1:00 - 10:00 PM Poster Viewing INEC Conference Centre Foyer
4:30 - 5:00 PM Coffee Available INEC Conference Centre Foyer
5:00 - 7:15 PM Intracellular Signaling INEC Main Auditorium
* Jonathan A. Javitch, Columbia University
Xia Zhang, University of Ottawa
Role of PTEN and 5-HT2c Receptor Coupling in Drug Abuse
Lan Ma, Fudan University
Beta-Arrestin and Synaptic Plasticity
Joan Heller Brown, University of California, San Diego
GPCR Regulation of Cell Proliferation
Brigitte L. Kieffer, IGBMC
A New Approach to Study GPCR Trafficking in vivo
7:15 - 8:15 PM Social Hour w/ Lite Bites INEC Conference Centre Foyer
7:30 - 10:00 PM Poster Session 1 INEC Conference Centre Foyer
Tuesday, May 20
7:00 - 8:00 AM Breakfast INEC Conference Centre Foyer
8:00 - 11:00 AM Interacting Proteins INEC Main Auditorium
* Joan Heller Brown, University of California, San Diego
John J.G. Tesmer, University of Michigan
Structural Analysis of an Ancient Pathway Linking Gq-Coupled Receptors to RhoA
Emiliana Borrelli, University of California, Irvine
Specificity of Dopamine Mediated Signaling Differentially Directed by the Two D2 Receptor Isoforms
Taroh Iiri, University of Tokyo
Talk Title to be Determined
Zoe Jade Barclay, University of Edinburgh
Short Talk: Evidence for the Formation of a Functional Signaling Complex of the 5-HT2A Receptor with ARF1 and PLD1 and its Disruption in an H452Y Polymorphic Variant of the Receptor
Dominique Massotte, Institut de Génétique et de Biologie Moléculaire et Cellulaire
9:20 - 9:40 AM Coffee Break INEC Conference Centre Foyer
11:00 AM - 1:00 PM Poster Setup INEC Conference Centre Foyer
11:00 AM - On Own for Lunch
1:00 - 10:00 PM Poster Viewing INEC Conference Centre Foyer
4:30 - 5:00 PM Coffee Available INEC Conference Centre Foyer
5:00 - 7:00 PM Deorphanized GPCRs INEC Main Auditorium
* Olivier Civelli, University of California, Irvine
Frank Gannon, Science Foundation Ireland
Welcome Remarks
Stefan Offermanns, Universität Heidelberg
Nicotinic Acid Receptor - Pharmacological and Physiological Functions
Rainer K. Reinscheid, University of California, Irvine
Neuropeptide S Modulates Arousal and Stress Responses
Hans Bräuner-Osborne, University of Copenhagen, Faculty of Pharmaceutical Sciences
Basic Amino Acid Receptor GPRC6A Uncovered
Deborah Nguyen, Genomics Institute of the Novartis Research Foundation
Short Talk: Utilizing High-Throughput Profiling to Identify Modulators of Novel GPCRs
7:00 - 8:00 PM Social Hour w/ Lite Bites INEC Conference Centre Foyer
7:30 - 10:00 PM Poster Session 2 INEC Conference Centre Foyer
Wednesday, May 21
7:00 - 8:00 AM Breakfast INEC Conference Centre Foyer
7:00 - 8:00 AM Poster Setup INEC Conference Centre Foyer
8:00 - 11:15 AM GPCRs in Physiology 1 INEC Main Auditorium
* Stefan Offermanns, Universität Heidelberg
Kenji Kangawa, National Cardiovascular Center Research Institute
Ghrelin: Physiological Significance and Therapeutic Potential for Cardiovascular Diseases
Mark J. Zoller, Senomyx, Inc.
Using Sweet and Umami Taste Receptors to Discover Taste Enhancers
William Henry Colledge, University of Cambridge
GPR54 and Kisspeptins
Shuh Narumiya, Kyoto University
Physiology and Clinical Application of the Prostanoid Receptors
Garret A. FitzGerald, University of Pennsylvania
Prostaglandin Receptors in Cardiovascular Disease
9:20 - 9:40 AM Coffee Break INEC Conference Centre Foyer
11:15 AM - 12:00 PM Lunch INEC Conference Centre Foyer
12:00 - 2:30 PM Poster Session 3 INEC Conference Centre Foyer
2:30 - 4:30 PM Workshop: Can Industry and Academic Scientists Cooperate to Facilitate Drug Discovery? INEC Main Auditorium
* P. Jeffrey Conn, Vanderbilt University School of Medicine
A Model for Early Stage Drug Discovery in an Academic Setting
Roy G. Smith, Baylor College of Medicine
Growth Hormone Secretagogue Receptor
Gerard J. Marek, Abbott Laboratories
Academic-Industry Collaborations: An Industry Perspective
Hugh Rosen, The Scripps Research Institute
Chemical Probes not Drugs from Academia
Bruce A. Posner, Pfizer Inc.
The Pfizer-TSRI Collaboration: Partnering for Success in Early Lead Discovery
4:30 - 5:00 PM Coffee Available INEC Conference Centre Foyer
5:00 - 7:00 PM GPCRs in Physiology 2 INEC Main Auditorium
* Brigitte L. Kieffer, IGBMC
Wylie W. Vale, The Salk Institute
Corticotropin Releasing Factor Family of Ligands and their Receptors and Binding Protein
Gilbert Vassart, Université Libre de Bruxelles
Constitutive Activity of Wild Type GPCRs: Physiological and Evolutionary Significance
Masayasu Kojima, Kurume University
Phenotypic Analysis of Ghrelin Knockout Mouse
Jean-Pierre Vilardaga, Massachusetts General Hospital & Harvard Medical School
Short Talk: Conformational Cross-Talk between GPCR Heterodimers Controls Cell Signaling
7:00 PM - On Own for Dinner
Thursday, May 22
7:00 - 8:00 AM Breakfast INEC Conference Centre Foyer
8:00 - 11:00 AM GPCRs in Preclinical Drug Programs INEC Main Auditorium
* Heidi E. Hamm, Vanderbilt University School of Medicine
Hugh Rosen, The Scripps Research Institute
Under the Influence: S1P Receptor Therapeutics
Timothy W. Lovenberg, Johnson & Johnson Pharmaceutical Research and Development LLC
Relaxin 3 and Insulin 5 as Unique GPCR Agonists: Pharmacology and Preclinical Challenges
Andrew D. Howard, Merck Research Laboratories
GPCRs in Metabolism
Colleen Marie Niswender, Vanderbilt University
Allosteric Modulation of mGluR4 as a Novel Therapeutic Direction for the Treatment of Parkinson's Disease
Katsutoshi Sasaki, Kyowa Hakko Kirin Co., Ltd.
Short Talk: Reverse Chemical Genetics Approach Using a GPR4 Antagonist to Find a Novel Drug Candidate for Respiratory Diseases
9:20 - 9:40 AM Coffee Break INEC Conference Centre Foyer
11:00 AM - On Own for Lunch
4:30 - 5:00 PM Coffee Available INEC Conference Centre Foyer
5:00 - 7:00 PM Novel GPCR Drugs in the Clinic INEC Main Auditorium
Vincent Mutel, Addex Pharmaceuticals SA
Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Clinical Efficacy in Gastroesophageal Reflux Disease, Migraine and Acute Anticipatory Anxiety
* Gerard J. Marek, Abbott Laboratories
Use of mGluR Allosteric Modulators in Schizophrenia
Madhu Chintala, Schering Plough Research Institute
PAR1 Antagonist
Javier González-Maeso, Mount Sinai School of Medicine
Short Talk: Identification of a Serotonin/Glutamate Receptor Complex Implicated in Psychosis
7:00 - 8:00 PM Social Hour w/ Lite Bites INEC Conference Centre Foyer
8:00 - 11:00 PM Entertainment INEC Conference Centre Foyer
Friday, May 23
Departure
*Session Chair   †Speaker invited, not yet responded.



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