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Molecular Pharmacology
Gordon Research Conference

GPCRs: From Single Molecules to New Forms of Treatment

Dates

March 12-17, 2017

Location

Renaissance Tuscany Il Ciocco
Lucca (Barga), Italy

Organizers

Chairs:
Martin J. Lohse & Jurgen Wess

Vice Chairs:
Roger Sunahara & Laura M. Bohn

Meeting Description

The Gordon Research Conference (GRC) on Molecular Pharmacology will highlight the most recent advances in the area of G protein-coupled receptors (GPCRs), both at the molecular and translational (drug development) level. Topics will include new high-resolution structural investigations, single molecule studies, mechanisms involved in GPCR signaling, compartmentation, and activation, and studies of novel physiological and pathophysiological roles of specific GPCRs. Particular focus will be put on the identification of druggable targets for several important diseases, including various diseases of the CNS, diabetes, and obesity, and the use of emerging new technologies useful for drug development. Experts from neighboring fields will present new technologies and approaches not yet widely used in the GPCR field.

The program will include the following general areas: i) novel GPCR structures and potential clinical relevance, ii) single molecule studies, iii) GPCR signaling and compartmentation, iv) novel technologies for GPCR research and drug development, v) GPCR signaling in physiology and disease with primary emphasis on identifying new drug targets, and (vi) diversity of GPCR ligands and resulting clinical implications.

The GRC on Molecular Pharmacology is one of the key meetings in the GPCR field. The 2017 meeting will take place in the heart of Tuscany, Italy (near Pisa/Lucca). This meeting generally attracts an enthusiastic and diverse group of students, postdoctoral fellows and faculty at all stages to create a scientifically exciting and collegial atmosphere to advance novel ideas and concepts in the GPCR field. The meeting will also feature several informal interactive sessions to encourage interactions between junior and senior participants.

Related Meeting

This GRC was held in conjunction with the "Molecular Pharmacology" Gordon Research Seminar (GRS). Refer to the associated GRS program page for more information.

Contributors

Meeting Program

Sunday
4:00 pm - 8:00 pmArrival and Check-in
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmStructural Basis of GPCR Function
Discussion Leader: Roger Sunahara (University of California, San Diego, USA)
7:40 pm - 7:50 pmIntroduction by Discussion Leader
7:50 pm - 8:20 pmTracy Handel (University of California, San Diego, USA)
"Structure, Activation and Inhibition of Chemokine Receptors"
8:20 pm - 8:30 pmDiscussion
8:30 pm - 9:20 pmBrian Kobilka (Stanford University, USA)
"The Role of Protein Dynamics in GPCR Action"
9:20 pm - 9:30 pmDiscussion
Monday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmNovel GPCR Structures and Structure-Based Drug Design
Discussion Leader: Gebhard Schertler (Paul Scherrer Institute / ETH Zurich, Switzerland)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:35 amQing Fan (Columbia University Medical Center, USA)
"Structural Mechanisms of Ligand Activation in Class C GPCRs"
9:35 am - 9:45 amDiscussion
9:45 am - 10:10 amFiona Marshall (Heptares Therapeutics, United Kingdom)
"X-Ray Structures of GPCRs Provide Insights into New Binding Sites for Drug Discovery"
10:10 am - 10:20 amDiscussion
10:20 am - 10:55 amCoffee Break
10:55 am - 11:20 amPatrick Sexton (Monash University, Australia)
"A Structural Understanding of Class B GPCR Activation and G Protein Interaction"
11:20 am - 11:30 amDiscussion
11:30 am - 11:55 amBrian Shoichet (University of California, San Francisco, USA)
"Structure-Based Screens for New Chemotypes Conferring New GPCR Biology"
11:55 am - 12:05 pmDiscussion
12:05 pm - 12:20 pmCedric Leyrat (Institut de Génomique Fonctionnelle (IGF), France)
"Structure and Function of Adiponectin Receptors"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:30 pmFree Time
3:00 pm - 4:00 pmPower Hour
The GRC Power Hour is an optional informal gathering open to all meeting participants. It is designed to help address the challenges women face in science and support the professional growth of women in our communities by providing an open forum for discussion and mentoring.
Organizers: Martine Smit (Vrije Universiteit Amsterdam, The Netherlands) and Kathleen Caron (University of North Carolina at Chapel Hill, USA)
4:30 pm - 6:00 pmPoster Session
6:00 pm - 8:00 pmSingle Molecule Studies
Discussion Leader: Ralf Jockers (Institut Cochin, INSERM U1016, France)
6:00 pm - 6:10 pmIntroduction by Discussion Leader
6:10 pm - 6:35 pmRinshi Kasai (Kyoto University, Japan)
"Transient GPCR Dimers and Their Functions as Revealed by Single-Molecule Tracking"
6:35 pm - 6:45 pmDiscussion
6:45 pm - 7:10 pmBenjamin Kaupp (Center of Advanced European Studies and Research, Germany)
"Oligomeric Architecture of Membrane Receptors"
7:10 pm - 7:20 pmDiscussion
7:20 pm - 7:35 pmGeorgios Skiniotis (University of Michigan, USA)
"Breaking into GPCR Structural Space with CryoEM"
7:35 pm - 7:40 pmDiscussion
7:40 pm - 7:55 pmTitiwat Sungkaworn (University of Wuerzburg, Germany)
"Single-Molecule Analysis of Receptor:G Protein Interactions"
7:55 pm - 8:00 pmDiscussion
8:00 pmDinner
Tuesday
7:30 am - 8:30 amBreakfast
8:30 amGroup Photo
9:00 am - 12:30 pmNovel Tools and Technologies for GPCR Research
Discussion Leaders: JoAnn Trejo (University of California, San Diego, USA) and Michel Bouvier (Université de Montréal, Canada)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:35 amBryan Roth (University of North Carolina at Chapel Hill, USA)
"Towards a Molecular Understanding of Psychoactive Drug Actions at GPCRs"
9:35 am - 9:45 amDiscussion
9:45 am - 10:10 amAnne Andrews (University of California, Los Angeles, USA)
"5-HT1A Autoreceptor Control of Serotonin Signaling - Rethinking Modes of Inhibitory Feedback"
10:10 am - 10:20 amDiscussion
10:20 am - 10:55 amCoffee Break
10:55 am - 11:20 amMeritxell Canals (Monash University, Australia)
"GPCR Signaling Platforms for Pain and Analgesia"
11:20 am - 11:30 amDiscussion
11:30 am - 11:55 amKathleen Caron (University of North Carolina at Chapel Hill, USA)
"RAMPs and Atypical Chemokine Receptors"
11:55 am - 12:05 pmDiscussion
12:05 pm - 12:20 pmAmadeu Llebaria (MCS Institute of Advanced Chemistry of Catalonia, CSIC, Spain)
"Using Light and Photoregulated Allosteric Ligands for Precise Control of mGluRs Activity In Vivo"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:30 pmFree Time
4:30 pm - 6:00 pmPoster Session
6:00 pm - 8:00 pmGPCRs: Signal Compartmentation
Discussion Leader: Alan Smrcka (University of Michigan, USA)
6:00 pm - 6:10 pmIntroduction by Discussion Leader
6:10 pm - 6:35 pmJean-Pierre Vilardaga (University of Pittsburgh School of Medicine, USA)
"Endosomal and Mitochondrial GPCR Signaling: Mechanisms and Biological Significance"
6:35 pm - 6:45 pmDiscussion
6:45 pm - 7:10 pmManuela Zaccolo (University of Oxford, United Kingdom)
"cAMP: From Long-Range Messenger to Nano-Domain Signalling"
7:10 pm - 7:20 pmDiscussion
7:20 pm - 7:45 pmJin Zhang (University of California, San Diego, USA)
"Compartmentalized cAMP/PKA Signaling in Living Cells"
7:45 pm - 8:00 pmDiscussion
8:00 pmDinner
Wednesday
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmCentral GPCRs as Drug Targets
Discussion Leader: Marc Caron (Duke University Medical Center, USA)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:35 amKathryn Cunningham (University of Texas Medical Branch, USA)
"Allosteric Modulators of the Serotonin 5-HT2C Receptor"
9:35 am - 9:45 amDiscussion
9:45 am - 10:10 amGregory Scherrer (Stanford University, USA)
"Opioid Receptor Mechanisms Controlling Neurotransmission in Pain Pathways"
10:10 am - 10:20 amDiscussion
10:20 am - 10:55 amCoffee Break
10:55 am - 11:20 amMichael Bruchas (Washington University School of Medicine, USA)
"Optical Approaches for Dissecting GPCR Signalling in Neural Circuits"
11:20 am - 11:30 amDiscussion
11:30 am - 11:55 amJeffrey Witkin (Lilly Research Laboratories, USA)
"Potential Application of mGlu Modulators for Treatment of Neurological and Psychiatric Disorders"
11:55 am - 12:05 pmDiscussion
12:05 pm - 12:20 pmSophie Bradley (University of Glasgow, United Kingdom)
"M1-Muscarinic Allosteric Modulators Slow Prion Neurodegeneration and Restore Memory Loss"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:30 pmFree Time
4:30 pm - 6:00 pmPoster Session
6:00 pm - 8:00 pmDiversity of GPCR Ligands: Clinical Implications
Discussion Leader: Laura Bohn (Scripps Florida, USA)
6:00 pm - 6:10 pmIntroduction by Discussion Leader
6:10 pm - 6:35 pmArthur Christopoulos (Monash University, Australia)
"Structural and Translational Studies of GPCR Allostery"
6:35 pm - 6:45 pmDiscussion
6:45 pm - 7:10 pmJeff Conn (Vanderbilt University, USA)
"Allosteric Modulators of GPCRs for the Treatment of CNS Disorders"
7:10 pm - 7:20 pmDiscussion
7:20 pm - 7:35 pmTobias Langenhan (Leipzig University, Germany)
"Converting Force into Signal: Metabotropic Mechanosensing Through Adhesion GPCRs"
7:35 pm - 7:40 pmDiscussion
7:40 pm - 7:55 pmCharlotte Avet (Université de Montréal, Canada)
"Exploring the Role of PAR-2 Functional Selectivity for the Development of Anti-Inflammatory Drugs"
7:55 pm - 8:00 pmDiscussion
8:00 pmDinner
Thursday
7:30 am - 8:30 amBreakfast
8:30 am - 9:00 amBusiness Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
9:00 am - 12:30 pmGPCRs and Metabolism: Clinical Implications
Discussion Leader: Graeme Milligan (University of Glasgow, United Kingdom)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:35 amAlexander Pfeifer (University of Bonn, Germany)
"GPCRs in Brown Adipose Tissue"
9:35 am - 9:45 amDiscussion
9:45 am - 10:10 amStefan Offermanns (Max Planck Institute for Heart and Lung Research, Germany)
"Autocrine Regulation of Metabolic Functions Through Metabolite GPCRs"
10:10 am - 10:20 amDiscussion
10:20 am - 10:55 amCoffee Break
10:55 am - 11:20 amLora Heisler (University of Aberdeen, United Kingdom)
"5-HT2C Receptor: A Target for Obesity and Type 2 Diabetes Treatment"
11:20 am - 11:30 amDiscussion
11:30 am - 11:55 amMichael Krashes (National Institutes of Health, USA)
"Chemogenetic Control of Energy Balance"
11:55 am - 12:05 pmDiscussion
12:05 pm - 12:20 pmSofia Cabezudo (CBMSO, Universidad Autónoma de Madrid, Spain)
"Gq-Coupled GPCR Pathways Open New Avenues for the Modulation of Autophagy"
12:20 pm - 12:30 pmDiscussion
12:30 pmLunch
1:30 pm - 4:30 pmFree Time
4:30 pm - 6:00 pmPoster Session
6:00 pm - 8:00 pmGPCR Activation and Signaling
Discussion Leader: Paul Insel (University of California, San Diego, USA)
6:00 pm - 6:10 pmIntroduction by Discussion Leader
6:10 pm - 6:40 pmTorsten Schoeneberg (Leipzig University, Germany)
"What Are They Waiting For? - Signaling of GPCRs with Large Ectodomains"
6:40 pm - 6:50 pmDiscussion
6:50 pm - 7:40 pmRobert Lefkowitz (Howard Hughes Medical Institute / Duke University Medical Center, USA)
"G-Protein Coupled Receptors (GPCRs) and Arrestin Coupled Receptors (ACRs): A Tale of Two Transducers"
7:40 pm - 8:00 pmDiscussion
8:00 pmDinner
Friday
7:30 am - 8:30 amBreakfast
9:00 amDeparture
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