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This meeting took place in 2016



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G Protein-Coupled Receptors: Structure, Signaling and Drug Discovery (B3)


Organizer(s) Arthur Christopoulos, Laura M. Bohn and Dominic P. Behan
February 21—25, 2016
Keystone Resort • Keystone, Colorado USA
Discounted Abstract Deadline: Oct 21, 2015
Abstract Deadline: Nov 19, 2015
Scholarship Deadline: Oct 21, 2015
Discounted Registration Deadline: Dec 21, 2015

Sponsored by Arena Pharmaceuticals, Inc., Merck & Co., Inc. and Novo Nordisk A/S

Summary of Meeting:
The field of G protein-coupled receptors has recently seen major advances in high-resolution structure determination, as well as the validation of novel paradigms of drug action, such as allosteric modulation and biased agonism, as likely universal mechanisms. These studies are opening new insights into the diversity of this receptor superfamily, teaching us new lessons in receptor functionality and hinting at novel avenues to investigate. At the same time, we are seeing exciting discoveries in GPCR intracellular signaling and physiology. The timing is right to bring together researchers in these different areas. This Keystone Symposia meeting will focus on the interplay between these discoveries and how they are being used to advance GPCR-based research toward improved clinical outcomes.

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No registration fees are used to fund entertainment or alcohol at this conference

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


The meeting will begin on Sunday, February 21 with registration from 16:00 to 20:00 and a welcome mixer from 18:00 to 20:00. Conference events conclude on Thursday, February 25 with a closing plenary session from 17:00 to 19:00, followed by a social hour and entertainment. We recommend return travel on Friday, February 26 in order to fully experience the meeting.

SUNDAY, FEBRUARY 21

16:00—20:00
Arrival and Registration

Keystone Lodge Lobby
18:00—20:00
Welcome Mixer
No registration fees are used to fund alcohol served at this function.

Keystone Lodge-Bighorn Bar

MONDAY, FEBRUARY 22

07:00—08:00
Breakfast

Shavano/Torreys
08:00—09:00
Welcome and Keynote Address
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Arthur Christopoulos, Monash University, Australia

Brian K. Kobilka, Stanford University School of Medicine, USA
Structural Insights into G Protein-Coupled Receptor Signaling

09:00—12:15
GPCR Structure-Function I
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Brian K. Kobilka, Stanford University School of Medicine, USA

Laurence J. Miller, Mayo Clinic, USA
Allosteric Regulation of the Type 1 Cholecystokinin Receptor

Patrick M. Sexton, Monash University, Australia
Molecular Mechanisms Governing Signaling and Bias at Class B GPCRs

Tracy M. Handel, University of California, San Diego, USA
Structure and Implications of the Metastasis Promoting Chemokine Receptor, CXCR4, in Complex with Chemokine.

Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany
Optical Monitoring of Receptor Signaling - From Molecules to Intact Organisms

Byron Carpenter, MRC Laboratory of Molecular Biology, UK
Short Talk: Crystal Structure of the Human Adenosine A2a Receptor Bound to an Engineered G Protein

Philippe Rondard, Institut de Génomique Fonctionnelle, France
Short Talk: Hippocampal mGlu2 Receptor Homodimers Tune Context Fear Consolidation as Revealed with Positive Allosteric Nanobodies

10:20—10:40
Coffee Break

Longs Peak Foyer
12:15—13:00
Poster Setup

Shavano/Torreys
13:00—22:00
Poster Viewing

Shavano/Torreys
12:15—17:00
On Own for Lunch

16:30—17:00
Coffee Available

Longs Peak Foyer
17:00—19:00
GPCR Structure-Function II
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Laurence J. Miller, Mayo Clinic, USA

Graeme Milligan, University of Glasgow, UK
Exploring Novel Roles for Free Fatty Acid Receptor 4 (GPR120)

Michel Bouvier, University of Montreal, Canada
Novel Approaches to Interrogating GPCR Signaling

Arthur Christopoulos, Monash University, Australia
Insights into Allosteric Modulation of GPCRs

Alexey Bondar, Institute of Nanobiology and Structural Biology, Czech Republic
Short Talk: Precoupling of G Proteins with GPCRs Visualized by Two-Photon Polarization Microscopy

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Shavano/Torreys
19:30—22:00
Poster Session 1

Shavano/Torreys

TUESDAY, FEBRUARY 23

07:00—08:00
Breakfast

Shavano/Torreys
08:00—11:15
GPCRs and CNS Biology
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Laura M. Bohn, The Scripps Research Institute, USA

Marc G. Caron, Duke University Medical Center, USA
Integrated Approaches to Understanding GPCRs in the CNS

Bryan Roth, University of North Carolina, Chapel Hill, USA
Illuminating a Subterranean GPCR-ome

P. Jeffrey Conn, Vanderbilt University School of Medicine, USA
Impact of Diverse Modes of Efficacy on Potential Therapeutic Effects of Allosteric Modulators of GPCRs

Karen O'Malley, Washington University School of Medicine, USA
Intracellular Signaling of Metabotropic Glutamate Receptors

Christopher Wild, University of Texas Medical Branch, USA
Short Talk: Serotonin (5-HT) 5-HT2C Receptor (5-HT2CR) Allosteric Modulators as Novel Neurotherapeutics

Neah Likhite, University at Buffalo, USA
Short Talk: The Protein Arginine Methyltransferase PRMT5 Promotes D2-like Dopamine Receptor Signaling

09:20—09:40
Coffee Break

Longs Peak Foyer
11:15—13:00
Poster Setup

Shavano/Torreys
13:00—22:00
Poster Viewing

Shavano/Torreys
11:15—17:00
On Own for Lunch

16:30—17:00
Coffee Available

Longs Peak Foyer
17:00—19:00
Computational Studies of GPCRs
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Patrick M. Sexton, Monash University, Australia

Chris de Graaf, VU University Amsterdam, Netherlands
Computational Medicinal Chemistry Approaches to GPCR Drug Discovery

Brian K. Shoichet, University of California, San Francisco, USA
Structure-Based and Network Pharmacology for GPCR Ligand Discovery

Marta Filizola, Icahn School of Medicine at Mount Sinai, USA
Atomistic Level Approach to Allosteric Modulation and Biased Agonism to Develop Non-Addictive Painkillers

Nagarajan Vaidehi, City of Hope National Medical Center, USA
Short Talk: Dynamics of Thermostable Mutant Receptors in Detergent Micelles

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Shavano/Torreys
19:30—22:00
Poster Session 2

Shavano/Torreys

WEDNESDAY, FEBRUARY 24

07:00—08:00
Breakfast

Shavano/Torreys
08:00—11:15
GPCRs in Physiology and Disease
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Michel Bouvier, University of Montreal, Canada

Melanie H. Cobb, University of Texas Southwestern Medical Center, USA
Nutrient-Sensing GPCRs in Pancreatic Beta Cells

Dominic P. Behan, Beacon Discovery, USA
GPCR Modulation of Persistent Signaling and Energy Homeostasis with Specific Reference to Serotonin Receptors and Lorcaserin HCL’s Selectivity

Lora K. Heisler, University of Aberdeen, UK
GPCRs in Obesity and Type 2 Diabetes

Maree Smith, University of Queensland, Australia
Selective Small Molecule Angiotensin II Type 2 (AT2) for Neuropathic Pain

Rui Chang, Harvard Medical School, USA
Short Talk: GPCR-Based Genetic Identification of Two Sensory Neuron Types that Differentially Control Breathing

Derek Bone, NIDDK, National Institutes of Health, USA
Short Talk: Skeletal Muscle Gq-DREADD Signaling Greatly Enhances Glucose Tolerance and Insulin Sensitivity in Mice

09:20—09:40
Coffee Break

Longs Peak Foyer
11:15—13:00
Poster Setup

Shavano/Torreys
13:00—22:00
Poster Viewing

Shavano/Torreys
11:15—17:00
On Own for Lunch

16:30—17:00
Coffee Available

Longs Peak Foyer
17:00—19:00
GPCR Signaling and Bias
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Dominic P. Behan, Beacon Discovery, USA

Martine J. Smit, VU University Amsterdam, Netherlands
Nanobodies Targeting Oncogenic GPCRs

Louis M. Luttrell, Medical University of South Carolina, USA
Impact of Ligand Bias on GPCR Signaling Networks

Laura M. Bohn, The Scripps Research Institute, USA
Biasing Opioid Receptor Signaling Away from Negative Side Effects

Patricia H. McDonald, The Scripps Research Institute, USA
Short Talk: Development and Characterization of a Long-acting GLP-1R G-protein Biased Agonist

19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Shavano/Torreys
19:30—22:00
Poster Session 3

Shavano/Torreys

THURSDAY, FEBRUARY 25

07:00—08:00
Breakfast

Shavano/Torreys
08:00—11:15
GPCR Drug Discovery
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Bryan Roth, University of North Carolina, Chapel Hill, USA

Christopher Langmead, Monash University, Australia
Challenges and Opportunities for CNS Drug Discovery

Dimitri E. Grigoriadis, Neurocrine Biosciences, Inc., USA
Targeting CRF and GnRH Receptors in Central Nervous System and Endocrine Disorders

Fiona H. Marshall, Heptares Therapeutics Ltd., UK
Structure-Based Design Applied to Allosteric Modulators of GPCRs

Alexandros Makriyannis, Northeastern University, USA
The Endocannabinoid System as a Therapeutic Target

Irina Kufareva, University of California, San Diego, USA
Short Talk: Using the Pocketome to Identify Binding Pocket Neighbours for Surrogate Ligand Screening at Orphan G Protein-Coupled Receptors

Asuka Inoue, Tohoku University, Japan
Short Talk: G Protein-Depleted HEK293 Cells and Beta-Arrestin-Depleted HEK293 Cells: A Toolbox for GPCR Signaling Researches and its Application to Understanding Landscapes of G Protein Coupling

09:20—09:40
Coffee Break

Longs Peak Foyer
11:15—17:00
On Own for Lunch

16:30—17:00
Coffee Available

Longs Peak Foyer
17:00—18:45
Recent Developments in GPCR Discovery
Meeting has ended...abstracts no longer viewable online.

Grays Peak
* Graeme Milligan, University of Glasgow, UK

Andrew B. Tobin, University of Leicester, UK
Genetic and Chemo-Genetic Approaches to Determine the Modes of Action of G Protein Coupled-Receptors and their Ligands

Ron O. Dror, Stanford University, USA
Structural Basis for Nucleotide Exchange in Heterotrimeric G Proteins

18:45—19:00
Meeting Wrap-Up: Outcomes and Future Directions (Organizers)

Grays Peak
19:00—20:00
Social Hour with Lite Bites
No registration fees are used to fund alcohol served at this function.

Shavano/Torreys
20:00—23:00
Entertainment
Entertainment is not subsidized by conference registration fees nor any U.S. federal government grants. Funding for this expense is provided by other revenue sources.

Shavano/Torreys

FRIDAY, FEBRUARY 26

 
Departure


*Session Chair †Invited, not yet responded.



Keystone Symposia thanks our Sponsors for generously supporting this meeting:

Arena Pharmaceuticals, Inc. Merck & Co., Inc.
Novo Nordisk A/S
 

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



Heptares Therapeutics Ltd


Neurocrine Biosciences, Inc.


We appreciate the organizations that provide Keystone Symposia with additional support, such as marketing and advertising:


Click here to view more of these organizations


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


Click here to view more of these organizations


If your organization is interested in joining these entities in support of Keystone Symposia, please contact: Sarah Lavicka, Assistant Director of Development, Email: sarahl@keystonesymposia.org,
Phone:+1 970-262-2690

Click here for more information on Industry Support and Recognition Opportunities.

If you are interested in becoming an advertising/marketing in-kind partner, please contact:
Yvonne Psaila, Director, Marketing and Communications, Email: yvonnep@keystonesymposia.org,
Phone:+1 970-262-2676