Web Desc
G Protein-Coupled Receptors: Structure, Signaling and Drug Discovery
Organizer(s): Arthur Christopoulos, Laura M. Bohn and Dominic P. Behan
Date: February 21 - 25, 2016
Location: Keystone Resort, Keystone, CO, USA
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.
Scholarship Deadline: October 21 2015
Discounted Abstract Deadline: October 21 2015
Abstract Deadline: November 19 2015
Discounted Registration Deadline: December 21 2015
Keystone Symposia thanks our Sponsor(s) for generously supporting this meeting:
Arena Pharmaceuticals, Inc.Merck & Co., Inc.Novo Nordisk A/S
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

Program

Sunday, February 21 | 4:00PM - 8:00PM
Arrival and Registration
Room: Keystone Lodge Lobby


Sunday, February 21 | 6:00PM - 8:00PM
Welcome Mixer
Room: Keystone Lodge-Bighorn Bar
No registration fees are used to fund alcohol served at this function.

Monday, February 22 | 7:00AM - 8:00AM
Breakfast
Room: Shavano/Torreys


Monday, February 22 | 8:00AM - 9:00AM
Welcome and Keynote Address
Room: Grays Peak

Speaker 1 of 2
* Arthur Christopoulos, Monash University, Australia

Monday, February 22 | 8:00AM - 9:00AM
Welcome and Keynote Address
Room: Grays Peak

Speaker 2 of 2
Brian K. Kobilka, Stanford University School of Medicine, USA
Structural Insights into G Protein-Coupled Receptor Signaling

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 1 of 7
* Brian K. Kobilka, Stanford University School of Medicine, USA

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 2 of 7
Laurence J. Miller, Mayo Clinic, USA
Allosteric Regulation of the Type 1 Cholecystokinin Receptor

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 3 of 7
Patrick M. Sexton, Monash University, Australia
Molecular Mechanisms Governing Signaling and Bias at Class B GPCRs

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 4 of 7
Tracy M. Handel, University of California, San Diego, USA
Structure and Implications of the Metastasis Promoting Chemokine Receptor, CXCR4, in Complex with Chemokine.

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 5 of 7
Martin J. Lohse, Max Delbrück Center for Molecular Medicine, Germany
Optical Monitoring of Receptor Signaling - From Molecules to Intact Organisms

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 6 of 7
Byron Carpenter, MRC Laboratory of Molecular Biology, UK
Short Talk: Crystal Structure of the Human Adenosine A2a Receptor Bound to an Engineered G Protein

Monday, February 22 | 9:00AM - 12:15PM
GPCR Structure-Function I
Room: Grays Peak

Speaker 7 of 7
Philippe Rondard, Institut de Génomique Fonctionnelle, France
Short Talk: Hippocampal mGlu2 Receptor Homodimers Tune Context Fear Consolidation as Revealed with Positive Allosteric Nanobodies

Monday, February 22 | 10:20AM - 10:40AM
Coffee Break
Room: Longs Peak Foyer


Monday, February 22 | 12:15PM - 1:00PM
Poster Setup
Room: Shavano/Torreys


Monday, February 22 | 12:15PM - 5:00PM
On Own for Lunch


Monday, February 22 | 1:00PM - 10:00PM
Poster Viewing
Room: Shavano/Torreys


Monday, February 22 | 4:30PM - 5:00PM
Coffee Available
Room: Longs Peak Foyer


Monday, February 22 | 5:00PM - 7:00PM
GPCR Structure-Function II
Room: Grays Peak

Speaker 1 of 5
* Laurence J. Miller, Mayo Clinic, USA

Monday, February 22 | 5:00PM - 7:00PM
GPCR Structure-Function II
Room: Grays Peak

Speaker 2 of 5
Graeme Milligan, University of Glasgow, UK
Exploring Novel Roles for Free Fatty Acid Receptor 4 (GPR120)

Monday, February 22 | 5:00PM - 7:00PM
GPCR Structure-Function II
Room: Grays Peak

Speaker 3 of 5
Michel Bouvier, University of Montreal, Canada
Novel Approaches to Interrogating GPCR Signaling

Monday, February 22 | 5:00PM - 7:00PM
GPCR Structure-Function II
Room: Grays Peak

Speaker 4 of 5
Arthur Christopoulos, Monash University, Australia
Insights into Allosteric Modulation of GPCRs

Monday, February 22 | 5:00PM - 7:00PM
GPCR Structure-Function II
Room: Grays Peak

Speaker 5 of 5
Alexey Bondar, Institute of Nanobiology and Structural Biology, Czech Republic
Short Talk: Precoupling of G Proteins with GPCRs Visualized by Two-Photon Polarization Microscopy

Monday, February 22 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Shavano/Torreys
No registration fees are used to fund alcohol served at this function.

Monday, February 22 | 7:30PM - 10:00PM
Poster Session 1
Room: Shavano/Torreys


Tuesday, February 23 | 7:00AM - 8:00AM
Breakfast
Room: Shavano/Torreys


Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 1 of 7
* Laura M. Bohn, The Scripps Research Institute, USA

Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 2 of 7
Marc G. Caron, Duke University Medical Center, USA
Integrated Approaches to Understanding GPCRs in the CNS

Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 3 of 7
Bryan Roth, University of North Carolina at Chapel Hill, USA
Illuminating a Subterranean GPCR-ome

Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 4 of 7
Jeffrey Jeffrey Conn, Vanderbilt University, USA
Impact of Diverse Modes of Efficacy on Potential Therapeutic Effects of Allosteric Modulators of GPCRs

Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 5 of 7
Karen O'Malley, Washington University School of Medicine, USA
Intracellular Signaling of Metabotropic Glutamate Receptors

Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 6 of 7
Christopher Wild, University of Texas Medical Branch, USA
Short Talk: Serotonin (5-HT) 5-HT2C Receptor (5-HT2CR) Allosteric Modulators as Novel Neurotherapeutics

Tuesday, February 23 | 8:00AM - 11:15AM
GPCRs and CNS Biology
Room: Grays Peak

Speaker 7 of 7
Neah Likhite, University at Buffalo, USA
Short Talk: The Protein Arginine Methyltransferase PRMT5 Promotes D2-like Dopamine Receptor Signaling

Tuesday, February 23 | 9:20AM - 9:40AM
Coffee Break
Room: Longs Peak Foyer


Tuesday, February 23 | 11:15AM - 1:00PM
Poster Setup
Room: Shavano/Torreys


Tuesday, February 23 | 11:15AM - 5:00PM
On Own for Lunch


Tuesday, February 23 | 1:00PM - 10:00PM
Poster Viewing
Room: Shavano/Torreys


Tuesday, February 23 | 4:30PM - 5:00PM
Coffee Available
Room: Longs Peak Foyer


Tuesday, February 23 | 5:00PM - 7:00PM
Computational Studies of GPCRs
Room: Grays Peak

Speaker 1 of 5
* Patrick M. Sexton, Monash University, Australia

Tuesday, February 23 | 5:00PM - 7:00PM
Computational Studies of GPCRs
Room: Grays Peak

Speaker 2 of 5
Chris de Graaf, VU University Amsterdam, Netherlands
Computational Medicinal Chemistry Approaches to GPCR Drug Discovery

Tuesday, February 23 | 5:00PM - 7:00PM
Computational Studies of GPCRs
Room: Grays Peak

Speaker 3 of 5
Brian K. Shoichet, University of California, San Francisco, USA
Structure-Based and Network Pharmacology for GPCR Ligand Discovery

Tuesday, February 23 | 5:00PM - 7:00PM
Computational Studies of GPCRs
Room: Grays Peak

Speaker 4 of 5
Marta Filizola, Icahn School of Medicine at Mount Sinai, USA
Atomistic Level Approach to Allosteric Modulation and Biased Agonism to Develop
Non-Addictive Painkillers


Tuesday, February 23 | 5:00PM - 7:00PM
Computational Studies of GPCRs
Room: Grays Peak

Speaker 5 of 5
Nagarajan Vaidehi, City of Hope National Medical Center, USA
Short Talk: Dynamics of Thermostable Mutant Receptors in Detergent Micelles

Tuesday, February 23 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Shavano/Torreys
No registration fees are used to fund alcohol served at this function.

Tuesday, February 23 | 7:30PM - 10:00PM
Poster Session 2
Room: Shavano/Torreys


Wednesday, February 24 | 7:00AM - 8:00AM
Breakfast
Room: Shavano/Torreys


Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 1 of 7
* Michel Bouvier, University of Montreal, Canada

Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 2 of 7
Melanie H. Cobb, University of Texas Southwestern Medical Center, USA
Nutrient-Sensing GPCRs in Pancreatic Beta Cells

Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 3 of 7
Dominic P. Behan, Sentia Medical Sciences, Inc., USA
GPCR Modulation of Persistent Signaling and Energy Homeostasis with Specific Reference to Serotonin Receptors and Lorcaserin HCL’s Selectivity

Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 4 of 7
Lora K. Heisler, Rowett Institute, University of Aberdeen, UK
GPCRs in Obesity and Type 2 Diabetes

Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 5 of 7
Maree Smith, University of Queensland, Australia
Selective Small Molecule Angiotensin II Type 2 (AT2) for Neuropathic Pain

Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 6 of 7
Rui Chang, Harvard Medical School, USA
Short Talk: GPCR-Based Genetic Identification of Two Sensory Neuron Types that Differentially Control Breathing

Wednesday, February 24 | 8:00AM - 11:15AM
GPCRs in Physiology and Disease
Room: Grays Peak

Speaker 7 of 7
Derek Bone, NIDDK, National Institutes of Health, USA
Short Talk: Skeletal Muscle Gq-DREADD Signaling Greatly Enhances Glucose Tolerance and Insulin Sensitivity in Mice

Wednesday, February 24 | 9:20AM - 9:40AM
Coffee Break
Room: Longs Peak Foyer


Wednesday, February 24 | 11:15AM - 1:00PM
Poster Setup
Room: Shavano/Torreys


Wednesday, February 24 | 11:15AM - 5:00PM
On Own for Lunch


Wednesday, February 24 | 1:00PM - 10:00PM
Poster Viewing
Room: Shavano/Torreys


Wednesday, February 24 | 4:30PM - 5:00PM
Coffee Available
Room: Longs Peak Foyer


Wednesday, February 24 | 5:00PM - 7:00PM
GPCR Signaling and Bias
Room: Grays Peak

Speaker 1 of 5
* Dominic P. Behan, Sentia Medical Sciences, Inc., USA

Wednesday, February 24 | 5:00PM - 7:00PM
GPCR Signaling and Bias
Room: Grays Peak

Speaker 2 of 5
Martine J. Smit, VU University Amsterdam, Netherlands
Nanobodies Targeting Oncogenic GPCRs

Wednesday, February 24 | 5:00PM - 7:00PM
GPCR Signaling and Bias
Room: Grays Peak

Speaker 3 of 5
Louis M. Luttrell, Medical University of South Carolina, USA
Impact of Ligand Bias on GPCR Signaling Networks

Wednesday, February 24 | 5:00PM - 7:00PM
GPCR Signaling and Bias
Room: Grays Peak

Speaker 4 of 5
Laura M. Bohn, The Scripps Research Institute, USA
Biasing Opioid Receptor Signaling Away from Negative Side Effects

Wednesday, February 24 | 5:00PM - 7:00PM
GPCR Signaling and Bias
Room: Grays Peak

Speaker 5 of 5
Patricia H. McDonald, The Scripps Research Institute, USA
Short Talk: Development and Characterization of a Long-acting GLP-1R G-protein Biased Agonist

Wednesday, February 24 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Shavano/Torreys
No registration fees are used to fund alcohol served at this function.

Wednesday, February 24 | 7:30PM - 10:00PM
Poster Session 3
Room: Shavano/Torreys


Thursday, February 25 | 7:00AM - 8:00AM
Breakfast
Room: Shavano/Torreys


Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 1 of 7
* Bryan Roth, University of North Carolina at Chapel Hill, USA

Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 2 of 7
Christopher Langmead, Monash University, Australia
Challenges and Opportunities for CNS Drug Discovery

Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 3 of 7
Dimitri E. Grigoriadis, Neurocrine Biosciences, Inc., USA
Targeting CRF and GnRH Receptors in Central Nervous System and Endocrine Disorders

Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 4 of 7
Fiona H. Marshall, Heptares Therapeutics Ltd., UK
Structure-Based Design Applied to Allosteric Modulators of GPCRs

Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 5 of 7
Alexandros Makriyannis, Northeastern University, USA
The Endocannabinoid System as a Therapeutic Target

Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 6 of 7
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

Thursday, February 25 | 8:00AM - 11:15AM
GPCR Drug Discovery
Room: Grays Peak

Speaker 7 of 7
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

Thursday, February 25 | 9:20AM - 9:40AM
Coffee Break
Room: Longs Peak Foyer


Thursday, February 25 | 11:15AM - 5:00PM
On Own for Lunch


Thursday, February 25 | 4:30PM - 5:00PM
Coffee Available
Room: Longs Peak Foyer


Thursday, February 25 | 5:00PM - 6:45PM
Recent Developments in GPCR Discovery
Room: Grays Peak

Speaker 1 of 3
* Graeme Milligan, University of Glasgow, UK

Thursday, February 25 | 5:00PM - 6:45PM
Recent Developments in GPCR Discovery
Room: Grays Peak

Speaker 2 of 3
Andrew B. Tobin, University of Glasgow, UK
Genetic and Chemo-Genetic Approaches to Determine the Modes of Action of G Protein Coupled-Receptors and their Ligands

Thursday, February 25 | 5:00PM - 6:45PM
Recent Developments in GPCR Discovery
Room: Grays Peak

Speaker 3 of 3
Ron O. Dror, Stanford University, USA
Structural Basis for Nucleotide Exchange in Heterotrimeric G Proteins

Thursday, February 25 | 6:45PM - 7:00PM
Meeting Wrap-Up: Outcomes and Future Directions (Organizers)
Room: Grays Peak


Thursday, February 25 | 7:00PM - 8:00PM
Social Hour with Lite Bites
Room: Shavano/Torreys
No registration fees are used to fund alcohol served at this function.

Thursday, February 25 | 8:00PM - 11:00PM
Entertainment
Room: Shavano/Torreys
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.

Thursday, February 25 | 8:00PM - 11:00PM
Cash Bar
Room: Shavano/Torreys


Friday, February 26 | 10:25AM - 10:25AM
Departure


*Session Chair.