Saturday
2:00 pm - 5:00 pm
Arrival and Check-in
3:30 pm - 3:45 pm
Introductory Comments by GRC Site Staff / Welcome from the GRS Chair
3:45 pm - 4:30 pm
Structural Biology of GPCRs
This session will focus on the structure determination of GPCRs by X-ray crystallography and electron microscopy.
Discussion Leaders: Nicole Perry (Vanderbilt University, USA) and Zachary DeBruine (Van Andel Research Institute, USA)
3:45 pm - 3:50 pm
Opening Remarks
3:50 pm - 4:05 pm
Linda Johansson (University of Southern California, USA)
"XFEL Structures of the Human MT2 Melatonin Receptor Reveal Dual Ligand Entry Pathways"
4:05 pm - 4:10 pm
Discussion
4:10 pm - 4:25 pm
Daniel Hilger (Stanford University, USA)
"Structural Basis of GCGR Activation"
4:25 pm - 4:30 pm
Discussion
4:30 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
GPCR Functional Studies
This session will explore the biochemical, and biophysical mechanisms of GPCR activation and regulation, and will also emphasize novel approaches for studying these mechanisms.
Discussion Leaders: Franziska Heydenreich (Stanford University, USA) and Daniel Hilger (Stanford University, USA)
7:30 pm - 7:35 pm
Introduction by Discussion Leader
7:35 pm - 7:50 pm
Lachlan Clydesdale (Monash University, Australia)
"Assessing Biased Ligand Interactions Within the Transmembrane Domain Binding Site of the Glucagon-Like Peptide 1 Receptor"
7:50 pm - 7:55 pm
Discussion
7:55 pm - 8:10 pm
Dennis Fernandes (University of Toronto Mississauga, Canada)
"Conformational States and Switching Dynamics in the A2A Adenosine Receptor Revealed by Single-Molecule Fluorescence"
8:10 pm - 8:15 pm
Discussion
8:15 pm - 8:30 pm
Tony Ngo (University of California, San Diego, USA)
"Experiment-Guided Molecular Modeling Reveals the Geometry of a Complete CXC Receptor-Chemokine Complex"
8:30 pm - 8:35 pm
Discussion
8:35 pm - 8:50 pm
Manbir Sandhu (Beckman Research Institute, City of Hope, USA)
"Functional Evolution of Barcodes for G-Protein Selectivity Emerges from Sequence, Structure and Dynamics"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:10 pm
Nicole Perry (Vanderbilt University, USA)
"Arrestin-3 Scaffolding of the JNK3 Cascade Suggests a Mechanism for Signal Amplification"
9:10 pm - 9:15 pm
Discussion
9:15 pm - 9:30 pm
General Discussion
Sunday
7:30 am - 8:30 am
Breakfast
9:00 am - 11:00 am
GPCR Signaling and Pharmacology In Vitro and In Vivo
Discussion Leader: Jeffrey Liu (Max Planck Institute of Biochemistry, Germany)
9:00 am - 9:05 am
Introduction by Discussion Leader
9:05 am - 9:20 am
Elke Miess (Jena University Hospital / Friedrich Schiller University Jena, Germany)
"Multisite Phosphorylation Is Required for Sustained Interaction with GRKs and Arrestins During Rapid µ-Opioid Receptor Desensitization"
9:20 am - 9:25 am
Discussion
9:25 am - 9:40 am
Andrea Kliewer (Institute of Pharmacology and Toxicology, Jena University Hospital, Germany)
"Phosphorylation-Deficient G-Protein-Biased μ-Opioid Receptors Improve Analgesia and Diminish Tolerance but Worsen Opioid Side Effects"
9:40 am - 9:45 am
Discussion
9:45 am - 10:00 am
Andreas Bock (Max Delbrück Center for Molecular Medicine in the Helmholtz Association, Germany)
"cAMP Nanodomains Dictate Localized PKA Activity"
10:00 am - 10:05 am
Discussion
10:05 am - 10:20 am
Michael Ippolito (Thomas Jefferson University, USA)
"Negative Allosteric Modulation of Arrestin Recruitment to the β2-Adrenergic Receptor"
10:20 am - 10:25 am
Discussion
10:25 am - 10:40 am
Hideaki Yano (National Institutes of Health, USA)
"Interactions of Synthetic Cannabinoids with the 5HT1A Receptor"
10:40 am - 10:45 am
Discussion
10:45 am - 11:00 am
General Discussion
11:00 am - 12:30 pm
Poster Session
Coffee will be served in the poster area from 11:00 am - 11:30 am
12:30 pm - 1:30 pm
Lunch
1:30 pm - 2:30 pm
GPCR Computational Biology
This session will highlight new work seeking to improve our computational toolbox, and showcase how these tools may be used to further our understanding of GPCR function and the design of better therapeutics.
Discussion Leader: Brian Bender (Vanderbilt University, USA)
1:30 pm - 1:35 pm
Introduction by Discussion Leader
1:35 pm - 1:50 pm
Maria Marti Solano (MRC Laboratory of Molecular Biology, United Kingdom)
"Alternative Splicing of GPCR Signalling Components as a Source of Tissue-Specific Receptor Pharmacology"
1:50 pm - 1:55 pm
Discussion
1:55 pm - 2:10 pm
Alexander Hauser (University of Copenhagen, Denmark)
"Novel Strategies to Elucidate Orphan Peptide-Receptor Signaling Systems"
2:10 pm - 2:15 pm
Discussion
2:15 pm - 2:25 pm
General Discussion
2:25 pm - 2:30 pm
Closing Remarks
2:30 pm - 3:00 pm
Evaluation Period
Fill in GRS Evaluation Forms
3:00 pm
Seminar Concludes