Sunday
4:00 pm - 8:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Keynote Session: Pharmacology of GPCR Function in Neurological Disorders
From genetic models to ligands beyond opioids.
Discussion Leader: Laura Bohn (The Scripps Research Institute - Florida, USA)
7:40 pm - 8:15 pm
Michel Bouvier (Université de Montréal, Canada)
"Structural and Spatiotemporal Basis of GPCR Pluridimensional Functional Selectivity"
8:15 pm - 8:25 pm
Discussion
8:25 pm - 8:45 pm
Amy Newman (National Institute on Drug Abuse Intramural Research Program, NIH, USA)
"Reducing Abuse and Aiding Analgesia: Targeting the Dopamine D3 Receptor to Address the Opioid Crisis"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:10 pm
Martine Smit (Vrije Universiteit Amsterdam, The Netherlands)
"Viral GPCRs Rewire Signaling and Accelerate Glioblastoma Growth"
9:10 pm - 9:15 pm
Discussion
9:15 pm - 9:25 pm
Selected from Poster Abstracts: Volodymyr Korkhov (Paul Scherrer Institute / ETH Zurich, Switzerland)
"Structure of a Membrane Adenylyl Cyclase Bound to a G Protein α-Subunit"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
The Importance of Subcellular Location to Drug Targeting and Signaling
Whether in real estate or in drug targeting, subcellular location is still critical to targeting and signaling.
Discussion Leader: Mark von Zastrow (University of California, San Francisco, USA)
9:00 am - 9:25 am
Terry Kenakin (University of North Carolina School of Medicine, USA)
"Novel Allosteric Modulators"
9:25 am - 9:30 am
Discussion
9:30 am - 9:55 am
JoAnn Trejo (University of California, San Diego, USA)
"Ubiquitin Drives GPCR Inflammatory Signaling"
9:55 am - 10:00 am
Discussion
10:00 am - 10:25 am
Jean-Pierre Vilardaga (University of Pittsburgh School of Medicine, USA)
"Disease-Associated Mutation in PTH Unveils Ca2+ Allostery and the Role of Gq in PTH-Receptor Signaling via cAMP"
10:25 am - 10:30 am
Discussion
10:30 am - 10:55 am
Coffee Break
10:55 am - 11:05 am
Roshanak Irannejad (University of California, San Francisco, USA)
"The Role of Spatial Signaling in GPCR Function"
11:05 am - 11:10 am
Discussion
11:10 am - 11:35 am
Martin Lohse (Max Delbrück Center for Molecular Medicine, Germany)
"Compartmentalized Signaling of GPCRs"
11:35 am - 11:40 am
Discussion
11:40 am - 12:00 pm
Andrew Kruse (Harvard Medical School, USA)
"Structural Basis for Rapid Desensitization of GPCR Signaling"
12:00 pm - 12:05 pm
Discussion
12:05 pm - 12:25 pm
Mertixell Canals (University of Nottingham, United Kingdom)
"GPCR Signaling in Time and Space"
12:25 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
3:00 pm - 4:00 pm
The GRC Power Hour™
The GRC Power Hour™ is designed to address challenges women face in science and issues of diversity and inclusion. The program supports the professional growth of all members of our communities by providing an open forum for discussion and mentoring.
Organizers: Martine Smit (Vrije Universiteit Amsterdam, The Netherlands) and JoAnn Trejo (University of California, San Diego, USA)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Biased Signaling
Biased receptors/biased agonism - going in vivo to address functional selectivity, context or just selectivity.
Discussion Leader: Terry Kenakin (University of North Carolina School of Medicine, USA)
7:30 pm - 7:55 pm
Jonathan Javitch (Columbia University / New York State Psychiatric Institute, USA)
"Single Molecule Analysis of GPCR Coupling in Living Cells"
7:55 pm - 8:00 pm
Discussion
8:00 pm - 8:20 pm
Evi Kostenis (University of Bonn, Germany)
"Biased GPCR Signaling: Progress, Prospects and a Fresh Perspective"
8:20 pm - 8:25 pm
Discussion
8:25 pm - 8:45 pm
Jurgen Wess (National Institute of Diabetes and Digestive and Kidney Diseases, NIH, USA)
"In Vivo Metabolic Roles of Distinct G Protein- and β-Arrestin-Dependent Signaling Pathways"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:10 pm
Andrew Tobin (University of Glasgow, United Kingdom)
"GPCRs: Opening the Gateway to Pathways that Prevent Neurodegeneration"
9:10 pm - 9:15 pm
Discussion
9:15 pm - 9:25 pm
Magdalena Korczynska (University of California, San Francisco, USA)
"Screening Complex Mega and Giga Compound Libraries by Docking"
9:25 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Group Photo
9:00 am - 12:30 pm
Opiate and Non-Opiate Analgesics
Identifying the issues with classical opiate and non-analgesics and discussing mechanisms and novel therapeutics.
Discussion Leader: Brigitte Kieffer (Douglas Hospital Research Centre, McGill University, Canada)
9:00 am - 9:25 am
Wolfgang Sadee (The Ohio State University, USA)
"Neutral Antagonists at MOR and Opportunities for Treating Neonatal Abstinence Withdrawal Syndromes"
9:25 am - 9:30 am
Discussion
9:30 am - 9:55 am
Debbie Hay (The University of Auckland, New Zealand)
"Molecular Pharmacology of CGRP Receptors: Migraine and Beyond"
9:55 am - 10:00 am
Discussion
10:00 am - 10:20 am
Arthur Christopoulos (Monash University, Australia)
"Tone-Specific Pharmacology: GPCR Allosteric Modulators for Targeting Pain"
10:20 am - 10:25 am
Discussion
10:25 am - 11:00 am
Coffee Break
11:00 am - 11:25 am
Andrea Hohmann (Indiana University, USA)
"Mechanisms of CB2 Receptor-Induced Analgesia"
11:25 am - 11:30 am
Discussion
11:30 am - 11:50 am
Nurulain Zaveri (Astraea Therapeutics, USA)
"NOP/MOP Bifunctional Non-Addicting Analgesics for Opioid Crisis"
11:50 am - 11:55 am
Discussion
11:55 am - 12:05 pm
Aashish Manglik (University of California, San Francisco, USA)
"Structural Bases of μ-Opioid Receptor (MOPr) Activation and Coupling"
12:05 pm - 12:10 pm
Discussion
12:10 pm - 12:30 pm
General Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
New Tools for GPCRs as Therapeutic Targets for Neurological Disorders
Novel strategies and progress in drug development for neurological disorders.
Discussion Leader: Marta Filizola (Icahn School of Medicine at Mount Sinai, USA)
7:30 pm - 7:55 pm
Ehud Isacoff (University of California, Berkeley, USA)
"Optical Probing of Neuromodulatory GPCRs"
7:55 pm - 8:00 pm
Discussion
8:00 pm - 8:25 pm
Philippe Rondard (CNRS / INSERM, France)
"Activation and Allosteric Modulation of Neuroreceptors"
8:25 pm - 8:30 pm
Discussion
8:30 pm - 8:55 pm
Rob Leurs (Vrije Universiteit Amsterdam, The Netherlands)
"Photopharmacology of G Protein-Coupled Receptor Signaling"
8:55 pm - 9:00 pm
Discussion
9:00 pm - 9:10 pm
Alisa Glukhova (Monash Institute of Pharmaceutical Sciences, Monash University, Australia)
"Insights into the Selectivity of Adenosine Receptors"
9:10 pm - 9:15 pm
Discussion
9:15 pm - 9:30 pm
General Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Atypical GPCRs: Adhesion and Deorphanized GPCR Superfamily Members
Recent developments in figuring out what some of the GPRx family members do.
Discussion Leader: Olivier Civelli (University of California, Irvine, USA)
9:00 am - 9:25 am
Graeme Milligan (University of Glasgow, United Kingdom)
"Chemogenetic Approaches to Validate Poorly Characterized GPCRs"
9:25 am - 9:30 am
Discussion
9:30 am - 9:55 am
Brigitte Kieffer (Douglas Hospital Research Centre, McGill University, Canada)
"New Players in Neurological Functions: GPR88"
9:55 am - 10:00 am
Discussion
10:00 am - 10:20 am
Frederic Bassilana (Novartis Institutes for BioMedical Research, Switzerland)
"Finding Receptors for Bioactive Molecules"
10:20 am - 10:25 am
Discussion
10:25 am - 10:50 am
Coffee Break
10:50 am - 11:10 am
William Weis (Stanford University School of Medicine, USA)
"Force-Dependent Allostery in Cell-Cell Adhesion"
11:10 am - 11:15 am
Discussion
11:15 am - 11:35 am
Demet Arac (University of Chicago, USA)
"Structural and Functional Studies of Adhesion GPCRs and Their Ligands"
11:35 am - 11:40 am
Discussion
11:40 am - 12:00 pm
Xianhua Piao (University of California, San Francisco, USA)
"Adhesion GPCR-Mediated Cell-Matrix Interaction in Neural Development"
12:00 pm - 12:05 pm
Discussion
12:05 pm - 12:25 pm
Gregory Tall (University of Michigan, USA)
"Collagen Regulation of a New GPR56-Directed Signaling Process"
12:25 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:00 pm - 7:30 pm
Business Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
7:30 pm - 9:30 pm
Systems and Proteomics
Recent development in data mining, the implications of drug development, and their influence on complex signaling pathways.
Discussion Leader: J. Silvio Gutkind (University of California, San Diego, USA)
7:30 pm - 7:50 pm
Ruth Huttenhain (University of California, San Francisco, USA)
"An Approach for Spatiotemporally Resolving GPCR Protein Interaction Networks Regulating Receptor Signaling"
7:50 pm - 7:55 pm
Discussion
7:55 pm - 8:15 pm
Chad Myers (University of Minnesota, USA)
"Genome-Wide Discovery of New Microbial Molecular Probes from Chemical Genetic Interactions"
8:15 pm - 8:20 pm
Discussion
8:20 pm - 8:40 pm
Bryan Roth (University of North Carolina at Chapel Hill, USA)
"Illuminating the Dark Corridors of the GPCR-ome"
8:40 pm - 8:45 pm
Discussion
8:45 pm - 9:05 pm
Heidi Hamm (Vanderbilt University, USA)
"Regulation of Exocytosis by Inhibitory GPCRs and Gβγ Subunits"
9:05 pm - 9:10 pm
Discussion
9:10 pm - 9:25 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"
9:25 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
How Form and Function Are Tightly Linked in GPCRs
How structures continue to provide mechanistic insight; high resolution structure determination by x-ray diffraction and cryoEM; how structures finally help drug design; GPCRs as moving pictures: more than telling a thousand words.
Discussion Leader: Tracy Handel (University of California, San Diego, USA)
9:00 am - 9:25 am
Klaus-Peter Hofmann (Institute of Medical Physics and Biophysics, Charité - Universitätsmedizin Berlin, Germany)
"Multiple Conformations of Photoactivated Rhodopsin: Role in Signal Transduction"
9:25 am - 9:30 am
Discussion
9:30 am - 9:55 am
Brian Kobilka (Stanford University, USA)
"The Role of GPCR Dynamic in Signaling"
9:55 am - 10:00 am
Discussion
10:00 am - 10:25 am
Christopher Tate (Medical Research Council, United Kingdom)
"The Molecular Basis for High-Affinity Agonist Binding at the β1-Adrenoceptor"
10:25 am - 10:30 am
Discussion
10:30 am - 10:40 am
Joshua Ziarek (Indiana University, USA)
"Probing Conformational Dynamics by Solution NMR"
10:40 am - 10:45 am
Discussion
10:45 am - 11:10 am
Coffee Break
11:10 am - 11:35 am
Irina Kufareva (UC San Diego Skaggs School of Pharmacy and Pharmaceutical Sciences, USA)
"Structural Basis for CXCR Signaling Illuminated by Experimental and Computational Approaches"
11:35 am - 11:40 am
Discussion
11:40 am - 12:00 pm
Arun Shukla (Indian Institute of Technology, India)
"Structural and Functional Diversity in Receptor-Arrestin Complexes"
12:00 pm - 12:05 pm
Discussion
12:05 pm - 12:25 pm
Denise Wootten (Monash Institute of Pharmaceutical Sciences, Monash University, Australia)
"Structural Insights into Class B GPR Signalling and Allostery"
12:25 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: Innovative Drug Screening and Design Approaches
Computational and novel methodologies and good old fashioned medicinal chemistry - repurposing GPCR drugs for disease: new life as anti-cancer therapeutics.
Discussion Leader: Brian Shoichet (University of California, San Francisco, USA)
7:30 pm - 7:50 pm
Brian Paegel (The Scripps Research Institute, USA)
"DNA-Encoded Libraries for Drug Discovery"
7:50 pm - 7:55 pm
Discussion
7:55 pm - 8:15 pm
Vsevolod Katritch (University of Southern California, USA)
"Structure-Based Virtual Ligand Screening and Design for New GPCR Probes"
8:15 pm - 8:20 pm
Discussion
8:20 pm - 8:40 pm
Peter Gmeiner (Friedrich-Alexander University Erlangen-Nürnberg, Germany)
"Structure-Guided Strategies: How to Find Useful GPCR Ligands"
8:40 pm - 8:45 pm
Discussion
8:45 pm - 9:10 pm
Robert Lefkowitz (Howard Hughes Medical Institute / Duke University Medical Center, USA)
"From Binding to Biophysics: My 50 Years (and Counting) of GPCR Research"
9:10 pm - 9:15 pm
Discussion
9:15 pm - 9:25 pm
Laura Wingler (Duke University Medical Center, USA)
"Molecular Mechanisms of Biased Agonism at the Angiotensin Receptor"
9:25 pm - 9:30 pm
Discussion
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure
